WO2020254940A1 - Glucose sustained release compositions and it's process - Google Patents
Glucose sustained release compositions and it's process Download PDFInfo
- Publication number
- WO2020254940A1 WO2020254940A1 PCT/IB2020/055573 IB2020055573W WO2020254940A1 WO 2020254940 A1 WO2020254940 A1 WO 2020254940A1 IB 2020055573 W IB2020055573 W IB 2020055573W WO 2020254940 A1 WO2020254940 A1 WO 2020254940A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- sustained release
- pellets
- film coated
- release
- glucose
- Prior art date
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- 238000007796 conventional method Methods 0.000 description 1
- 230000018044 dehydration Effects 0.000 description 1
- 238000006297 dehydration reaction Methods 0.000 description 1
- 229940111833 dex4 Drugs 0.000 description 1
- 230000001079 digestive effect Effects 0.000 description 1
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
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- 230000004110 gluconeogenesis Effects 0.000 description 1
- 125000002791 glucosyl group Chemical group C1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)* 0.000 description 1
- 229940096919 glycogen Drugs 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 235000012907 honey Nutrition 0.000 description 1
- 230000002218 hypoglycaemic effect Effects 0.000 description 1
- 239000012729 immediate-release (IR) formulation Substances 0.000 description 1
- 239000012535 impurity Substances 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 230000000873 masking effect Effects 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 150000004682 monohydrates Chemical group 0.000 description 1
- 230000036651 mood Effects 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- 210000000663 muscle cell Anatomy 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 239000002357 osmotic agent Substances 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 229940093429 polyethylene glycol 6000 Drugs 0.000 description 1
- 235000021067 refined food Nutrition 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 238000009491 slugging Methods 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- 238000005563 spheronization Methods 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 235000015961 tonic Nutrition 0.000 description 1
- 230000001256 tonic effect Effects 0.000 description 1
- 229960000716 tonics Drugs 0.000 description 1
- DBRXOUCRJQVYJQ-CKNDUULBSA-N withaferin A Chemical compound C([C@@H]1[C@H]([C@@H]2[C@]3(CC[C@@H]4[C@@]5(C)C(=O)C=C[C@H](O)[C@@]65O[C@@H]6C[C@H]4[C@@H]3CC2)C)C)C(C)=C(CO)C(=O)O1 DBRXOUCRJQVYJQ-CKNDUULBSA-N 0.000 description 1
Classifications
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Definitions
- the present invention specifically relates to sustained release carbohydrate oral compositions.
- the present invention relates to compositions of sustained release glucose oral film coated tablets, film coated pellets, sachets, minitablets, pellets and powder for suspension
- the present invention also relates to compositions of sustained release glucose oral film coated tablets, film coated pellets, sachets, minitablets, pellets, powder for suspension comprising dextrose monohydrate as active ingredient and pharmaceutically acceptable excipients.
- the present invention also relates to compositions of sustained release glucose oral film coated tablets, film coated pellets, sachets, minitablets, pellets, powder for suspension comprising dextrose monohydrate and pharmaceutically acceptable excipients to ensure continuous energy.
- the present invention also relates to simple process for the preparation of glucose oral sustained release film coated tablets and film coated pellets by using simple direct compression process comprising mainly the steps of sifting, blending, compressing and film coating.
- the present invention also relates to simple process for the preparation of glucose oral sustained release minitablets and pellets by using simple direct compression process comprising the steps of sifting, dissolving, drying, blending and compressing.
- the present invention also relates to simple process for the preparation of glucose oral sustained release sachets and powder for suspension comprising the steps of sifting, drying, coating and blending.
- Carbohydrates are absorbed especially quickly as a single component, the monosaccharide known as glucose or dextrose. In many foods, however, glucose is not present in this unbound, easily absorbed form, but in complex structures instead.
- the carbohydrates consumed through food are broken down into individual components in the digestive tract-with glucose as the main product of this process. This kind of conversion takes time, however.
- the glucose now travels into the bloodstream via the small intestine. Once there, it appears in the form of blood glucose and is transported to the cells, where it is finally converted into energy. Now it is available for the brain and muscles.
- Glucose that is not used right away is stored in the muscle cells and the liver in a special form called glycogen.
- Glucose is one of the group of carbohydrates known as simple sugars (monosaccharides). Glucose (from Greek glykys;“sweet”) has the molecular formula C 6 H 12 0 6 . It is found in fruits and honey and is the major free sugar circulating in the blood of higher animals. It is the source of energy in cell function, and the regulation of its metabolism is of great importance (see fermentation; gluconeogenesis). Molecules of starch, the major energy-reserve carbohydrate of plants, consist of thousands of linear glucose units. Another major compound composed of glucose is cellulose, which is also linear. Dextrose is the molecule D-glucose. Dextrose Monohydrate is the monohydrate form of D-glucose, a natural monosaccharide and carbohydrate. Dextrose serves to replenish lost nutrients and electrolytes. It has a structural formula of;
- US 6,451,122 discloses dextrose in powder form, characterized in that it has a dextrose content at least equal to 99%, a a crystalline form content at least equal to 95%, a water content at most equal to 1% and a compressibility, determined according to a test A, at least equal to 80 N, preferably in the range 100 N and 200 N. It also discloses dextrose in powder form favours its use in applications of tablets to be sucked, chewed, dissolved, and swallowed.
- US 6,881,432 discloses dextrose hydrate in powder form, having a dextrose content at least equal to 98%, an a crystalline form content at least equal to 95%, a water content greater than 1%, a compressibility determined according to a test A, at least equal to 70 N.
- US 2013/0075948 discloses direct compressible dextrose composition, a process for preparing such a direct compressible dextrose composition by compression and subsequent granulation, and processes for preparing pharmaceutical formulations or food formulations in tablet form using the direct compressible dextrose composition. It also discloses that dextrose composition is compacted by roller compaction to form flakes or by slugging using a tablet press to form slugs, crushing the flakes or the slugs to form granules; and screening the granules to obtain a direct compressible dextrose composition in the form of granules with a given particle size distribution.
- Dextrose tablets are available in the market like Dextro Energy, Dex4 ® , Vitalp Raspberry Dextrose Tablets, DextroCare etc.
- dextrose is used to provide energy; dextrose tablets are available in market having immediate release profile.
- the content of dextrose in powder form is at least equal to 99%, process for preparing direct compressible dextrose composition using roller compaction.
- the inventors of present invention provide compositions of sustained release glucose oral film coated tablets, film coated pellets, sachets, minitablets, pellets, powder for suspension comprising dextrose monohydrate as active ingredient and pharmaceutically acceptable excipients.
- the inventors of present invention provide simple process for the preparation of glucose oral sustained release film coated tablets and film coated pellets by using simple direct compression process comprising mainly the steps of sifting, blending, compressing and film coating.
- the inventors of present invention also provide simple process for the preparation of glucose oral sustained release minitablets and pellets by using simple direct compression process comprising the steps of sifting, dissolving, drying, blending and compressing.
- the inventors of present invention also provide simple process for the preparation of glucose oral sustained release sachets and powder for suspension comprising the steps of sifting, drying, coating and blending.
- the main objective of the present invention is to provide sustained release carbohydrate oral compositions.
- Another objective of the present invention compositions of sustained release glucose oral film coated tablets, film coated pellets, sachets, minitablets, pellets and powder for suspension.
- Another objective of the present invention is to provide compositions of sustained release glucose oral film coated tablets, film coated pellets, sachets, minitablets, pellets, powder for suspension comprising dextrose monohydrateas active ingredient and pharmaceutically acceptable excipients.
- Still another objective of the present invention is to provide sustained release glucose oral film coated tablets composition comprising dextrose monohydrate as carbohydrate and diluent, lubricant, release-controlling polymer, coating solution, plasticizer as pharmaceutically acceptable excipients to ensure continuous energy.
- Still another objective of the present invention is to provide simple process for the preparation of glucose oral sustained release minitablets, and pellets by using simple direct compression process comprising the steps of sifting, dissolving, drying, blending and compressing.
- Still another objective of the present invention is to provide simple process for the preparation of glucose oral sustained release sachets and powder for suspension comprising the steps of sifting, drying, coating and blending.
- Still another objective of the present invention is to provide continuous energy for a longer duration by the administration of sustained release glucose pellets, film coated oral tablets, film coated pellets, sachets, minitablets and powder for suspension SUMMARY OF INVENTION
- compositions of sustained release glucose oral dosage forms useful in providing continuous energy for a longer duration.
- the present invention provides compositions of sustained release glucose oral film coated tablets, film coated pellets, minitablets, powder for suspension, sachets and pellets useful in providing continuous energy for a longer duration.
- the present invention provides sustained release glucose oral film coated tablets, film coated pellets, minitablets, powder for suspension, sachets, pellets compositions comprising carbohydrate as active ingredient and pharmaceutically acceptable excipients.
- the present invention provides sustained release glucose oral film coated tablets composition
- dextrose monohydrate as carbohydrate and diluent, lubricant, coating solution as pharmaceutically acceptable excipients to ensure continuous energy.
- the present invention provides sustained release glucose oral film coated pellets composition
- dextrose monohydrate as carbohydrate and diluent, release-controlling polymer, lubricant, solvent, coating solution as pharmaceutically acceptable excipients to ensure continuous energy.
- the present invention provides composition of sustained release glucose oral minitablets and pellets comprising dextrose monohydrate as carbohydrate and diluent, release-controlling polymers, disintegrant, binder, lubricant as pharmaceutically acceptable excipients to ensure continuous energy.
- the present invention provides compositions of sustained release glucose sachets and powder for suspension comprising dextrose monohydrate as carbohydrate and diluent, release-controlling polymer, extragranular materials, coating solution as pharmaceutically acceptable excipients to ensure continuous energy.
- the present invention provides sustained release glucose oral film coated tablets composition
- dextrose monohydrate as carbohydrate
- microcrystalline Cellulose PH 102 as diluent
- magnesium stearate as lubricant
- surelease 25% dispersion as coating solution for weight gain of 5%.
- the present invention provides sustained release glucose oral film coated tablets composition
- dextrose monohydrate as carbohydrate
- microcrystalline Cellulose PH-101 microcrystalline Cellulose PH 102 as diluent
- magnesium stearate as lubricant
- Eudragit RS 30D Eudragit RS 30D
- HPMC K4M HPMC K100M
- HPMC E50 release-controlling polymer
- triethyl Citrate as plasticizer.
- the present invention provides sustained release glucose oral film coated pellets composition
- dextrose monohydrate as carbohydrate
- microcrystalline cellulose PH 102 as diluent
- hypromellose E6 premium as release-controlling polymer
- magnesium stearate as lubricant
- purified water as solvent
- surelease 25% dispersion as coating solution for weight gain of 3%, 5% and 7%.
- the present invention provides composition of sustained release glucose oral minitablets, and pellets comprising dextrose monohydrate as carbohydrate, microcrystalline Cellulose PH-102 and maize starch as diluent, hypromellose K100LV CR, hypromellose K4M CR, HPMC K4M, HPMC K100M as release-controlling polymers, croscarmellose sodium as disintegrant, povidone K-30 as binder and magnesium stearate as lubricant.
- the present invention provides simple process for the preparation of glucose oral sustained release film coated tablets and film coated pellets by using simple direct compression process comprising mainly the steps of sifting, blending, compressing and film coating.
- the present invention provides simple process for the preparation of glucose oral sustained release minitablets, and pellets by using simple direct compression process comprising the steps of sifting, dissolving, drying, blending and compressing.
- the present invention provides simple process for the preparation of glucose oral sustained release sachets and powder for suspension comprising the steps of sifting, drying, coating and blending.
- the present invention provides sustained release dosage form composition comprising:
- the present invention provides sustained release film coated oral tablets composition comprising:
- the present invention provides sustained release film coated pellets composition comprising:
- the present invention provides sustained release minitablet and pellet compositions comprising:
- the present invention provides sustained release sachets and powder for suspension compositions comprising:
- the present invention provides a simple process for the preparation of provides glucose sustained release oral film coated tablets, film coated pellets, minitablets, powder for suspension, pellets, sachets by using simple direct compression process which is cost effective, stable, less wear & tear of punches, simplified validation and requires fewer excipients.
- the present invention provides a process for preparing sustained oral release film coated tablets, the process comprising the steps of:
- step (b) sifting lubricant through # 60 mesh, adding to step (a) and blending for 5 minutes, (c) compressing the lubricated blend using compression machine having 4.75 mm tablet punches, and
- coating solution of which is prepared by dispersing 100 gm of surelease aqueous dispersion in 120 gm of water under stirring to obtain film coated tablets.
- the present invention provides a process for preparing sustained release film coated pellets, the process comprising the steps of:
- step (c) drying the obtained wet granules of step (b) and blending with lubricant
- the present invention provides a process for preparing sustained release minitablets and pellets, the process comprising the steps of:
- step (c) drying the obtained wet granules of step (b) and blending with lubricant
- the present invention provides a process for preparing glucose oral sustained release sachets and powder for suspension, the process comprising the steps of:
- step (b) sprinkling little water to prepare wet mass and passing through # 20 mesh, (c) drying the obtained wet granules of step (b) and coating the obtained granules using coating solution which is prepared by dispersing 100 gm of surelease aqueous dispersion in 120 gm of water under stirring to obtain coated granules, and
- the present invention provides a process for preparing glucose oral sustained release film coated tablets, the process comprising the steps of:
- step (b) sifting magnesium stearate through # 60 mesh, adding to step (a) and blending for 5 minutes,
- the present invention provides a process for preparing glucose oral sustained release film coated pellets, the process comprising the steps of:
- step (c) drying the obtained wet granules of step (b) and blending with magnesium stearate,
- the present invention provides a process for preparing sustained release minitablets and pellets, the process comprising the steps of:
- step (c) drying the obtained wet granules of step (b) and blending with magnesium stearate, and
- the present invention provides a process for preparing glucose oral sustained release film coated tablets, the process comprising the steps of:
- step (c) drying the obtained wet granules of step (b) and coating the obtained granules using coating solution which is prepared by dispersing 100 gm of surelease aqueous dispersion in 120 gm of water under stirring to obtain coated granules, and
- active ingredients of the present invention is used to provide continuous energy for a longer duration.
- active ingredient is carbohydrate.
- active ingredient is dextrose.
- the present invention provides sustained release glucose oral film coated tablets, film coated pellets, minitablets, pellets comprising carbohydrate as active ingredient and pharmaceutically acceptable excipients.
- the present invention provide sustained release glucose oral film coated tablets composition
- dextrose monohydrate as carbohydrate and diluent, lubricant, coating solution as pharmaceutically acceptable excipients to ensure continuous energy.
- the present invention provide sustained release glucose oral film coated pellets composition
- dextrose monohydrate as carbohydrate and diluent, release controlling polymer, lubricant, solvent, coating solution as pharmaceutically acceptable excipients to ensure continuous energy.
- the present invention provide sustained release glucose oral film coated pellets composition
- active ingredient diluent, release-controlling polymer, solvent in intra granular components and lubricant in extra granular component.
- the present invention provide sustained release glucose oral minitablets, and pellets compositions comprising dextrose monohydrate as carbohydrate and diluent, release-controlling polymers, disintegrant, binder, lubricant as pharmaceutically acceptable excipients to ensure continuous energy.
- the present invention provides compositions of sustained release glucose sachets and powder for suspension comprising dextrose monohydrate as carbohydrate and diluent, release-controlling polymer, extragranular materials, coating solution as pharmaceutically acceptable excipients to ensure continuous energy.
- Dextrose is the name of a simple sugar that is made from corn and is chemically identical to glucose, or blood sugar. Simple sugars can raise blood sugar levels very quickly, and they often lack nutritional value. Dextrose is often used in baking products as a sweetener, and can be commonly found in items such as processed foods and corn syrup. Dextrose also has medical purposes. It is dissolved in solutions that are given intravenously, which can be combined with other drugs, or used to increase blood sugar. Dextrose is used in various concentrations for different purposes. For example, dextrose is used as an IV solution in case of dehydration and low blood sugar. Dextrose IV solutions can also be combined with many drugs, for IV administration. Dextrose gel or tablets are used in diabetes or hypoglycaemic patients having low blood sugar.
- Diluents may be selected from any such pharmaceutically acceptable excipients, which give bulk to the composition and improve compressibility.
- Diluent used in glucose oral film coated tablets and film coated pellets compositions of the present invention include, but are not limited to starch and starch derivatives like corn starch, potato starch, wheat starch, maize starch, pregelatinized starch, dicalcium phosphate, calcium phosphate tribasic, calcium carbonate, calcium sulphate, sorbitol, microcrystalline cellulose, lactose, lactose anhydrous, lactose monohydrate, spray dried lactose, glucose, mannitol, alginates, alkali earth metal salts, clay, polyethylene glycols or similar materials.
- Preferably used diluent in glucose oral film coated tablets and film coated pellets is selected from microcrystalline Cellulose PH-101, microcrystalline cellulose PH-102.
- Preferably used diluent in mini tablets and pellets is selected from microcrystalline Cellulose PH-102 maize starch.
- Preferably used diluent in sachets and powder for suspension is microcrystalline cellulose PH- 102.
- Release-controlling polymer used in glucose film coated pellets, minitablets and pellets compositions of the present invention include, but are not limited to methylcellulose, ethylcellulose, hydroxyethylcellulose, propylcellulose, hydroxypropylcellulose, hydroxypropyl methylcellulose (hypromellose), hypromellose E6 premium, hypromellose K100LV CR, hypromellose K4M CR, carboxymethylcellulose, polymethyl methacrylate, polyethyl methacrylate, polybutyl methacrylate, polyisobutyl methacrylate, polyhexyl methacrylate, polyisodecyl methacrylate, polylauryl methacrylate, polyphenyl methacrylate, polymethyl acrylate, polyisopropyl acrylate, polyisobutyl acrylate, polyoctadecyl acrylate, polyethylene, polypropylene, polyethylene oxide, polyethylene terephthalate, polyviny
- Preferably used release-controlling polymer in glucose film coated tablets and glucose film coated pellets is selected from Eudragit RS 30D, HPMC K4M, HPMC K100M, HPMC E50 and hypromellose E6 premium.
- Preferably used release-controlling polymer in glucose minitablets and pellets are HPMC K4M, HPMC K100M, HPMC E3, Eudragit RS 30D, hypromellose K100LV CR and hypromellose K4M CR.
- Disintegrants used in the composition of the present invention include, but are not limited to low substituted hydroxypropyl cellulose (L-HPC), sodium starch glycolate, sodium croscarmellose, cross-linked polyvinylpyrrolidone, soy polysaccharide, cross-linked alginic acid, gellan gum, xanthan gum, calcium silicate and ion exchange resin.
- L-HPC low substituted hydroxypropyl cellulose
- sodium starch glycolate sodium croscarmellose
- cross-linked polyvinylpyrrolidone soy polysaccharide
- cross-linked alginic acid gellan gum
- xanthan gum calcium silicate and ion exchange resin
- croscarmellose croscarmellose
- Lubricants used in the composition of the present invention include, but are not limited to talc, magnesium stearate, other alkali earth metal stearates like zinc, calcium stearate etc; sodium lauryl sulphate, hydrogenated vegetable oil, sodium benzoate, sodium stearyl fumarate, glyceryl monostearate, polyethylene glycol and similar materials.
- Preferably used lubricant is magnesium stearate.
- Binders used in the compositions of present invention include, but not limited to sugars such as starch (potato starch, corn starch, wheat starch), sucrose, glucose, dextrose, lactose, maltodextrin, methylene dichloride, natural and synthetic gums (e.g. acacia), gelatin, cellulose derivatives (e.g. microcrystalline cellulose, HPC, HEC, HPMC, carboxymethyl cellulose, methyl cellulose, ethyl cellulose), polyvinylpyrrolidone, polyethyleneglycols, waxes, calcium carbonate, calcium phosphate.
- sugars such as starch (potato starch, corn starch, wheat starch), sucrose, glucose, dextrose, lactose, maltodextrin, methylene dichloride, natural and synthetic gums (e.g. acacia), gelatin, cellulose derivatives (e.g. microcrystalline cellulose, HPC, HEC, HPMC, carboxymethyl
- extragranular material used in sachets and powder for suspension includes but not limited to mannitol, sucralose, citric acid anhydrous, orange flavour, strawberry flavour, talc and sucrose.
- Coating solution may be selected from any such pharmaceutically acceptable excipients, which give film coating to the tablet for sustained release.
- Preferably used coating solution is surelease 25% dispersion.
- Surelease ® aqueous ethylcellulose dispersion is used for modified release and taste masking applications.
- Film coating used in the present invention is prepared by dispersing 25% surelease aqueous dispersion in 120 gm of water under stirring.
- Sustained release glucose film coated tablets, film coated pellets, minitablets and pellets of the present invention has been prepared by using direct compression which is cost effective, stable, less wear & tear of punches, simplified validation and requires fewer excipients.
- Sustained release glucose film coated tablets, film coated pellets, minitablets, powder for suspension, sachets and pellets of the present invention is used to provide continuous release of energy, supports endurance, management of stress, fatigue and suitable for diabetic patients.
- Sustained release film coated tablets and film coated pellets by using simple direct compression process comprising mainly the steps of sifting, blending, compressing and film coating.
- Sustained release minitablets, and pellets by using simple direct compression process comprising the steps of sifting, dissolving, drying, blending and compressing.
- Sustained release sachets and powder for suspension comprising the steps of sifting, drying, coating and blending.
- Sustained release glucose film coated tablets, powder for suspension, sachets, film coated pellets, minitablet and pellets of the present invention provides continuous release of Dextrose for a period of 30 to 240 minutes.
- Sustained release film coated tablets of glucose can be fortified with adoptogens like ashwagandha, brain tonics like brahmi, phosphatidyl serine, gensing, mood elevators like caffeine etc.
- the present invention provides composition of sustained release glucose oral film coated tablets composition
- composition comprising dextrose monohydrate as carbohydrate, microcrystalline Cellulose PH 102 as diluent, magnesium stearate as lubricant and surelease 25% dispersion as coating solution for weight gain of 5%.
- the present invention is to provide sustained release glucose oral film coated tablets composition
- dextrose monohydrate as carbohydrate
- microcrystalline Cellulose PH-101 microcrystalline Cellulose PH 102 as diluent
- magnesium stearate as lubricant
- Eudragit RS 30D Eudragit RS 30D
- HPMC K4M HPMC K100M
- HPMC E50 release-controlling polymer
- triethyl citrate as plasticizer.
- the present invention provides composition of sustained release glucose oral film coated pellets composition
- composition comprising dextrose monohydrate as carbohydrate, microcrystalline cellulose PH 102 as diluent, hypromellose E6 premium as release controlling polymer, magnesium stearate as lubricant, purified water as solvent and surelease 25% dispersion as coating solution for weight gain of 3%, 5% and 7%.
- the present invention provides composition of sustained release glucose oral film coated pellets composition
- composition comprising dextrose monohydrate, microcrystalline cellulose PH 102, hypromellose E6 premium, purified water in intra granular components and magnesium stearate in extra granular component.
- the present invention provides composition of sustained release glucose oral minitablets and pellets comprising dextrose monohydrate as carbohydrate, microcrystalline Cellulose PH-102 and maize starch as diluent, hypromellose K100LV CR, hypromellose K4M CR, HPMC K4M, HPMC K100M as release-controlling polymers, croscarmellose sodium as disintegrant, povidone K-30 as binder and magnesium stearate as lubricant.
- the present invention is to provide composition of sustained release glucose oral sachets and powder for suspension comprising dextrose monohydrate as carbohydrate, microcrystalline cellulose PH-102 as diluent, Eudragit RS PO, Hypromellose E6 premium as release-controlling polymers, mannitol, sucralose, citric acid anhydrous, orange flavour, strawberry flavour, talc, sucrose as extragranular materials, Surelease 25% dispersion as coating solution.
- the invention disclosed herein is process for the preparation of sustained release pellets and film coated tablets of glucose useful to ensure continuous energy.
- Weight of each tablet is 110.00 mg
- Dextrose monohydrate and microcrystalline cellulose PH-102 were co-sifted through 40# and Loaded in GPCG.
- Binder solution prepared using Eudragit RS 30D with
- Plasticizer Triethyl Citrate Polymeric dispersion sprayed into above dry mix materials at product temperature 30°C. The dried granules sifted through 24# and lubricated with Magnesium Stearate for 5 minutes. Lubricated blend was compressed into tablet using compression machine with suitable punch tooling.
- Weight of each tablet is 100.00 mg
- Dextrose monohydrate, Microcrystalline cellulose PH-102, HPMC K4M and HPMC K100M were co-sifted through 30# and Loaded into blender and Blended for 30 minutes and lubricated with Magnesium Stearate for 5 minutes. Lubricated blend was compressed into tablet using compression machine with suitable punch tooling.
- Weight of each film tablet is 75.60 mg Manufacturing process
- Dextrose monohydrate and microcrystalline cellulose PH-102 were co-sifted through # 40 mesh and blended for 30 minutes.
- Magnesium stearate is sifted through # 60 mesh, added to the above obtained blend and blended for 5 minutes.
- Lubricated blend was compressed into tablet using compression machine. 100 gm of 25% surelease aqueous dispersion was dispersed in 120 gm of water and stirred for 45 minutes at 1600-1800 rpm to obtain 5% weight gain of film coating.
- Glucose tablets were coated with surelease 25% dispersion to obtain embedded coated sustained release glucose tablets.
- Weight of each tablet is 85.00 mg
- Dextrose monohydrate and microcrystalline cellulose PH-102 were co-sifted through # 40 mesh and blended for 30 minutes.
- Magnesium stearate is sifted through # 60 mesh, added to the above obtained blend and blended for 5 minutes.
- Lubricated blend was compressed into tablet using compression machine.
- Coating dispersion was prepared HPMC E50, Polyethylene Glycol 6000, Purified Talc and Ti02 with purified water stirred for 45 minutes. Glucose tablets were coated with dispersion to obtain embedded coated sustained release glucose tablets.
- Weight of mini tablet is 5.00 mg
- Dextrose monohydrate, Microcrystalline cellulose PH-102, HPMC K4M and HPMC K100M were co-sifted through 30# and Loaded into blender and Blended for 30 minutes and lubricated with Magnesium Stearate for 5 minutes. Lubricated blend was compressed into tablet using compression machine with 2 mm tooling.
- Weight of each sustained release mini tablet is 760 mg
- Dextrose monohydrate, maize starch, hypromellose K100LV CR, hypromellose K4M CR, croscarmellose sodium were co-sifted through # 30 mesh and mixed well.
- Povidone K-30 was dissolved in purified water and wet mass was prepared by adding sifted blend. Passed through # 20 mesh. Dried the wet granules and blended with magnesium stearate. Lubricated blend was compressed using 4.5 mm tablet punches to obtain sustained release glucose minitablets.
- Dextrose monohydrate, Microcrystalline cellulose PH-102 were co-sifted through 30# and Pellets were prepared using HPMC E3 binder solution using extrusion and spheronization technique. Then Dextrose pellets were loaded into GPCG and Polymer coating done using Eudragit RS 30D coating dispersion.
- Weight of each film coated pellet of 3% weight gain is 20.6 mg.
- Weight of each film coated pellet of 5% weight gain is 21.00 mg
- Weight of each film coated pellet of 7% weight gain is 21.4 mg.
- Weight of each sustained release pellets is 2000 mg
- Dextrose monohydrate, maize starch, hypromellose K100LV CR, hypromellose K4M CR, croscarmellose sodium were co-sifted through # 30 mesh and mixed well.
- Povidone K-30 was dissolved in purified water and wet mass was prepared by adding sifted blend. Passed through # 20 mesh. Dried the wet granules and blended with magnesium stearate. Lubricated blend was compressed using 3.5 mm tablet punches to obtain sustained release glucose pellets.
- Dextrose monohydrate, Eudragit RS PO were co-sifted through 30# and granulated using Povidone K30 solution. Wet granules were dried and sifted through 40#. Finally, Dextrose granules mixed with extragranular materials and filled in pouches.
- Dextrose monohydrate, microcrystalline cellulose PH 102, hypromellose E6 premium were co-sifted through # 30 mesh.
- Wet mass was prepared by sprinkling little water and passed through # 20 mesh. Dried the wet granules.
- Granules were coated by fluidized bed coating methods using solution which is prepared by dispersing 100 gm of 25% surelease aqueous dispersion in 120 gm of water to obtain sustained release glucose coated granules. The granules were then blended with extragranular materials and packed into pouches / sachets.
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Abstract
The present invention also relates to compositions of sustained release glucose oral film coated tablets, film coated pellets, sachets, minitablets, pellets, powder for suspension comprising dextrose monohydrate and pharmaceutically acceptable excipients to ensure continuous energy. The present invention also relates to simple process for the preparation of glucose oral sustained release film coated tablets and film coated pellets by using simple direct compression process comprising mainly the steps of sifting, blending, compressing and film coating. The present invention also relates to simple process for the preparation of glucose oral sustained release minitablets and pellets by using simple direct compression process comprising the steps of sifting, dissolving, drying, blending and compressing. The present invention also relates to simple process for the preparation of glucose oral sustained release sachets and powder for suspension comprising the steps of sifting, drying, coating and blending.
Description
GLUCOSE SUSTAINED RELEASE COMPOSITIONS AND
IT’S PROCESS
FIELD OF INVENTION
The present invention specifically relates to sustained release carbohydrate oral compositions.
The present invention relates to compositions of sustained release glucose oral film coated tablets, film coated pellets, sachets, minitablets, pellets and powder for suspension
The present invention also relates to compositions of sustained release glucose oral film coated tablets, film coated pellets, sachets, minitablets, pellets, powder for suspension comprising dextrose monohydrate as active ingredient and pharmaceutically acceptable excipients.
The present invention also relates to compositions of sustained release glucose oral film coated tablets, film coated pellets, sachets, minitablets, pellets, powder for suspension comprising dextrose monohydrate and pharmaceutically acceptable excipients to ensure continuous energy.
The present invention also relates to simple process for the preparation of glucose oral sustained release film coated tablets and film coated pellets by using simple direct compression process comprising mainly the steps of sifting, blending, compressing and film coating.
The present invention also relates to simple process for the preparation of glucose oral sustained release minitablets and pellets by using simple direct compression process comprising the steps of sifting, dissolving, drying, blending and compressing.
The present invention also relates to simple process for the preparation of glucose oral sustained release sachets and powder for suspension comprising the steps of sifting, drying, coating and blending.
BACKGROUND OF INVENTION
Every living being needs energy-but none of them can generate it on their own. It has to be taken in from outside. Carbohydrates and most especially glucose (also known as dextrose) play a key role in this process.
Carbohydrates are absorbed especially quickly as a single component, the monosaccharide known as glucose or dextrose. In many foods, however, glucose is not present in this unbound, easily absorbed form, but in complex structures instead.
The carbohydrates consumed through food are broken down into individual components in the digestive tract-with glucose as the main product of this process. This kind of conversion takes time, however. The glucose now travels into the bloodstream via the small intestine. Once there, it appears in the form of blood glucose and is transported to the cells, where it is finally converted into energy. Now it is available for the brain and muscles. Glucose that is not used right away is stored in the muscle cells and the liver in a special form called glycogen.
Glucose is one of the group of carbohydrates known as simple sugars (monosaccharides). Glucose (from Greek glykys;“sweet”) has the molecular formula C6H1206. It is found in fruits and honey and is the major free sugar circulating in the blood of higher animals. It is the source of energy in cell function, and the regulation of its metabolism is of great importance (see fermentation; gluconeogenesis). Molecules of starch, the major energy-reserve carbohydrate of plants, consist of thousands of linear glucose units. Another major compound composed of glucose is cellulose, which is also linear. Dextrose is the molecule D-glucose.
Dextrose Monohydrate is the monohydrate form of D-glucose, a natural monosaccharide and carbohydrate. Dextrose serves to replenish lost nutrients and electrolytes. It has a structural formula of;
US 6,451,122 discloses dextrose in powder form, characterized in that it has a dextrose content at least equal to 99%, a a crystalline form content at least equal to 95%, a water content at most equal to 1% and a compressibility, determined according to a test A, at least equal to 80 N, preferably in the range 100 N and 200 N. It also discloses dextrose in powder form favours its use in applications of tablets to be sucked, chewed, dissolved, and swallowed.
US 6,881,432 discloses dextrose hydrate in powder form, having a dextrose content at least equal to 98%, an a crystalline form content at least equal to 95%, a water content greater than 1%, a compressibility determined according to a test A, at least equal to 70 N. Process for the preparation thereof and the use of said dextrose hydrate in powder form as a sweetener, osmotic agent, nutrient or excipient. It also discloses dextrose hydrate in powder form favours its use in the preparation of tablets to be sucked, chewed, dissolved or swallowed.
US 2013/0075948 discloses direct compressible dextrose composition, a process for preparing such a direct compressible dextrose composition by compression and subsequent granulation, and processes for preparing pharmaceutical formulations or food formulations in tablet form using the direct compressible dextrose composition. It also discloses that dextrose composition is compacted by roller compaction to form flakes or by slugging using a tablet press to form slugs, crushing the flakes or the slugs to form granules; and screening the granules to obtain a direct
compressible dextrose composition in the form of granules with a given particle size distribution.
Dextrose tablets are available in the market like Dextro Energy, Dex4®, Vitalp Raspberry Dextrose Tablets, DextroCare etc.
All the prior art references shows that dextrose is used to provide energy; dextrose tablets are available in market having immediate release profile. The content of dextrose in powder form is at least equal to 99%, process for preparing direct compressible dextrose composition using roller compaction. However, the inventors of present invention provide compositions of sustained release glucose oral film coated tablets, film coated pellets, sachets, minitablets, pellets, powder for suspension comprising dextrose monohydrate as active ingredient and pharmaceutically acceptable excipients. The inventors of present invention provide simple process for the preparation of glucose oral sustained release film coated tablets and film coated pellets by using simple direct compression process comprising mainly the steps of sifting, blending, compressing and film coating. The inventors of present invention also provide simple process for the preparation of glucose oral sustained release minitablets and pellets by using simple direct compression process comprising the steps of sifting, dissolving, drying, blending and compressing. The inventors of present invention also provide simple process for the preparation of glucose oral sustained release sachets and powder for suspension comprising the steps of sifting, drying, coating and blending. OBJECTIVE OF INVENTION
The main objective of the present invention is to provide sustained release carbohydrate oral compositions.
Another objective of the present invention compositions of sustained release glucose oral film coated tablets, film coated pellets, sachets, minitablets, pellets and powder for suspension. Another objective of the present invention is to provide compositions of sustained release glucose oral film coated tablets, film coated pellets, sachets, minitablets, pellets, powder for suspension comprising dextrose monohydrateas active ingredient and pharmaceutically acceptable excipients. Still another objective of the present invention is to provide sustained release glucose oral film coated tablets composition comprising dextrose monohydrate as carbohydrate and diluent, lubricant, release-controlling polymer, coating solution, plasticizer as pharmaceutically acceptable excipients to ensure continuous energy. Still another objective of the present invention is to provide sustained release glucose oral film coated pellets composition comprising dextrose monohydrate as carbohydrate and diluent, release-controlling polymer, lubricant, solvent, coating solution as pharmaceutically acceptable excipients to ensure continuous energy. Still another objective of the present invention is to provide compositions of sustained release glucose oral minitablets and pellets comprising dextrose monohydrate as carbohydrate and diluent, release-controlling polymers, disintegrant, binder, lubricant as pharmaceutically acceptable excipients to ensure continuous energy.
Still another objective of the present invention is to provide compositions of sustained release glucose sachets and powder for suspension comprising dextrose monohydrate as carbohydrate and diluent, release-controlling polymer, extragranular materials, coating solution as pharmaceutically acceptable excipients to ensure continuous energy.
Still another objective of the present invention is to provide simple process for the preparation of glucose oral sustained release film coated tablets and film coated pellets by using simple direct compression process comprising mainly the steps of sifting, blending, compressing and film coating.
Still another objective of the present invention is to provide simple process for the preparation of glucose oral sustained release minitablets, and pellets by using simple direct compression process comprising the steps of sifting, dissolving, drying, blending and compressing.
Still another objective of the present invention is to provide simple process for the preparation of glucose oral sustained release sachets and powder for suspension comprising the steps of sifting, drying, coating and blending. In yet another objective of the present invention is to provide continuous energy for a longer duration by the administration of sustained release glucose pellets, film coated oral tablets, film coated pellets, sachets, minitablets and powder for suspension SUMMARY OF INVENTION
Accordingly, the present invention provides compositions of sustained release glucose oral dosage forms useful in providing continuous energy for a longer duration.
In one embodiment, the present invention provides compositions of sustained release glucose oral film coated tablets, film coated pellets, minitablets, powder for suspension, sachets and pellets useful in providing continuous energy for a longer duration.
In one embodiment, the present invention provides sustained release glucose oral film coated tablets, film coated pellets, minitablets, powder for suspension, sachets, pellets compositions comprising carbohydrate as active ingredient and pharmaceutically acceptable excipients.
In another embodiment, the present invention provides sustained release glucose oral film coated tablets composition comprising dextrose monohydrate as carbohydrate and diluent, lubricant, coating solution as pharmaceutically acceptable excipients to ensure continuous energy.
In another embodiment, the present invention provides sustained release glucose oral film coated pellets composition comprising dextrose monohydrate as carbohydrate and diluent, release-controlling polymer, lubricant, solvent, coating solution as pharmaceutically acceptable excipients to ensure continuous energy.
In another embodiment, the present invention provides composition of sustained release glucose oral minitablets and pellets comprising dextrose monohydrate as carbohydrate and diluent, release-controlling polymers, disintegrant, binder, lubricant as pharmaceutically acceptable excipients to ensure continuous energy.
In another embodiment, the present invention provides compositions of sustained release glucose sachets and powder for suspension comprising dextrose monohydrate as carbohydrate and diluent, release-controlling polymer, extragranular materials, coating solution as pharmaceutically acceptable excipients to ensure continuous energy.
In another embodiment, the present invention provides sustained release glucose oral film coated tablets composition comprising dextrose monohydrate as
carbohydrate, microcrystalline Cellulose PH 102 as diluent, magnesium stearate as lubricant and surelease 25% dispersion as coating solution for weight gain of 5%.
In another embodiment, the present invention provides sustained release glucose oral film coated tablets composition comprising dextrose monohydrate as carbohydrate, microcrystalline Cellulose PH-101, microcrystalline Cellulose PH 102 as diluent, magnesium stearate as lubricant, Eudragit RS 30D, HPMC K4M, HPMC K100M, HPMC E50 as release-controlling polymer and triethyl Citrate as plasticizer.
In another embodiment, the present invention provides sustained release glucose oral film coated pellets composition comprising dextrose monohydrate as carbohydrate, microcrystalline cellulose PH 102 as diluent, hypromellose E6 premium as release-controlling polymer, magnesium stearate as lubricant, purified water as solvent and surelease 25% dispersion as coating solution for weight gain of 3%, 5% and 7%.
In another embodiment, the present invention provides composition of sustained release glucose oral minitablets, and pellets comprising dextrose monohydrate as carbohydrate, microcrystalline Cellulose PH-102 and maize starch as diluent, hypromellose K100LV CR, hypromellose K4M CR, HPMC K4M, HPMC K100M as release-controlling polymers, croscarmellose sodium as disintegrant, povidone K-30 as binder and magnesium stearate as lubricant.
In another embodiment, the present invention provides simple process for the preparation of glucose oral sustained release film coated tablets and film coated pellets by using simple direct compression process comprising mainly the steps of sifting, blending, compressing and film coating.
In another embodiment, the present invention provides simple process for the preparation of glucose oral sustained release minitablets, and pellets by using simple
direct compression process comprising the steps of sifting, dissolving, drying, blending and compressing.
In another embodiment, the present invention provides simple process for the preparation of glucose oral sustained release sachets and powder for suspension comprising the steps of sifting, drying, coating and blending.
In yet another embodiment, the present invention provides sustained release dosage form composition comprising:
(a) 3% to 90%(w/w) of dextrose monohydrate,
(b) 0.5% to 20% (w/w) of diluent,
(c) 0.2% to 40% (w/w) of release-controlling polymer, and
(d) optionally 1 to 10% of coating solution. In yet another embodiment, the present invention provides sustained release film coated oral tablets composition comprising:
(a) 50% to 85%(w/w) of dextrose monohydrate,
(b) 5% to 20% (w/w) of diluent,
(c) 1% to 40% (w/w) of release-controlling polymer
(d) 0.5% to 3%(w/w) of lubricant, and
(e) optionally 1 to 10% of coating solution.
In yet another embodiment, the present invention provides sustained release film coated pellets composition comprising:
(a) 60% to 80% (w/w) of dextrose monohydrate,
(b) 10% to 20% (w/w) of diluent,
(c) 1 % to 10% (w/w) of release-controlling polymer,
(d) 0.5 to 1.0%(w/w) of lubricant, and
(e) 1 to 10% of coating solution.
In yet another embodiment, the present invention provides sustained release minitablet and pellet compositions comprising:
(a) 50% to 90% (w/w) of dextrose monohydrate,
(b) 1% to 10% (w/w) of diluent,
(c) 1% to 40% (w/w) of release-controlling polymers,
(d) 1% to 3% (w/w) of disintegrant,
(e) 1% to 5%(w/w) of binder, and
(f) 0.1% to 3% (w/w) of lubricant. In yet another embodiment, the present invention provides sustained release sachets and powder for suspension compositions comprising:
(a) 2% to 10% of dextrose monohydrate,
(b) 0.1% to 3% of diluent,
(c) 0.1% to 5% of release-controlling polymer, and
(d) 90% to 95% of extragranular material.
In still another embodiment, the present invention provides a simple process for the preparation of provides glucose sustained release oral film coated tablets, film coated pellets, minitablets, powder for suspension, pellets, sachets by using simple direct compression process which is cost effective, stable, less wear & tear of punches, simplified validation and requires fewer excipients.
In yet another embodiment the present invention provides a process for preparing sustained oral release film coated tablets, the process comprising the steps of:
(a) sifting active ingredient and diluent through #40 mesh and blend for 10 minutes,
(b) sifting lubricant through # 60 mesh, adding to step (a) and blending for 5 minutes,
(c) compressing the lubricated blend using compression machine having 4.75 mm tablet punches, and
(d) coating the obtained tablets using coating solution of which is prepared by dispersing 100 gm of surelease aqueous dispersion in 120 gm of water under stirring to obtain film coated tablets.
In yet another embodiment the present invention provides a process for preparing sustained release film coated pellets, the process comprising the steps of:
(a) sifting active ingredient, diluent, release-controlling polymer through # 30 mesh,
(b) sprinkling little water to obtain wet mass and passing through # 20 mesh,
(c) drying the obtained wet granules of step (b) and blending with lubricant,
(d) compressing the lubricated blend using compression machine having 3.5 mm tablet punches, and
(e) coating the obtained pellets using coating solution of which is prepared by dispersing 100 gm of surelease aqueous dispersion in 120 gm of water under stirring to obtain film coated pellets.
In yet another embodiment the present invention provides a process for preparing sustained release minitablets and pellets, the process comprising the steps of:
(a) sifting active ingredient, diluent, release-controlling polymers, disintegrant through # 30 mesh and mixing well,
(b) dissolving binder in solvent, adding to sifted blend to obtain wet mass and passing through # 20 mesh,
(c) drying the obtained wet granules of step (b) and blending with lubricant, and
(d) compressing the lubricated blend using compression machine having 4.5 mm tablet punches or lesser than 4.5 mm to obtain minitablets, or
(e) compressing the lubricated blend using compression machine having 3.5 mm tablet punches or lesser than 3.5 mm to obtain pellets.
In yet another embodiment the present invention provides a process for preparing glucose oral sustained release sachets and powder for suspension, the process comprising the steps of:
(a) sifting active ingredient, diluent, release-controlling polymers, through # 30 mesh and mixing well,
(b) sprinkling little water to prepare wet mass and passing through # 20 mesh, (c) drying the obtained wet granules of step (b) and coating the obtained granules using coating solution which is prepared by dispersing 100 gm of surelease aqueous dispersion in 120 gm of water under stirring to obtain coated granules, and
(d) blending the granules with extragranular materials and packing into pouches / sachets.
In yet another embodiment the present invention provides a process for preparing glucose oral sustained release film coated tablets, the process comprising the steps of:
(a) sifting dextrose monohydrate and microcrystalline cellulose PH-102 through #40 mesh and blend for 10 minutes,
(b) sifting magnesium stearate through # 60 mesh, adding to step (a) and blending for 5 minutes,
(c) compressing the lubricated blend using compression machine having 4.75 mm tablet punches, and
(d) coating the obtained tablets using 25% surelease dispersion which is prepared by dispersing 100 gm of 25% surelease aqueous dispersion in 120 gm of water under stirring to obtain glucose film coated tablets.
In yet another embodiment the present invention provides a process for preparing glucose oral sustained release film coated pellets, the process comprising the steps of:
(a) sifting dextrose monohydrate, microcrystalline cellulose PH-102, hypromellose E6 premium through # 30 mesh,
(b) sprinkling very little water to obtain wet mass and passing through # 20 mesh,
(c) drying the obtained wet granules of step (b) and blending with magnesium stearate,
(d) compressing the lubricated blend using compression machine having 3.5 mm tablet punches, and
(e) coating the obtained pellets using 25% surelease dispersion which is prepared by dispersing 100 gm of 25% surelease aqueous dispersion in 120 gm of water under stirring to obtain film coated pellets.
In yet another embodiment the present invention provides a process for preparing sustained release minitablets and pellets, the process comprising the steps of:
(a) sifting dextrose monohydrate, maize starch, hypromellose K100LV CR, hypromellose K4M CR, croscarmellose through # 30 mesh and mixing well,
(b) dissolving povidone K-30 in purified water, adding to sifted blend to obtain wet mass and passing through # 20 mesh,
(c) drying the obtained wet granules of step (b) and blending with magnesium stearate, and
(d) compressing the lubricated blend using compression machine having 4.5 mm tablet punches or lesser than 4.5mm punches to obtain minitablets, or
(e) compressing the lubricated blend using compression machine having 3.5 mm tablet punches or lesser than 3.5mm punches to obtain pellets.
In yet another embodiment the present invention provides a process for preparing glucose oral sustained release film coated tablets, the process comprising the steps of:
(a) sifting Dextrose monohydrate, microcrystalline cellulose PH-102, hypromellose E6 premium through # 30 mesh and mixing well,
(b) sprinkling little water to prepare wet mass and passing through # 20 mesh,
(c) drying the obtained wet granules of step (b) and coating the obtained granules using coating solution which is prepared by dispersing 100 gm of surelease aqueous dispersion in 120 gm of water under stirring to obtain coated granules, and
(d) blending the granules with extragranular materials and packing into pouches / sachets.
DETAILED DESCRIPTION OF THE INVENTION
The term "comprising", which is synonymous with "including", "containing", or "characterized by" here is defined as being inclusive or open-ended, and does not exclude additional, unrecited elements or method steps, unless the context clearly requires otherwise. The term“active ingredients” of the present invention is used to provide continuous energy for a longer duration. Preferably used active ingredient is carbohydrate. Most preferably used active ingredient is dextrose.
The present invention provides sustained release glucose oral film coated tablets, film coated pellets, minitablets, pellets comprising carbohydrate as active ingredient and pharmaceutically acceptable excipients.
The present invention provide sustained release glucose oral film coated tablets composition comprising dextrose monohydrate as carbohydrate and diluent, lubricant,
coating solution as pharmaceutically acceptable excipients to ensure continuous energy.
The present invention provide sustained release glucose oral film coated pellets composition comprising dextrose monohydrate as carbohydrate and diluent, release controlling polymer, lubricant, solvent, coating solution as pharmaceutically acceptable excipients to ensure continuous energy.
The present invention provide sustained release glucose oral film coated pellets composition comprising active ingredient, diluent, release-controlling polymer, solvent in intra granular components and lubricant in extra granular component.
The present invention provide sustained release glucose oral minitablets, and pellets compositions comprising dextrose monohydrate as carbohydrate and diluent, release-controlling polymers, disintegrant, binder, lubricant as pharmaceutically acceptable excipients to ensure continuous energy.
The present invention provides compositions of sustained release glucose sachets and powder for suspension comprising dextrose monohydrate as carbohydrate and diluent, release-controlling polymer, extragranular materials, coating solution as pharmaceutically acceptable excipients to ensure continuous energy.
Dextrose is the name of a simple sugar that is made from corn and is chemically identical to glucose, or blood sugar. Simple sugars can raise blood sugar levels very quickly, and they often lack nutritional value. Dextrose is often used in baking products as a sweetener, and can be commonly found in items such as processed foods and corn syrup. Dextrose also has medical purposes. It is dissolved in solutions that are given intravenously, which can be combined with other drugs, or used to increase blood sugar.
Dextrose is used in various concentrations for different purposes. For example, dextrose is used as an IV solution in case of dehydration and low blood sugar. Dextrose IV solutions can also be combined with many drugs, for IV administration. Dextrose gel or tablets are used in diabetes or hypoglycaemic patients having low blood sugar.
Diluents may be selected from any such pharmaceutically acceptable excipients, which give bulk to the composition and improve compressibility. Diluent used in glucose oral film coated tablets and film coated pellets compositions of the present invention include, but are not limited to starch and starch derivatives like corn starch, potato starch, wheat starch, maize starch, pregelatinized starch, dicalcium phosphate, calcium phosphate tribasic, calcium carbonate, calcium sulphate, sorbitol, microcrystalline cellulose, lactose, lactose anhydrous, lactose monohydrate, spray dried lactose, glucose, mannitol, alginates, alkali earth metal salts, clay, polyethylene glycols or similar materials. Preferably used diluent in glucose oral film coated tablets and film coated pellets is selected from microcrystalline Cellulose PH-101, microcrystalline cellulose PH-102. Preferably used diluent in mini tablets and pellets is selected from microcrystalline Cellulose PH-102 maize starch. Preferably used diluent in sachets and powder for suspension is microcrystalline cellulose PH- 102.
Release-controlling polymer used in glucose film coated pellets, minitablets and pellets compositions of the present invention include, but are not limited to methylcellulose, ethylcellulose, hydroxyethylcellulose, propylcellulose, hydroxypropylcellulose, hydroxypropyl methylcellulose (hypromellose), hypromellose E6 premium, hypromellose K100LV CR, hypromellose K4M CR, carboxymethylcellulose, polymethyl methacrylate, polyethyl methacrylate, polybutyl methacrylate, polyisobutyl methacrylate, polyhexyl methacrylate, polyisodecyl methacrylate, polylauryl methacrylate, polyphenyl methacrylate, polymethyl acrylate,
polyisopropyl acrylate, polyisobutyl acrylate, polyoctadecyl acrylate, polyethylene, polypropylene, polyethylene oxide, polyethylene terephthalate, polyvinyl isobutyl ether, polyvinyl acetate, polyvinyl chloride, polyurethane, Eudragit RS 30D, HPMC K4M, HPMC K100M, HPMC E50, HPMC E3 or mixtures thereof. Preferably used release-controlling polymer in glucose film coated tablets and glucose film coated pellets is selected from Eudragit RS 30D, HPMC K4M, HPMC K100M, HPMC E50 and hypromellose E6 premium. Preferably used release-controlling polymer in glucose minitablets and pellets are HPMC K4M, HPMC K100M, HPMC E3, Eudragit RS 30D, hypromellose K100LV CR and hypromellose K4M CR.
Disintegrants used in the composition of the present invention include, but are not limited to low substituted hydroxypropyl cellulose (L-HPC), sodium starch glycolate, sodium croscarmellose, cross-linked polyvinylpyrrolidone, soy polysaccharide, cross-linked alginic acid, gellan gum, xanthan gum, calcium silicate and ion exchange resin. Preferably used disintegrant in glucose minitablets and pellets is croscarmellose.
Lubricants used in the composition of the present invention include, but are not limited to talc, magnesium stearate, other alkali earth metal stearates like zinc, calcium stearate etc; sodium lauryl sulphate, hydrogenated vegetable oil, sodium benzoate, sodium stearyl fumarate, glyceryl monostearate, polyethylene glycol and similar materials. Preferably used lubricant is magnesium stearate.
Binders used in the compositions of present invention include, but not limited to sugars such as starch (potato starch, corn starch, wheat starch), sucrose, glucose, dextrose, lactose, maltodextrin, methylene dichloride, natural and synthetic gums (e.g. acacia), gelatin, cellulose derivatives (e.g. microcrystalline cellulose, HPC, HEC, HPMC, carboxymethyl cellulose, methyl cellulose, ethyl cellulose), polyvinylpyrrolidone, polyethyleneglycols, waxes, calcium carbonate, calcium phosphate. Preferably used binder in glucose minitablets and pellets is povidone K-30.
The term“solvent” used in the present invention is water. Most preferably purified water.
The term extragranular material used in sachets and powder for suspension includes but not limited to mannitol, sucralose, citric acid anhydrous, orange flavour, strawberry flavour, talc and sucrose.
Coating solution may be selected from any such pharmaceutically acceptable excipients, which give film coating to the tablet for sustained release. Preferably used coating solution is surelease 25% dispersion. Surelease®, aqueous ethylcellulose dispersion is used for modified release and taste masking applications.
Characteristics of Surelease dispersion:
Aqueous dispersion
Complete, optimally formulated system
Easy to use and environmentally friendly
Consistent and reproducible drug release profiles.
Film coating used in the present invention is prepared by dispersing 25% surelease aqueous dispersion in 120 gm of water under stirring.
Sustained release glucose film coated tablets, film coated pellets, minitablets and pellets of the present invention has been prepared by using direct compression which is cost effective, stable, less wear & tear of punches, simplified validation and requires fewer excipients.
Sustained release glucose film coated tablets, film coated pellets, minitablets, powder for suspension, sachets and pellets of the present invention is used to provide continuous release of energy, supports endurance, management of stress, fatigue and suitable for diabetic patients.
Sustained release film coated tablets and film coated pellets by using simple direct compression process comprising mainly the steps of sifting, blending, compressing and film coating.
Sustained release minitablets, and pellets by using simple direct compression process comprising the steps of sifting, dissolving, drying, blending and compressing.
Sustained release sachets and powder for suspension comprising the steps of sifting, drying, coating and blending.
Sustained release glucose film coated tablets, powder for suspension, sachets, film coated pellets, minitablet and pellets of the present invention provides continuous release of Dextrose for a period of 30 to 240 minutes.
Sustained release film coated tablets of glucose can be fortified with adoptogens like ashwagandha, brain tonics like brahmi, phosphatidyl serine, gensing, mood elevators like caffeine etc.
The present invention provides composition of sustained release glucose oral film coated tablets composition comprising dextrose monohydrate as carbohydrate, microcrystalline Cellulose PH 102 as diluent, magnesium stearate as lubricant and surelease 25% dispersion as coating solution for weight gain of 5%.
The present invention is to provide sustained release glucose oral film coated tablets composition comprising dextrose monohydrate as carbohydrate, microcrystalline Cellulose PH-101, microcrystalline Cellulose PH 102 as diluent, magnesium stearate as lubricant, Eudragit RS 30D, HPMC K4M, HPMC K100M, HPMC E50 as release-controlling polymer and triethyl citrate as plasticizer.
The present invention provides composition of sustained release glucose oral film coated pellets composition comprising dextrose monohydrate as carbohydrate, microcrystalline cellulose PH 102 as diluent, hypromellose E6 premium as release controlling polymer, magnesium stearate as lubricant, purified water as solvent and surelease 25% dispersion as coating solution for weight gain of 3%, 5% and 7%.
The present invention provides composition of sustained release glucose oral film coated pellets composition comprising dextrose monohydrate, microcrystalline cellulose PH 102, hypromellose E6 premium, purified water in intra granular components and magnesium stearate in extra granular component.
The present invention provides composition of sustained release glucose oral minitablets and pellets comprising dextrose monohydrate as carbohydrate, microcrystalline Cellulose PH-102 and maize starch as diluent, hypromellose K100LV CR, hypromellose K4M CR, HPMC K4M, HPMC K100M as release-controlling polymers, croscarmellose sodium as disintegrant, povidone K-30 as binder and magnesium stearate as lubricant.
The present invention is to provide composition of sustained release glucose oral sachets and powder for suspension comprising dextrose monohydrate as carbohydrate, microcrystalline cellulose PH-102 as diluent, Eudragit RS PO, Hypromellose E6 premium as release-controlling polymers, mannitol, sucralose, citric acid anhydrous, orange flavour, strawberry flavour, talc, sucrose as extragranular materials, Surelease 25% dispersion as coating solution.
The invention disclosed herein is process for the preparation of sustained release pellets and film coated tablets of glucose useful to ensure continuous energy.
The present invention is illustrated in detail but not limiting to, the following examples. It will be apparent to those skilled in the art that many modifications, both
to materials and methods, may be practiced without departing from the scope of the invention.
Example 1: Preparation of sustained release tablets:
Weight of each tablet is 110.00 mg
Manufacturing process
Dextrose monohydrate and microcrystalline cellulose PH-102 were co-sifted through 40# and Loaded in GPCG. Binder solution prepared using Eudragit RS 30D with
Plasticizer Triethyl Citrate. Polymeric dispersion sprayed into above dry mix materials at product temperature 30°C. The dried granules sifted through 24# and lubricated with Magnesium Stearate for 5 minutes. Lubricated blend was compressed into tablet using compression machine with suitable punch tooling.
Example 2:
Preparation of sustained release tablets:
Weight of each tablet is 100.00 mg
Manufacturing process
Dextrose monohydrate, Microcrystalline cellulose PH-102, HPMC K4M and HPMC K100M were co-sifted through 30# and Loaded into blender and Blended for 30 minutes and lubricated with Magnesium Stearate for 5 minutes. Lubricated blend was compressed into tablet using compression machine with suitable punch tooling.
Example 3:
Preparation of sustained release tablets:
Weight of each film tablet is 75.60 mg
Manufacturing process
Dextrose monohydrate and microcrystalline cellulose PH-102 were co-sifted through # 40 mesh and blended for 30 minutes. Magnesium stearate is sifted through # 60 mesh, added to the above obtained blend and blended for 5 minutes. Lubricated blend was compressed into tablet using compression machine. 100 gm of 25% surelease aqueous dispersion was dispersed in 120 gm of water and stirred for 45 minutes at 1600-1800 rpm to obtain 5% weight gain of film coating. Glucose tablets were coated with surelease 25% dispersion to obtain embedded coated sustained release glucose tablets.
Example 4:
Preparation of sustained release tablets:
Weight of each tablet is 85.00 mg
Manufacturing process
Dextrose monohydrate and microcrystalline cellulose PH-102 were co-sifted through # 40 mesh and blended for 30 minutes. Magnesium stearate is sifted through # 60 mesh,
added to the above obtained blend and blended for 5 minutes. Lubricated blend was compressed into tablet using compression machine. Coating dispersion was prepared HPMC E50, Polyethylene Glycol 6000, Purified Talc and Ti02 with purified water stirred for 45 minutes. Glucose tablets were coated with dispersion to obtain embedded coated sustained release glucose tablets.
Example 5:
Preparation of mini tablets:
Manufacturing process
Dextrose monohydrate, Microcrystalline cellulose PH-102, HPMC K4M and HPMC K100M were co-sifted through 30# and Loaded into blender and Blended for 30 minutes and lubricated with Magnesium Stearate for 5 minutes. Lubricated blend was compressed into tablet using compression machine with 2 mm tooling.
Example 6:
Preparation of sustained release glucose 100 minitablets
Weight of each sustained release mini tablet is 760 mg
Manufacturing process
Dextrose monohydrate, maize starch, hypromellose K100LV CR, hypromellose K4M CR, croscarmellose sodium were co-sifted through # 30 mesh and mixed well. Povidone K-30 was dissolved in purified water and wet mass was prepared by adding sifted blend. Passed through # 20 mesh. Dried the wet granules and blended with magnesium stearate. Lubricated blend was compressed using 4.5 mm tablet punches to obtain sustained release glucose minitablets.
Example 7:
Preparation of Pellets:
Dextrose monohydrate, Microcrystalline cellulose PH-102 were co-sifted through 30# and Pellets were prepared using HPMC E3 binder solution using extrusion and spheronization technique. Then Dextrose pellets were loaded into GPCG and Polymer coating done using Eudragit RS 30D coating dispersion.
Example 8:
Preparation of sustained release glucose film coated pellets
Weight of each film coated pellet of 3% weight gain is 20.6 mg.
Weight of each film coated pellet of 5% weight gain is 21.00 mg
Weight of each film coated pellet of 7% weight gain is 21.4 mg.
Manufacturing process
Dextrose monohydrate, microcrystalline cellulose PH 102, hypromellose E6 premium were co-sifted through # 30 mesh. Wet mass was prepared by sprinkling little water and passed through # 20 mesh. Dried the wet granules and blended with magnesium stearate. Compressed using 3.5 mm tablet punches. Dedusted the obtained tablets to remove impurities. Obtained pellets were coated by conventional methods using film coating which is prepared by dispersing 100 gm of 25% surelease aqueous dispersion in 120 gm of water for weight gain of 3%, 5% and 7% to obtain sustained release glucose film coated pellets.
Example 9:
Preparation of sustained release glucose 100 pellets
Weight of each sustained release pellets is 2000 mg
Manufacturing process
Dextrose monohydrate, maize starch, hypromellose K100LV CR, hypromellose K4M CR, croscarmellose sodium were co-sifted through # 30 mesh and mixed well. Povidone K-30 was dissolved in purified water and wet mass was prepared by adding sifted blend. Passed through # 20 mesh. Dried the wet granules and blended with
magnesium stearate. Lubricated blend was compressed using 3.5 mm tablet punches to obtain sustained release glucose pellets.
Example 10:
Preparation of sachets:
Manufacturing process
Dextrose monohydrate, Eudragit RS PO were co-sifted through 30# and granulated using Povidone K30 solution. Wet granules were dried and sifted through 40#. Finally, Dextrose granules mixed with extragranular materials and filled in pouches.
Example 11:
Preparation of sustained release glucose powder for suspension /Sachets
Manufacturing process
Dextrose monohydrate, microcrystalline cellulose PH 102, hypromellose E6 premium were co-sifted through # 30 mesh. Wet mass was prepared by sprinkling little water and passed through # 20 mesh. Dried the wet granules. Granules were coated by fluidized bed coating methods using solution which is prepared by dispersing 100 gm of 25% surelease aqueous dispersion in 120 gm of water to obtain sustained release glucose coated granules. The granules were then blended with extragranular materials and packed into pouches / sachets.
Claims
1. Sustained release glucose oral compositions comprising dextrose monohydrate as active ingredient, diluent, release-controlling polymer, other pharmaceutically acceptable excipients.
2. The sustained release dosage form composition as claimed in claim 1 comprising:
(a) 3% to 90%(w/w) of dextrose monohydrate,
(b) 0.5% to 20% (w/w) of diluent,
(c) 0.2% to 40% (w/w) of release-controlling polymer,
(d) optionally 1 to 10% of coating solution, and
(e) and optionally other pharmaceutically acceptable excipients.
3. The sustained release glucose oral compositions as claimed in claims 1 and 2, wherein oral compositions are selected from film coated tablets, film coated pellets, minitablets, pellets, sachets and powder for suspension.
4. The sustained release glucose oral compositions as claimed in claim 3, wherein film coated tablets comprises:
(a) 50% to 85% (w/w) of dextrose monohydrate,
(b) 5% to 20% (w/w) of diluent,
(c) 1% to 40% (w/w) of release-controlling polymer,
(d) 0.5% to 3% (w/w) of lubricant, and
(e) optionally 1 to 10% (w/w) of coating solution.
5. The sustained release glucose oral compositions as claimed in claim 32, wherein film coated pellets comprises:
(a) 60% to 80% (w/w) of dextrose monohydrate,
(b) 10% to 20% (w/w) of diluent,
(c) 1% to 10% (w/w) of release-controlling polymer,
(d) 0.5 to 1.0% (w/w) of lubricant, and
(e) optionally 1 to 10% (w/w) of coating solution.
6. The sustained release glucose oral compositions as claimed in claim 3, wherein minitablets and pellets comprises:
(a) 50% to 90% (w/w) of dextrose monohydrate,
(b) 1% to 10% (w/w) of diluent,
(c) 1% to 40% (w/w) of release-controlling polymers,
(d) 1% to 3% (w/w) of disintegrant,
(e) 1% to 5%(w/w) of binder, and
(f) 0.1% to 3% (w/w) of lubricant.
7. The sustained release glucose oral compositions as claimed in claim 3, wherein sachets and powder for suspension comprises:
(a) 2% to 10% of dextrose monohydrate,
(b) 0.1% to 3% of diluent,
(c) 0.1% to 5% of release-controlling polymer, and
(d) 90% to 95% of extragranular material.
8. The sustained release glucose oral compositions as claimed in claims 1 to 7, wherein diluent is selected from starch and starch derivatives like corn starch, potato starch, wheat starch, maize starch, pregelatinized starch, dicalcium phosphate, calcium phosphate tribasic, calcium carbonate, calcium sulphate, sorbitol, microcrystalline cellulose, lactose, lactose anhydrous, lactose monohydrate, spray dried lactose, glucose, mannitol, alginates, alkali earth metal salts, clay, polyethylene glycols or similar materials.
9. The sustained release glucose oral compositions as claimed in claims 1 to 7, wherein release-controlling polymer is selected from methylcellulose, ethylcellulose, hydroxyethylcellulose, propylcellulose, hydroxypropylcellulose, hydroxypropyl methylcellulose (hypromellose), hypromellose E6 premium, hypromellose K100LV CR, hypromellose K4M CR, carboxymethylcellulose, polymethyl methacrylate, polyethyl methacrylate, polybutyl methacrylate, polyisobutyl methacrylate, polyhexyl methacrylate, polyisodecyl methacrylate, polylauryl methacrylate, polyphenyl methacrylate, polymethyl acrylate, polyisopropyl acrylate, polyisobutyl acrylate, polyoctadecyl acrylate, polyethylene, polypropylene, polyethylene oxide, polyethylene terephthalate, polyvinyl isobutyl ether, polyvinyl acetate, polyvinyl chloride, polyurethane, Eudragit RS 30D, HPMC K4M, HPMC K100M, HPMC E50, HPMC E3 or mixtures thereof.
10. The sustained release glucose oral compositions as claimed in claims 1 to 2, wherein pharmaceutically acceptable excipients are selected from lubricant, disintegrant, binder, extragranular material.
11. The sustained release glucose oral compositions as claimed in claim 10, wherein lubricant is selected from talc, magnesium stearate, other alkali earth metal stearates like zinc, calcium stearate etc; sodium lauryl sulphate, hydrogenated vegetable oil, sodium benzoate, sodium stearyl fumarate, glyceryl monostearate, polyethylene glycol and similar materials.
12. The sustained release glucose oral compositions as claimed in claim 10, wherein disintegrant is selected from low substituted hydroxypropyl cellulose (L-HPC), sodium starch glycolate, sodium croscarmellose, cross-linked polyvinylpyrrolidone, soy polysaccharide, cross-linked alginic acid, gellan gum, xanthan gum, calcium silicate and ion exchange resin.
13. The sustained release glucose oral compositions as claimed in claim 10, wherein binder is selected from sugars such as starch (potato starch, corn starch, wheat starch), sucrose, glucose, dextrose, lactose, maltodextrin, methylene dichloride, natural and synthetic gums (e.g. acacia), gelatin, cellulose derivatives (e.g. microcrystalline cellulose, HPC, HEC, HPMC, carboxymethyl cellulose, methyl cellulose, ethyl cellulose), polyvinylpyrrolidone, polyethyleneglycols, waxes, calcium carbonate, calcium phosphate.
14. The sustained release glucose oral compositions as claimed in claim 10, extragranular material is selected from mannitol, sucralose, citric acid anhydrous, orange flavour, strawberry flavour, talc and sucrose.
15. The process for preparing sustained oral release film coated tablets as claimed in claim 4, the process comprising the steps of:
(a) sifting active ingredient and diluent through #40 mesh and blend for 10 minutes,
(b) sifting lubricant through # 60 mesh, adding to step (a) and blending for 5 minutes,
(c) compressing the lubricated blend using compression machine having 4.75 mm tablet punches, and
(d) coating the obtained tablets using coating solution of which is prepared by dispersing 100 gm of surelease aqueous dispersion in 120 gm of water under stirring to obtain film coated tablets.
16. The process for preparing sustained oral release film coated pellets as claimed in claim 5, the process comprising the steps of:
(a) sifting active ingredient, diluent, release-controlling polymer through # 30 mesh,
(b) sprinkling little water to obtain wet mass and passing through # 20 mesh,
(c) drying the obtained wet granules of step (b) and blending with lubricant,
(d) compressing the lubricated blend using compression machine having 3.5 mm tablet punches, and
(e) coating the obtained pellets using coating solution of which is prepared by dispersing 100 gm of surelease aqueous dispersion in 120 gm of water under stirring to obtain film coated pellets.
17. The process for preparing sustained oral release minitablets and pellets as claimed in claim 6, the process comprising the steps of:
(a) sifting active ingredient, diluent, release-controlling polymers, disintegrant through # 30 mesh and mixing well,
(b) dissolving binder in solvent, adding to sifted blend to obtain wet mass and passing through # 20 mesh,
(c) drying the obtained wet granules of step (b) and blending with lubricant, and
(d) compressing the lubricated blend using compression machine having 4.5 mm tablet punches or lesser than 4.5 mm to obtain minitablets, or
(e) compressing the lubricated blend using compression machine having 3.5 mm tablet punches or lesser than 3.5 mm to obtain pellets.
18. The process for preparing sustained oral release sachets and powder for suspension as claimed in claim 7, the process comprising the steps of:
(a) sifting active ingredient, diluent, release-controlling polymers, through # 30 mesh and mixing well,
(c) sprinkling little water to prepare wet mass and passing through # 20 mesh,
(e) drying the obtained wet granules of step (b) and coating the obtained granules using coating solution which is prepared by dispersing 100 gm of surelease aqueous dispersion in 120 gm of water under stirring to obtain coated granules, and
(f) blending the granules with extragranular materials and packing into pouches / sachets.
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|---|---|---|---|
| IN201941023800 | 2019-06-15 | ||
| IN201941023800 | 2019-06-15 |
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| WO2020254940A1 true WO2020254940A1 (en) | 2020-12-24 |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113069496A (en) * | 2021-03-18 | 2021-07-06 | 济川药业集团有限公司 | Traditional Chinese medicine granule composition for treating infantile common cold and preparation method thereof |
| WO2024060048A1 (en) * | 2022-09-21 | 2024-03-28 | 浙江汉脉医药科技有限公司 | Saccharide sustained-release composition and preparation method therefor |
| WO2024252015A1 (en) * | 2023-06-09 | 2024-12-12 | euvorio GmbH | Use of carbohydrate-containing compositions in tablet form for treatment of hypoglycemic states |
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|---|---|---|---|---|
| US20020122823A1 (en) * | 2000-12-29 | 2002-09-05 | Bunick Frank J. | Soft tablet containing dextrose monohydrate |
| WO2009015880A1 (en) * | 2007-07-31 | 2009-02-05 | Cargill, Incorporated | Direct compressible dextrose |
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2020
- 2020-06-15 WO PCT/IB2020/055573 patent/WO2020254940A1/en active Application Filing
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20020122823A1 (en) * | 2000-12-29 | 2002-09-05 | Bunick Frank J. | Soft tablet containing dextrose monohydrate |
| WO2009015880A1 (en) * | 2007-07-31 | 2009-02-05 | Cargill, Incorporated | Direct compressible dextrose |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113069496A (en) * | 2021-03-18 | 2021-07-06 | 济川药业集团有限公司 | Traditional Chinese medicine granule composition for treating infantile common cold and preparation method thereof |
| CN113069496B (en) * | 2021-03-18 | 2022-09-06 | 济川药业集团有限公司 | Traditional Chinese medicine granule composition for treating infantile common cold and preparation method thereof |
| WO2024060048A1 (en) * | 2022-09-21 | 2024-03-28 | 浙江汉脉医药科技有限公司 | Saccharide sustained-release composition and preparation method therefor |
| WO2024252015A1 (en) * | 2023-06-09 | 2024-12-12 | euvorio GmbH | Use of carbohydrate-containing compositions in tablet form for treatment of hypoglycemic states |
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