CN101536989B - Metformin hydrochloride intragastric floating sustained-release tablet and preparation method thereof - Google Patents
Metformin hydrochloride intragastric floating sustained-release tablet and preparation method thereof Download PDFInfo
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- CN101536989B CN101536989B CN200810019838XA CN200810019838A CN101536989B CN 101536989 B CN101536989 B CN 101536989B CN 200810019838X A CN200810019838X A CN 200810019838XA CN 200810019838 A CN200810019838 A CN 200810019838A CN 101536989 B CN101536989 B CN 101536989B
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- metformin hydrochloride
- release tablet
- intragastric floating
- floating sustained
- sustained
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- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin hydrochloride Natural products CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 title claims abstract description 47
- 229960004329 metformin hydrochloride Drugs 0.000 title claims abstract description 43
- OETHQSJEHLVLGH-UHFFFAOYSA-N metformin hydrochloride Chemical compound Cl.CN(C)C(=N)N=C(N)N OETHQSJEHLVLGH-UHFFFAOYSA-N 0.000 title claims abstract description 43
- 239000007939 sustained release tablet Substances 0.000 title claims abstract description 22
- 238000002360 preparation method Methods 0.000 title abstract description 16
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 23
- 239000000463 material Substances 0.000 claims abstract description 9
- 239000000314 lubricant Substances 0.000 claims abstract description 7
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 claims description 35
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims description 30
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 28
- 238000000034 method Methods 0.000 claims description 21
- 238000002156 mixing Methods 0.000 claims description 18
- 230000001476 alcoholic effect Effects 0.000 claims description 16
- 229910000030 sodium bicarbonate Inorganic materials 0.000 claims description 15
- 235000017557 sodium bicarbonate Nutrition 0.000 claims description 15
- 235000019359 magnesium stearate Nutrition 0.000 claims description 14
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 14
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 14
- 239000008187 granular material Substances 0.000 claims description 10
- 238000002844 melting Methods 0.000 claims description 10
- 230000008018 melting Effects 0.000 claims description 10
- 206010013786 Dry skin Diseases 0.000 claims description 9
- 239000002671 adjuvant Substances 0.000 claims description 9
- 238000001035 drying Methods 0.000 claims description 9
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 9
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 9
- 239000007779 soft material Substances 0.000 claims description 9
- 238000003756 stirring Methods 0.000 claims description 9
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 7
- 229960003943 hypromellose Drugs 0.000 claims description 7
- 239000011159 matrix material Substances 0.000 claims description 7
- 239000011230 binding agent Substances 0.000 claims description 6
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 4
- 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 claims description 4
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 claims description 4
- 239000001095 magnesium carbonate Substances 0.000 claims description 4
- 229910000021 magnesium carbonate Inorganic materials 0.000 claims description 4
- 239000000741 silica gel Substances 0.000 claims description 4
- 229910002027 silica gel Inorganic materials 0.000 claims description 4
- 238000005469 granulation Methods 0.000 claims description 2
- 230000003179 granulation Effects 0.000 claims description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 2
- 239000003814 drug Substances 0.000 abstract description 17
- 206010012601 diabetes mellitus Diseases 0.000 abstract description 2
- 239000000853 adhesive Substances 0.000 abstract 1
- 230000001070 adhesive effect Effects 0.000 abstract 1
- 239000000243 solution Substances 0.000 description 15
- -1 Hydroxypropyl Chemical group 0.000 description 12
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 12
- 229940079593 drug Drugs 0.000 description 8
- 235000021355 Stearic acid Nutrition 0.000 description 7
- 239000002775 capsule Substances 0.000 description 7
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 7
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 7
- 238000004080 punching Methods 0.000 description 7
- 239000008117 stearic acid Substances 0.000 description 7
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 5
- 238000010521 absorption reaction Methods 0.000 description 4
- 229960003105 metformin Drugs 0.000 description 4
- 239000003826 tablet Substances 0.000 description 4
- 239000001856 Ethyl cellulose Substances 0.000 description 3
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 3
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 3
- 239000001768 carboxy methyl cellulose Substances 0.000 description 3
- 238000013270 controlled release Methods 0.000 description 3
- 229920001249 ethyl cellulose Polymers 0.000 description 3
- 235000019325 ethyl cellulose Nutrition 0.000 description 3
- 230000002496 gastric effect Effects 0.000 description 3
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 3
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 3
- 210000002784 stomach Anatomy 0.000 description 3
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 2
- 206010000059 abdominal discomfort Diseases 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- 210000001072 colon Anatomy 0.000 description 2
- 230000001186 cumulative effect Effects 0.000 description 2
- 239000003405 delayed action preparation Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 230000000968 intestinal effect Effects 0.000 description 2
- 230000002045 lasting effect Effects 0.000 description 2
- 229940123208 Biguanide Drugs 0.000 description 1
- 206010012735 Diarrhoea Diseases 0.000 description 1
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 description 1
- 208000022531 anorexia Diseases 0.000 description 1
- 150000004283 biguanides Chemical class 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000001569 carbon dioxide Substances 0.000 description 1
- 229910002092 carbon dioxide Inorganic materials 0.000 description 1
- 206010061428 decreased appetite Diseases 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 210000004211 gastric acid Anatomy 0.000 description 1
- 210000004051 gastric juice Anatomy 0.000 description 1
- 210000001156 gastric mucosa Anatomy 0.000 description 1
- 230000002209 hydrophobic effect Effects 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 230000000630 rising effect Effects 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- 238000007086 side reaction Methods 0.000 description 1
- 239000002002 slurry Substances 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention relates to a medicament for treating diabetes, in particular to a metformin hydrochloride intragastric floating sustained-release tablet and a preparation method thereof. The invention adopts the formulas of a framework material, a gas generating agent, a lubricant, an adhesive and the like and uses a unique preparation process to prepare the metformin hydrochloride sustained-release tablet preparation, which can overcome the problem of low bioavailability of the metformin hydrochloride sustained-release tablet preparation in the prior art and provides the metformin hydrochloride intragastric floating sustained-release tablet preparation with high bioavailability.
Description
Technical field
The present invention relates to a kind of treatment diabetes medicament metformin hydrochloride intragastric floating sustained-release tablet and preparation method thereof.
Background technology
Metformin hydrochloride is a kind of biguanides OHA, is used for the treatment of type ii diabetes.At present, common metformin preparation dose is excessive, and medication is frequent, after nearly 30% patient takes apparent in view side reaction is arranged, and comprises stomach discomfort, feels sick, digestive tract reactions such as anorexia, diarrhoea.
The research of diabecron sustained-release preparation has now caused extensive concern.The relevant report of at present existing oral controlled-release or slow releasing preparation.Common metformin hydrochloride slow releasing preparation discharges initial amount excessive (2 hours cumulative release percentage rate＞40%, i.e. burst effects) at gastric, has caused the stimulation to gastric mucosa, and then possibly cause a series of digestive tract reactions; Simultaneously since the main absorption site of metformin medicine in the small intestinal upper end, the absorbability at colon place very a little less than, and common oral controlled-release or slow releasing preparation only have 2～3h mainly in the colon release in the holdup time of its absorption site, so bioavailability is low.
Summary of the invention
The objective of the invention is to overcome prominent phenomenon and the low problem of bioavailability released that causes owing to metformin hydrochloride is very easily water-soluble that the agent of metformin hydrochloride slow-release tablet exists in the prior art, a kind of slowly lasting metformin hydrochloride intragastric floating sustained-release tablet preparation that discharges medicine is provided.
Another object of the present invention provides the method for preparing of above-mentioned metformin hydrochloride intragastric floating sustained-release tablet.
The intragastric floating sustained-release preparation is meant a kind of drug delivery system that may float in the gastric juice and discharge medicine in a long time with constant speed.
Metformin hydrochloride intragastric floating sustained-release tablet according to the invention, form by following weight ratio by following each component:
Metformin hydrochloride: 55%～65%;
Matrix type material: 25%～35%;
Gas generating agent: 4%～8%;
Lubricant: 0.5%～2%;
Binding agent: 0.5%～4%.
Matrix type material among the present invention is two or more in hypromellose, ethyl cellulose, sodium carboxymethyl cellulose, octadecanol, hexadecanol and the stearic acid.Preferred matrix type material is hypromellose and octadecanol, and the weight ratio of hypromellose and octadecanol is 0.5～5: 1, and comparatively preferred ratio is 0.75～2: 1.Gas generating agent is a kind of in basic magnesium carbonate or the sodium bicarbonate, preferred sodium bicarbonate.Lubricant be in magnesium stearate, Pulvis Talci, the micropowder silica gel any one or more than one.Binding agent can be the water or the alcoholic solution of polyvinylpyrrolidone, hypromellose.
The method for preparing of metformin hydrochloride intragastric floating sustained-release tablet according to the invention comprises the steps:
1) it is subsequent use that principal agent and adjuvant are all crossed 80 mesh sieves.
2) with octadecanol (or hexadecanol, stearic acid) melting, add metformin hydrochloride, stir, pulverize, cross 80 mesh sieves;
3) with 2) with all the other matrix type materials, gas generating agent mixing, add binding agent system soft material, the granulation of 18 orders;
4) 40 ℃ of dryings are 2～4 hours, granulate;
5) add lubricant, compacting in flakes behind the mixing.
Key of the present invention is octadecanol of melting (or hexadecanol, stearic acid) and metformin mix homogeneously; Can make the hydrophobic octadecanol of medicine granule surface parcel one deck on the one hand, strengthen slow release effect, solve the prominent problem of bringing owing to principal agent is very easily water-soluble of releasing; On the other hand, because " solid bridge " phenomenon that octadecanol forms in the tabletting process can improve because metformin principal agent amount is big, compressibility is bad and cause the generation of phenomenons such as sliver.
Key of the present invention adds gas generating agent in also being, processes the floating in stomach sheet.Gas generating agent is met gastric acid under one's belt and is promptly produced carbon dioxide, simultaneously owing to the rapid aquation of hydrophilic framework material, makes tablet rise rapidly and floats, thereby prolonged the tablet holdup time under one's belt; Because the main absorption site of metformin hydrochloride is a upper part of small intestine, therefore, processing intragastric floating sustained-release tablet has its necessity.
Adopt the metformin hydrochloride intragastric floating sustained-release tablet preparation of the present invention's technology preparation, in release medium, float rapidly, 12 hours long-acting slow release medicines have avoided that local drug concentration is excessive to stimulate gastrointestinal; Floating in stomach time while is long, and medicine is discharged from slow releasing tablet before reaching absorption site fully, thereby reaches the purpose that improves bioavailability of medicament and blood drug level.Metformin hydrochloride intragastric floating sustained-release tablet can effectively be controlled release rate of drugs, avoids local drug concentration too high and cause stomach discomfort, can significantly improve bioavailability of medicament simultaneously.
The specific embodiment
Embodiment 1:
Prescription: metformin hydrochloride 500g;
Ethyl cellulose 124g;
Sodium carboxymethyl cellulose 40g
Stearic acid 80g;
Basic magnesium carbonate 48g;
Micropowder silica gel 4g;
Magnesium stearate 4g;
HPMC (50cps) 20% alcoholic solution is an amount of
Process 1000 altogether
Method for preparing: it is subsequent use that principal agent and adjuvant are all crossed 80 mesh sieves.At first stearic acid is heated melting, add metformin hydrochloride again, stir, pulverize, cross 80 mesh sieves; With ethyl cellulose, sodium carboxymethyl cellulose and basic magnesium carbonate mixing, add HPMC (50cps) 20% alcoholic solution system soft material, 18 orders are granulated; 40 ℃ of dryings 2 ~ 4 hours, 16 mesh sieve granulate; Add micropowder silica gel, magnesium stearate, mixing is processed sheet with the capsule shape punching press.
Embodiment 2:
Prescription: metformin hydrochloride 500g;
Hydroxypropyl emthylcellulose 184g;
Hexadecanol 60g;
Sodium bicarbonate 48g;
Pulvis Talci 8g;
10%PVP (K30) alcoholic solution is an amount of
Process 1000 altogether
Method for preparing: it is subsequent use that principal agent and adjuvant are all crossed 80 mesh sieves.At first hexadecanol is heated melting, add metformin hydrochloride again, stir, pulverize, cross 80 mesh sieves; With hydroxypropyl emthylcellulose, sodium bicarbonate mixing, add 10%PVP (K30) alcoholic solution system soft material, 18 orders are granulated; 40 ℃ of dryings 2 ~ 4 hours, 16 mesh sieve granulate; Add Pulvis Talci, mixing is processed sheet with the capsule shape punching press.
Embodiment 3:
Prescription: metformin hydrochloride 500g;
Hydroxypropyl emthylcellulose 100g;
Octadecanol 144g;
Sodium bicarbonate 48g;
Magnesium stearate 8g;
10%PVP (K30) alcoholic solution is an amount of
Process 1000 altogether
Method for preparing: it is subsequent use that principal agent and adjuvant are all crossed 80 mesh sieves.At first octadecanol is heated melting, add metformin hydrochloride again, stir, pulverize, cross 80 mesh sieves; With hydroxypropyl emthylcellulose, sodium bicarbonate mixing, add 10%PVP (K30) alcoholic solution system soft material, 18 orders are granulated; 40 ℃ of dryings 2 ~ 4 hours, 16 mesh sieve granulate; Add magnesium stearate, mixing is processed sheet with the capsule shape punching press.
Embodiment 4:
Prescription: metformin hydrochloride 500g;
Hydroxypropyl emthylcellulose 164g;
Octadecanol 100g;
Sodium bicarbonate 48g;
Magnesium stearate 8g;
10%PVP (K30) alcoholic solution is an amount of
Process 1000 altogether
Method for preparing: it is subsequent use that principal agent and adjuvant are all crossed 80 mesh sieves.At first octadecanol is heated melting, add metformin hydrochloride again, stir, pulverize, cross 80 mesh sieves; With hydroxypropyl emthylcellulose, sodium bicarbonate mixing, add 10%PVP (K30) alcoholic solution system soft material, 18 orders are granulated; 40 ℃ of dryings 2 ~ 4 hours, 16 mesh sieve granulate; Add magnesium stearate, mixing is processed sheet with the capsule shape punching press.
Embodiment 5:
Prescription: metformin hydrochloride 500g;
Hydroxypropyl emthylcellulose 220g;
Octadecanol 55g;
Sodium bicarbonate 48g;
Magnesium stearate 8g;
10%PVP (K30) alcoholic solution is an amount of
Process 1000 altogether
Method for preparing: it is subsequent use that principal agent and adjuvant are all crossed 80 mesh sieves.At first octadecanol is heated melting, add metformin hydrochloride again, stir, pulverize, cross 80 mesh sieves; With hydroxypropyl emthylcellulose, sodium bicarbonate mixing, add 10%PVP (K30) alcoholic solution system soft material, 18 orders are granulated; 40 ℃ of dryings 2 ~ 4 hours, 16 mesh sieve granulate; Add magnesium stearate, mixing is processed sheet with the capsule shape punching press.
Embodiment 6:
Embodiment among the present invention 3, example 4, example 5 are carried out release in vitro degree test in 12 hours respectively with patent 200310112200.8 embodiment 1, and result of the test is compared.
Test method: according to drug release determination (two ones first method slurries of Chinese Pharmacopoeia version in 2005 method), the 900ml simulated gastric fluid is as release medium, and rotating speed is that per minute 50 changes, operation in accordance with the law; In 1h, 2h, 4h, 6h; 8h, 10h, 12h; Sampling 5ml filters (release medium of in time replenishing the equal-volume equitemperature), dilution.
The external floating situation of each prescription is investigated and is seen table one.The cumulative release percentage rate of each time point is seen table two.
The external floating situation of table one, four prescriptions of comparison
Annotate: F floats for rising, and promptly is sunken among the liquid level fully.
The average accumulated of table two, each time point of four prescriptions of comparison discharges percentage rate
Through contrast, visible metformin hydrochloride intragastric floating sustained-release tablet of the present invention floats in release medium soon, rise and float longer duration, and release is slowly lasting, has solved the prominent problem of bringing owing to principal agent is very easily water-soluble of releasing preferably.
In addition, because the preparation of intragastric floating sustained-release tablet of the present invention success makes it drug release at stomach, be absorbed in the small intestinal upper end, thereby can improve bioavailability.
Embodiment 7:
Prescription: metformin hydrochloride 750g;
Hydroxypropyl emthylcellulose 216g;
Octadecanol 150g;
Sodium bicarbonate 72g;
Magnesium stearate 10g;
10%PVP (K30) alcoholic solution is an amount of
Process 1000 altogether
Method for preparing: it is subsequent use that principal agent and adjuvant are all crossed 80 mesh sieves.At first octadecanol is heated melting, add metformin hydrochloride again, stir, pulverize, cross 80 mesh sieves; With hydroxypropyl emthylcellulose, sodium bicarbonate mixing, add 10%PVP (K30) alcoholic solution system soft material, 18 orders are granulated; 40 ℃ of dryings 2 ~ 4 hours, 16 mesh sieve granulate; Add magnesium stearate, mixing is processed sheet with the capsule shape punching press.
Embodiment 8:
Prescription: metformin hydrochloride 1000g;
Hydroxypropyl emthylcellulose 248g;
Stearic acid 240g;
Sodium bicarbonate 96g;
Magnesium stearate 16g;
10%PVP (K30) alcoholic solution is an amount of
Process 1000 altogether
Method for preparing: it is subsequent use that principal agent and adjuvant are all crossed 80 mesh sieves.At first stearic acid is heated melting, add metformin hydrochloride again, stir, pulverize, cross 80 mesh sieves; With hydroxypropyl emthylcellulose, sodium bicarbonate mixing, add 10%PVP (K30) alcoholic solution system soft material, 18 orders are granulated; 40 ℃ of dryings 2 ~ 4 hours, 16 mesh sieve granulate; Add magnesium stearate, mixing is processed sheet with the capsule shape punching press.
Claims (5)
1. a metformin hydrochloride intragastric floating sustained-release tablet is characterized in that being processed by following weight ratio by following component: metformin hydrochloride: 55%～65%; Matrix type material: 25%～35%; Gas generating agent: 4%～8%; Lubricant: 0.5%～2%; Binding agent: 0.5%～4%; Said matrix type material is hypromellose and octadecanol, and the weight ratio of hypromellose and octadecanol is 0.75～2: 1; The method for preparing of this metformin hydrochloride intragastric floating sustained-release tablet may further comprise the steps:
1) it is subsequent use that principal agent and adjuvant are all crossed 80 mesh sieves;
2) with the octadecanol melting, add metformin hydrochloride, stir, put coldly, pulverize, cross 80 mesh sieves;
3) with 2) with all the other matrix type materials, gas generating agent mixing, add binding agent system soft material, the granulation of 18 orders;
4) 40 ℃ of dryings are 2～4 hours, granulate;
5) add lubricant, compacting in flakes behind the mixing.
2. metformin hydrochloride intragastric floating sustained-release tablet according to claim 1 is characterized in that gas generating agent is a kind of in basic magnesium carbonate or the sodium bicarbonate.
3. metformin hydrochloride intragastric floating sustained-release tablet according to claim 2 is characterized in that gas generating agent is a sodium bicarbonate.
4. metformin hydrochloride intragastric floating sustained-release tablet according to claim 1 is characterized in that lubricant is one or more in magnesium stearate, Pulvis Talci, the micropowder silica gel.
5. metformin hydrochloride intragastric floating sustained-release tablet according to claim 1 is characterized in that binding agent is the water or the alcoholic solution of polyvinylpyrrolidone, hypromellose.
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| Application Number | Priority Date | Filing Date | Title |
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| CN200810019838XA CN101536989B (en) | 2008-03-18 | 2008-03-18 | Metformin hydrochloride intragastric floating sustained-release tablet and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200810019838XA CN101536989B (en) | 2008-03-18 | 2008-03-18 | Metformin hydrochloride intragastric floating sustained-release tablet and preparation method thereof |
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| CN101536989B true CN101536989B (en) | 2012-04-25 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN107898767B (en) * | 2018-01-03 | 2021-07-20 | 临沂大学 | Metformin hydrochloride sustained-release chewable tablet for dogs and preparation method thereof |
| CN108969501A (en) * | 2018-08-20 | 2018-12-11 | 奕利制药有限公司 | A kind of Metformin hydrochloride intragastric floating tablets and preparation method thereof |
| CN111450069A (en) * | 2020-04-02 | 2020-07-28 | 南京致中生物科技有限公司 | Metformin hydrochloride oral sustained-release tablet and preparation method thereof |
| CN112999182B (en) * | 2020-08-19 | 2023-04-07 | 重庆康刻尔制药股份有限公司 | Metformin hydrochloride dual sustained and controlled release composition and preparation method and application thereof |
| CN114404376A (en) * | 2022-03-16 | 2022-04-29 | 成都恒瑞制药有限公司 | Metformin hydrochloride sustained-release tablet and preparation method thereof |
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- 2008-03-18 CN CN200810019838XA patent/CN101536989B/en active Active
Non-Patent Citations (2)
| Title |
|---|
| 朴洪泽等.辅料因素对胃漂浮片的制备及漂浮能力的影响.《沈阳药科大学学报》.2008,第25卷(第2期),89-95. * |
| 顿彬.盐酸二甲双胍胃漂浮缓释片的研制.《中国优秀博硕士学位论文全文数据库(硕士)医药卫生科技辑》.2004,E079-35. * |
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