CN108543072A - A kind of composition for coating and its associated uses - Google Patents
A kind of composition for coating and its associated uses Download PDFInfo
- Publication number
- CN108543072A CN108543072A CN201810308504.8A CN201810308504A CN108543072A CN 108543072 A CN108543072 A CN 108543072A CN 201810308504 A CN201810308504 A CN 201810308504A CN 108543072 A CN108543072 A CN 108543072A
- Authority
- CN
- China
- Prior art keywords
- composition
- weight
- coating
- drug
- parts
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 110
- 239000011248 coating agent Substances 0.000 title claims abstract description 30
- 238000000576 coating method Methods 0.000 title claims abstract description 30
- 239000003814 drug Substances 0.000 claims abstract description 39
- 229940079593 drug Drugs 0.000 claims abstract description 34
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 30
- 108010010803 Gelatin Proteins 0.000 claims description 18
- 239000008273 gelatin Substances 0.000 claims description 18
- 229920000159 gelatin Polymers 0.000 claims description 18
- 235000019322 gelatine Nutrition 0.000 claims description 18
- 235000011852 gelatine desserts Nutrition 0.000 claims description 18
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 claims description 12
- 239000000661 sodium alginate Substances 0.000 claims description 12
- 235000010413 sodium alginate Nutrition 0.000 claims description 12
- 229940005550 sodium alginate Drugs 0.000 claims description 12
- 239000000845 maltitol Substances 0.000 claims description 7
- 235000010449 maltitol Nutrition 0.000 claims description 7
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 claims description 7
- 229940035436 maltitol Drugs 0.000 claims description 7
- 150000001720 carbohydrates Chemical class 0.000 claims description 6
- 235000014633 carbohydrates Nutrition 0.000 claims description 6
- 239000003002 pH adjusting agent Substances 0.000 claims description 6
- 239000003086 colorant Substances 0.000 claims description 5
- 235000019871 vegetable fat Nutrition 0.000 claims description 5
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 4
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims description 4
- 239000000796 flavoring agent Substances 0.000 claims description 4
- 235000013355 food flavoring agent Nutrition 0.000 claims description 4
- 239000008103 glucose Substances 0.000 claims description 4
- 235000001727 glucose Nutrition 0.000 claims description 3
- OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 claims description 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 2
- 239000005715 Fructose Substances 0.000 claims description 2
- 229930091371 Fructose Natural products 0.000 claims description 2
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 claims description 2
- GUBGYTABKSRVRQ-PICCSMPSSA-N Maltose Natural products O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-PICCSMPSSA-N 0.000 claims description 2
- 229930195725 Mannitol Natural products 0.000 claims description 2
- 229920002472 Starch Polymers 0.000 claims description 2
- GUBGYTABKSRVRQ-QUYVBRFLSA-N beta-maltose Chemical compound OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O GUBGYTABKSRVRQ-QUYVBRFLSA-N 0.000 claims description 2
- 239000000594 mannitol Substances 0.000 claims description 2
- 235000010355 mannitol Nutrition 0.000 claims description 2
- 235000019698 starch Nutrition 0.000 claims description 2
- 239000008107 starch Substances 0.000 claims description 2
- 239000000463 material Substances 0.000 abstract description 42
- 238000002360 preparation method Methods 0.000 abstract description 19
- 241000167880 Hirundinidae Species 0.000 abstract description 5
- 239000002994 raw material Substances 0.000 abstract description 3
- 239000007787 solid Substances 0.000 abstract description 2
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 21
- 238000000034 method Methods 0.000 description 14
- 238000002156 mixing Methods 0.000 description 14
- 230000000052 comparative effect Effects 0.000 description 12
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
- 239000008199 coating composition Substances 0.000 description 6
- 235000019484 Rapeseed oil Nutrition 0.000 description 5
- 238000003756 stirring Methods 0.000 description 5
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 4
- 239000002253 acid Substances 0.000 description 4
- 230000008859 change Effects 0.000 description 4
- 239000000470 constituent Substances 0.000 description 4
- 238000002425 crystallisation Methods 0.000 description 4
- 230000008025 crystallization Effects 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 3
- 239000003513 alkali Substances 0.000 description 3
- 238000001816 cooling Methods 0.000 description 3
- 239000002552 dosage form Substances 0.000 description 3
- 238000001727 in vivo Methods 0.000 description 3
- 238000004321 preservation Methods 0.000 description 3
- 230000009747 swallowing Effects 0.000 description 3
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
- NIPNSKYNPDTRPC-UHFFFAOYSA-N N-[2-oxo-2-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethyl]-2-[[3-(trifluoromethoxy)phenyl]methylamino]pyrimidine-5-carboxamide Chemical compound O=C(CNC(=O)C=1C=NC(=NC=1)NCC1=CC(=CC=C1)OC(F)(F)F)N1CC2=C(CC1)NN=N2 NIPNSKYNPDTRPC-UHFFFAOYSA-N 0.000 description 2
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 239000002801 charged material Substances 0.000 description 2
- 239000002285 corn oil Substances 0.000 description 2
- 235000005687 corn oil Nutrition 0.000 description 2
- 230000006837 decompression Effects 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 239000012528 membrane Substances 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 238000010792 warming Methods 0.000 description 2
- 235000005979 Citrus limon Nutrition 0.000 description 1
- 244000131522 Citrus pyriformis Species 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- 235000019482 Palm oil Nutrition 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- 235000011054 acetic acid Nutrition 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000036760 body temperature Effects 0.000 description 1
- 239000010495 camellia oil Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000001934 delay Effects 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 235000013399 edible fruits Nutrition 0.000 description 1
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000000284 extract Substances 0.000 description 1
- 235000019197 fats Nutrition 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- 235000011087 fumaric acid Nutrition 0.000 description 1
- 210000004051 gastric juice Anatomy 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 229960001031 glucose Drugs 0.000 description 1
- 239000003292 glue Substances 0.000 description 1
- 150000004676 glycans Chemical class 0.000 description 1
- 235000011167 hydrochloric acid Nutrition 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 230000010355 oscillation Effects 0.000 description 1
- 239000002540 palm oil Substances 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 229910000027 potassium carbonate Inorganic materials 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 235000012424 soybean oil Nutrition 0.000 description 1
- 239000003549 soybean oil Substances 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/42—Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Inorganic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention relates to composition for coating and its associated uses, the composition is with good stability, can be as the coating material of solid dosage medicine, and while improving drug mouthfeel, improve drug swallows performance.Meanwhile the raw material of the composition is easy to get, preparation method is simple, is easy to store.
Description
Technical field：
This application involves a kind of composition, can as needed to different drugs and relevant preparation, such as：Piece
Agent, pill etc. are coated, and obtained drug has the advantages that, for the different of individual particular demands, to prevent in favor of swallowing
Drug is rotten, extends the storage life etc. of drug.
Background technology：
The different dosage forms of drug can be made by being coated to the active constituent with medical usage, according to different purposes
Select different composition for coating or component that can realize different purposes, such as：Improve the preservation of wherein active constituent
Time, the drug after coating have more preferably rate of release, promote dissolving and absorption of active constituents of medicine etc. in vivo.Patent
The method and apparatus being coated on the drug of various dosage forms are disclosed in WO0051569, it is disclosed that the group of coating
Object is closed, but does not relate to the description of the specific proportioning and performance of this kind of composition.In the specification of patent CN102292077
A kind of coating composition and relevant coating technique are then further disclosed, wherein coating composition can be applied to a variety of differences
On the tablet of type.According to the description of the patent, coating composition has preferable stability, has specific viscoplasticity,
Suitable for being coated with all size and variform tablet in the same apparatus.
Inventor has found when being conducted further research to above-mentioned coated composition, although coating group in the prior art
Closing object has preferable stability, but it needs the pH value of adjusting coating composition in a certain range, the range and makes
The isoelectric point of gelatin is related.And in coating or coating, in order to be suitable for more tablets and other dosage forms, need
It wants the pH of the composition as possible close to neutrality, the coating of composition or the film after coating is avoided to influence the drug being coated
Property, such as：To the drug etc. of acid-sensitive.Also, there is still a need for the stability for further increasing coating composition so that
Either the composition can be stored the longer time or be capable of the warp of long period apparatus for coating containing the composition
It is tested by the preservation condition of the given areas such as firmly high temperature or high humidity.In addition, by being coated with or being coated, it is also desirable to meet simultaneously
Other particular demands, such as：It is more advantageous to and swallows, the quick release etc. of drug.
Inventor's discovery, can be into one by the basis of existing coating composition, adding a certain amount of sodium alginate
Step improves the stability of composition, delays the crystallization process of the material in composition.Sodium alginate belongs to one kind in polysaccharide, adds
Enter to change after sodium alginate the gel strength of composition, by adjusting the content of each component in composition, composition exists
While obtaining good rheological characteristic, the larger offset of the pH value of composition is avoided.The uncomfortable whole composition pH the case where
Under, so that it may to obtain good stability, avoid carbohydrate crystallization therein from generating crystallization, and system can be kept simultaneously
Good viscoplasticity.Meanwhile the pH that avoids composition itself may excessively high either too low situation and it is sensitive for acid or alkali
Drug for, can preferably prevent influence of the coating membrane of the composition to be formed to wherein drug ingedient, for a long time
It will not cause drug rotten when preservation and drug effect reduces, extend the use scope of this kind of composition.Furthermore, it is not necessary that adjustment
Composition pH also saves the preparation process of composition, simplifies preparation time.
Meanwhile applicant swallows to enable the drug after coating to be more advantageous to, group can be helped to swallow obstacle
People, or swallowed in the case where not needing water or a small amount of water, he a certain amount of vegetable oil is further added in the composition
Fat swallows performance improve composition.During carrying out the research, applicant chances on, to the pH of composition into
After row is adjusted, the stability of composition has obtained further raising, and the pH ranges after adjusting, with gelatin in composition
Isoelectric point be standard, difference be at least 1 when can achieve the effect that stability significantly improves.Although as previously mentioned, combination
The pH value variation of object can have influence to drug, but consider two factors, while improving system stability, combination
The pH value of object, which suitably raises and reduces, to be similarly advantageous.
Invention content：
The present invention provides a kind of composition for coating, the composition includes：
(1) carbohydrate of 60%-90% parts by weight, the carbohydrate it is chosen from the followings two or more
Arbitrary combination：Mannitol, glucose, maltitol, starch, fructose, maltose；
(2) gelatin of 0.5%-10% parts by weight；
(3) sodium alginate of 0.5%-10% parts by weight；And
(4) water of 2%-20% parts by weight.
Further, the composition also includes the vegetable fat of (5) 0.1%-15% parts by weight.
Further, the composition also includes the pH adjusting agent of (6) 0.1%-3% parts by weight.
Further, the pH of the composition is differed at least with the pH value of the isoelectric point of the gelatin used in the composition
It is 1.
Further, the composition also includes the colorant of (7) 0.1%-0.5% parts by weight；And/or 0.1%-
The flavoring agent of 0.5% parts by weight.
Wherein, gelatin can be type A gelatin or type B gelatin.
Wherein, vegetable fat is preferably palm oil, tea-seed oil, one kind or combinations thereof in soybean oil or corn oil, more
Preferably rapeseed oil.
Wherein, pH adjusting agent is selected from pharmaceutical acid as needed or alkali, acid are：Tartaric acid, fumaric acid, acetic acid, hydrochloric acid,
Sorbic acid, one kind or combinations thereof in citric acid, more preferably citric acid.Alkali is：Sodium hydroxide, sodium carbonate, tertiary sodium phosphate,
Potassium hydroxide, potassium carbonate, more preferably sodium hydroxide.
Wherein, the pigment that colorant preferably naturally extracts, flavoring agent are preferably natural flavouring.
Preferably, the weight percentage of the carbohydrate is 65%-85%.
Preferably, the weight percentage of the gelatin is 0.8%-10%.
Preferably, the weight percentage of the sodium alginate is 0.7%-10%.
Preferably, the weight percentage of the vegetable fat is 5%-15%.
Preferably, the weight percentage of the pH adjusting agent is 0.5%-1.2%.
The present invention also provides be applied to disposably wrap drug for individual in need by the composition
The purposes of clothing.
The present invention also provides the composition is applied to needing the drug preserved temporarily or for a long time to wrap
The purposes of clothing.
The present invention also provides the composition is applied to being difficult to swallow or the drug directly swallowed being needed to carry out
Coating, the purposes of performance is swallowed to improve it.
The present invention adjusts the dosage of water by adding sodium alginate in the composition, can keep stability and good
Well viscoelastic simultaneously, avoids the adjustment to composition system pH value.The combination produce formed after adding vegetable fat
The excellent performance for being beneficial to swallow has been given birth to, it can be in the case where not needing water or little water, after being coated to drug
Directly swallowed.After the pH value range of adjustment composition, better stability is obtained, can adapt to various different situations
Under storage condition, the drug after coating can be preserved preferably.It takes several times for needing to divide or needs once to subtract
The solid drugs of few taking dose, the drug after being coated by hand can for a long time be stored without going bad.
The composition of the present invention can also be used to directly be coated active constituents of medicine, using existing technology and set
It is standby, after adding the other medicines auxiliary materials such as flavoring agent or colorant appropriate, it is directly prepared into final drug and is sold.
Specific implementation mode：
The raw material used in the present invention is food grade materials, or can be medicinal auxiliary material, these raw materials can pass through
Commercially available purchase obtains.
Embodiment 1：
The preparation method of composition for coating：By maltitol, sodium alginate and suitable water are mixed at 50 DEG C to object
Material dissolving, record are added the weight of water, obtain material A.The water of gelatin and its 3 times amounts is mixed at 70 DEG C, stirs evenly, obtains
To material B.Material A is added in material B, 90 DEG C are slowly warming up to after stirring evenly, maintains this temperature, and carry out to system
Decompression operation calculates the total of the moisture and composition for needing to remove according to charged material weight to evaporate wherein extra moisture
Weight.It when the moisture in system reaches requirement, stops operation, the composition natural cooling that will be obtained.
Embodiment 2：
The preparation manipulation method of composition is 55 DEG C with embodiment 1, the wherein mixing temperature of material A part, evaporable water
Temperature be 95 DEG C.
Embodiment 3：
The preparation manipulation method of composition is 45 DEG C with embodiment 1, the wherein mixing temperature of material A part, material part B
Mixing temperature be 65 DEG C, the water in material B is 2.5 times of amounts of gelatin weight.The temperature of evaporable water is 93 DEG C.
Embodiment 4：
The preparation manipulation method of composition is with embodiment 1, and by maltitol, sodium alginate and suitable water mix at 50 DEG C
It is bonded to material dissolution, writes down the weight of water, obtains material A 1.Water in material B is 3 times of amounts of gelatin weight, material part B
Mixing temperature is 75 DEG C.Material A 1 and rapeseed oil are added in material B and are stirred mixing.When system is evaporated moisture
Temperature be 93 DEG C.
Embodiment 5：
The preparation manipulation method of composition is 60 DEG C with embodiment 4, the wherein mixing temperature of 1 part of material A, the portions material B
The mixing temperature divided is 65 DEG C, and the water in material B is 3 times of amounts of gelatin weight.The temperature of evaporable water is 95 DEG C.
Embodiment 6：
The preparation manipulation method of composition replaces with citric acid with embodiment 4, by the rapeseed oil in embodiment 4, is added to
In material B.Also, temperature when system is evaporated moisture is 95 DEG C.
Embodiment 7：
The preparation manipulation method of composition exists maltitol, glucose, sodium alginate and suitable water with embodiment 4
It is mixed to material dissolution at 55 DEG C, records the weight of water, obtain material A 1.Water in material B is 3 times of amounts of gelatin weight, object
Expect that the mixing temperature of part B is 70 DEG C.By material A 1 and corn oil, citric acid, which is added in material B, is stirred mixing.Body
Temperature when system is evaporated moisture is 95 DEG C.
Embodiment 8：
The preparation manipulation method of composition is the same as embodiment 7.
Embodiment 9：
The preparation manipulation method of composition is 55 DEG C with embodiment 7, the wherein mixing temperature of 1 part of material A.
Embodiment 10：
The preparation manipulation method of composition is 50 DEG C with embodiment 7, the wherein mixing temperature of 1 part of material A.
Embodiment 11：
The preparation manipulation method of composition is 50 DEG C with embodiment 7, the wherein mixing temperature of 1 part of material A, material A 1,
Rapeseed oil, citric acid are added in material B and are stirred, and add colorant lemon yellow and futher stir mixing.System carries out
Temperature when evaporable water is 90 DEG C.
Comparative example 1：
The preparation method of composition is：Maltitol and suitable water are mixed to dissolving, record is added the weight of water, obtains
To material A.The water of gelatin and its 5 times amounts is mixed at 75 DEG C, stirs evenly, obtains material B.Material A is added to material B
In, it is slowly warming up to 85 DEG C after stirring evenly, maintains this temperature, and decompression operation is carried out to evaporate wherein extra water to system
Point, the total weight of the moisture and composition that need to remove is calculated according to charged material weight.It is needed when the inventory in system reaches
It when the proportioning wanted, stops operation, obtained composition natural cooling.
Comparative example 2：
The preparation method of composition is different only without addition citric acid with embodiment 6, and fits as needed
When the weight ratio for having adjusted water.
Comparative example 3：
The preparation method of composition is similar to embodiment 8, except that the sodium alginate in embodiment 8 is replaced with reality
Same gelatin in example 8 is applied, and in the preparation by maltitol, glucose adds water to be dissolved to obtain material A 1, in addition will
Gelatin obtains material B in water, and by material A 1 and rapeseed oil, citric acid, which is added in material B, is stirred mixing.
System evaporable water, it is cooling to be made.
Embodiment 12：Stability test
1, according to the description in patent CN102292077 specifications such as the 149th section, the most suitable composition of patent
And the stability conditions of formulation samples are：By in the gas-tight container of sample storage at about room temperatures, when by storage 1 year
Any significant changes of consistency, appearance or taste are not shown.
According to the storage method described in the patent, by embodiment 1-11, the composition that comparative example 1-3 is prepared is placed
In gas-tight container, it is placed at room temperature for and appointing for consistency and appearance etc. is not observed within 1 year, embodiment 1-11, comparative example 2-3
What significant change, and the sample of comparative example 1 then starts to crystallize in initial one month, and consistency has occurred significantly
Variation.The experiment shows that the stability of the composition of comparative example 1 is poor, is not suitable for long-term storage.It proves simultaneously provided by the invention
The stability of the composition of embodiment 1-11 is no worse than the composition in patent CN102292077.
2, accelerated test：
By embodiment 1-3,5-6,7-8,11 composition being prepared and the composition of comparative example 1-3, it is in temperature
It 40 ± 2 DEG C, places 0,3,6 months under conditions of relative humidity 75%RH ± 5%RH, investigates the stability of composition sample, tie
Fruit is shown in Table 1.
Table 1
According to the result of table 1 it is found that after 3rd month, the composition of embodiment 1-3,5-8,11 and comparative example 2
Composition does not change significantly, and the composition of comparative example 3 starts to change, and composition system is changed.Card
It is bright after addition sodium alginate, equally to improve the stability of composition in composition system.And after 6th month, do not have
The embodiment 1-3 of pH adjusting agent is added, 5 sample stability also begins to occur reducing, and a small amount of crystallization occurs.And it is added
Sample after pH adjusting agent is then without occurring apparent variation, it was demonstrated that after further adjusting pH value, the stability of composition
Further raising has been obtained, the longer time can be stored.
Embodiment 13：Ftheoloqical measurements are tested
The composition of composition and comparative example 3 for the embodiment 1-11 present invention being prepared carries out system
Rheological parameters measure, and specifically determine elastic modulus G ', viscous modulus G ", to determine the rheological property of these compositions.
According to the inventor's study, when the elastic modulus G ' of system, viscous modulus G " in a certain range when, composition has good
Viscosity and elasticity can be more advantageous to the coating membrane to form uniform and thin layer when being coated to medicament.And energy
It is enough more advantageous to and swallows, while will not cause to take object and generate too hard or too glutinous sense of discomfort when swallowing.
It is 30mm in plate diameter, tablet gap is 2mm, and temperature is using the advanced rheometer of Physica MCR301 types
Under conditions of 25 DEG C, using oscillation mode, in the frequency range of 0.01-1000Hz, to the elastic modulus G ' of sample, glue
Property modulus G " has carried out sweep measuring.
Range of the elastic modulus G ' of embodiment 1-11 and the sample of comparative example 3 at 0.1Hz in 200-20000Pa
Interior, viscous modulus G " is in the range of 200-30000Pa, and the elastic modulus G ' at 10Hz is 2000-1000000Pa's
In range, viscous modulus G " is in the range of 2000-1000000Pa.Such as：The composition of embodiment 8 is 0.01Hz-60Hz's
Elastic modulus G ' in range is less than viscous modulus G ", and in about 60Hz, elastic modulus G ' and viscous modulus G " are equal, and
When the frequency of 60Hz or more, the elastic modulus G ' of composition starts to be more than viscous modulus G ", and elastic modulus G ' and sticky mould
There is a degree of reduction with the increase that continues of frequency in amount G ".
Test result proves the composition of the present invention, has viscoplasticity appropriate under specific frequency, belongs to typical
Viscoelastic systems, while the correspondence of elasticity modulus, viscous modulus and frequency shows the composition of the present invention when being swallowed,
Performance is swallowed with good help.
By using the composition of the present invention, on the basis of obtaining excellent helping and swallowing performance, while can also protect
The pH value of composition system is held closer to neutrality.And in the case where not influencing drug, it can also be obtained more by adjusting pH
Excellent stability.This not only makes the stability of composition system be improved, but also ensure that composition connects with drug
When touching, the performance of drug itself can not be influenced, reduces the possibility for causing drug rotten, equally also improves medicine after coating
The storage time of object.In addition, the composition of the present invention is tests prove that also have good dissolubility energy, in the item of simulate the gastric juice
Under part (0.1mol/l hydrochloric acid), the composition that embodiment is prepared can dissolve rapidly in vivo (when be limited to 3 minutes with
It is interior), do not interfere with the release and absorption of drug in vivo.
Test operation described in the specification, which is those skilled in the art, to be carried out according to the Conventional wisdom of this field.
And the preferred embodiment that the embodiment in specification embodiment is the present invention, those skilled in the art can carry out certain to it
It modification, adjustment and replaces, it is this without changing the spirit and scope of the invention, and the modification for its effect that has the ability to anticipate and replace
It changes, and apparent adjustment, deformation, should all be comprised in the scope of the present invention, fall into the scope of protection of present invention.
Claims (8)
1. a kind of composition for coating, it is characterised in that the composition includes：
(1) carbohydrate of 60%-90% parts by weight, the carbohydrate two or more times chosen from the followings
Meaning combination：Mannitol, glucose, maltitol, starch, fructose, maltose；
(2) gelatin of 0.5%-10% parts by weight；
(3) sodium alginate of 0.5%-10% parts by weight；And
(4) water of 2%-20% parts by weight.
2. composition for coating according to claim 1, it is characterised in that the composition also includes：
(5) vegetable fat of 0.1%-15% parts by weight.
3. according to the composition for coating described in claim 1-2, it is characterised in that the composition also includes：
(6) pH adjusting agent of 0.1%-3% parts by weight.
4. according to the composition for coating described in claim 2-3, it is characterised in that the pH and the composition of the composition
Used in gelatin isoelectric point pH value difference be at least 1.
5. according to the composition for coating described in claim 1-4, it is characterised in that the composition also includes：
(7) colorant of 0.1%-0.5% parts by weight；And/or the flavoring agent of 0.1%-0.5% parts by weight.
6. a kind of purposes of the composition for coating described in claim 1-5, it is characterised in that the composition can be used for having
The individual needed is disposably coated drug.
7. a kind of purposes of the composition for coating described in claim 1-5, it is characterised in that the composition can be used for pair
The drug preserved is needed to be coated.
8. a kind of purposes of the composition for coating described in claim 1-5, it is characterised in that the composition can be used for pair
It is difficult to swallow or the drug directly swallowed is needed to be coated, performance is swallowed to improve it.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810308504.8A CN108543072A (en) | 2018-04-09 | 2018-04-09 | A kind of composition for coating and its associated uses |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810308504.8A CN108543072A (en) | 2018-04-09 | 2018-04-09 | A kind of composition for coating and its associated uses |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN108543072A true CN108543072A (en) | 2018-09-18 |
Family
ID=63514156
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201810308504.8A Pending CN108543072A (en) | 2018-04-09 | 2018-04-09 | A kind of composition for coating and its associated uses |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN108543072A (en) |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102292077A (en) * | 2009-01-20 | 2011-12-21 | 迈德涂料公司 | A new coating composition and use thereof |
| CN104857520A (en) * | 2015-04-29 | 2015-08-26 | 南京圣诺生物科技实业有限公司 | Sodium alginate coating liquid composition and coating method |
| CN105007949A (en) * | 2013-03-08 | 2015-10-28 | 狮王株式会社 | Coating composition, coated preparation and method for producing same |
| CN107865969A (en) * | 2016-09-28 | 2018-04-03 | 狮王株式会社 | Coated composition, coated preparation and its manufacture method |
-
2018
- 2018-04-09 CN CN201810308504.8A patent/CN108543072A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102292077A (en) * | 2009-01-20 | 2011-12-21 | 迈德涂料公司 | A new coating composition and use thereof |
| CN105007949A (en) * | 2013-03-08 | 2015-10-28 | 狮王株式会社 | Coating composition, coated preparation and method for producing same |
| CN104857520A (en) * | 2015-04-29 | 2015-08-26 | 南京圣诺生物科技实业有限公司 | Sodium alginate coating liquid composition and coating method |
| CN107865969A (en) * | 2016-09-28 | 2018-04-03 | 狮王株式会社 | Coated composition, coated preparation and its manufacture method |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP3649742B2 (en) | Sugar-free sugar coating products | |
| TW201601733A (en) | Clay compositions | |
| JP2020055856A (en) | Compositions as auxiliary means for oral drugs | |
| CN107812195A (en) | The stabilizing pharmaceutical composition of (6S) 5 methyl tetrahydrofolate calcium salt | |
| CN101495467A (en) | Method for preventing coloration of catechins and dentifrice composition | |
| US8911816B2 (en) | Coating composition and use thereof | |
| US4258179A (en) | Coating agents for solid medicaments | |
| JP6942342B2 (en) | Soft capsule film | |
| JP2019136036A (en) | Liquid food | |
| JP6365235B2 (en) | Liquid composition | |
| KR101144460B1 (en) | Chinese herbal medical composition in the form of jelly | |
| CN108578704A (en) | A kind of composition and its associated uses for swallowing | |
| JP7418679B2 (en) | Delayed gelling composition | |
| KR101175163B1 (en) | Isosorbide-containing jelly preparation | |
| CN108543072A (en) | A kind of composition for coating and its associated uses | |
| Ramu et al. | Preliminary investigation of patchaippasali mucilage (Basella alba) as tablet binder | |
| KR20080071557A (en) | Solid Formulations and Formulation Compositions | |
| WO2005011402A1 (en) | Masticatable capsule and process for producing the same | |
| JP7262894B2 (en) | JELLY GRANULATE AND FOOD CONTAINING THE JELLY GRANULE | |
| CN110448538A (en) | N-acetylglucosamine capsule preparations and preparation method thereof | |
| JP7366306B1 (en) | Method for manufacturing turmeric-containing tablets | |
| US10960076B2 (en) | Gummy dosage forms comprising serine | |
| JP6342552B1 (en) | Medication aids | |
| TW202327624A (en) | Sucralfate-containing jelly-like pharmaceutical composition | |
| JPS58103314A (en) | Tablet type guaiac grain oral administration and manufacture |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20180918 |