Application of Polyacrylic Resin Pharmaceutical Excipients in Solid Preparations
2019-07-25 00:02:04
Application of Polyacrylic Resin Pharmaceutical Excipients in Solid Preparations Acrylic resins are made by copolymerizing acrylic acid, methacrylic acid and vinegar with each other. Due to different compositions, different proportions and different degrees of polymerization, the product model and specifications are Different, foreign products are collectively called Eudragit, which have Eu-dragitE, L, S, RL, RS, etc., and China produces resin I.II, III. EudragitE and Resin II are copolymerized with dimethylamino methacrylate and other neutral methacrylic acids; Eudragit L. S, Resin I.II, III are methacrylic acid and methacrylic acid in different proportions. Copolymerized; Eudra-gitRL (10% trimethylamine methacrylate), RS (containing 5% trimethylamine methacrylate) is a copolymer of acrylic acid and methacrylic acid vinegar containing certain quaternary amine genes. Object.
They have a continuous hydrocarbon chain structure, are stable in the stomach, are not destroyed by digestive enzymes, and swell in body fluids; but they are not absorbed and do not participate in human physiological metabolism. After oral administration, it is quickly discharged by constant molecular formation and is harmless to the human body. It is widely used in solid preparations such as tablets, pills, granules and traditional Chinese medicine preparations, and is an excellent new auxiliary material. This article provides an overview of its application in this area.
Enteric film coating material
No. 1 resin emulsion liquid is used as enteric film coating material, water is dispersion. It is not solvent. Therefore, water can be evaporated quickly when the film is dry; 30% (W/W) film-forming material can be added. A human 3% (W/W) triacetin is used as a plasticizer, and it can be used by diluting with a certain amount of water, or it can be made into a colored film. The basic prescription of II, III resin coating liquid is shown in the attached table (omitted).
The resin No. II has a poor appearance, but the coating is not easy to adhere; the No. III resin is easy to form a film, and the gloss is good, but it is easy to stick. The practical application is a mixture of a certain proportion of the two. Applying the mixture of II and III to the full film coating of the sylvestre tablets, the results show that the film is tightly wrapped, the coat layer is solid, the appearance is ideal, and it is excellent in moisture resistance, heat resistance, friability and disintegration. In the case of enteric coated sugar tablets. There is also an enteric coating material which uses No. II resin as a traditional Chinese medicine extract sheet.
2. Gastric film coating material
Resin II quickly dissolved at pH 1-4 and swelled at pH 5%. It does not affect the efficacy of patients with too little gastric acid; the product is stable in nature, inert to the enzyme system, and does not cause prolongation of disintegration. It has good film forming properties, good gloss, toughness and moisture resistance. The film coating of the daning tablets is carried out by mixing the resin No. II with HPMC, and has the advantages of light weight, short coating time and good moisture resistance, which is unmatched by ordinary sugar-coated tablets. Resin II can be coated separately or in combination, and mixed with HPMC can increase film formability, disintegration degree and bioavailability; mixing with corn can improve moisture resistance.
3. Protective clothing material
Generally, the tablet has a slightly bitter taste or odor, and can be coated into a thin protective coat layer by appropriately adjusting the ratio of the II and III resin formulations. It can not only dissolve quickly but also make one-side light, no smell, easy to swallow. Prescription No. II: III resin (1:1) 3g; PEG-6 000 6g; Tween-80 1m1; castor oil 2m1; phthalic acid diethyl vinegar 7m1; ethanol 100m1; silicone oil 0. 5m1. Prescription 2, II resin 5 0r6 20m1 (ethanol solution); HPMC3 46100m1 (ethanol solution); phthalic acid diethyl vinegar 1m1; castor oil lml; Tween lml; talc powder 2-4g; PEG-6 000.1g; Moderate amount.
4. Adhesive material
Different concentrations of polyacrylic resin can be used as a binder for granulation. It has the ability to increase the compressibility of the particles, isolate the particle components and reduce the moisture absorption of the particles and tablets. The acetaminophen tablets are prepared by using 10% concentration II resin, which improves the compressibility, reduces the brittleness, and has no change in the absorption rate; The sodium granules reduce the wettability. The preparation of the sputum hepatic granules and the chloroacetic granules respectively improve the compressibility and stability.
5. Skeletal sustained release sheet material
The polyacrylic resin and the drug are made into an insoluble skeleton sustained-release tablet. After the tablet is taken, the drug is gradually released in the gastrointestinal tract, and the skeleton is discharged without change. The skeleton can form intricate pores with extremely fine pores, and the drug slowly diffuses into the body fluid through the pores to achieve sustained release. The type of acrylic resin and its amount can affect the release rate, select the appropriate type of acrylic resin, and determine the appropriate drug and resin ratio is the key to the speed of controlled release drugs. Different types of resins have different penetrating properties, and the use of different penetrating properties resins can achieve the desired release rate. In the poorly penetrating resin, some water-soluble substances such as PVP can be added to increase the penetration. Aspirin tablets are prepared with Eudragit S-100, and the drug release lasts for 8 hours.
6. Hui ball material
Insulin microspheres were prepared with Eudragit L-100 and Eudragit S-100, releasing more than 90% insulin in 60 minutes at pH 7.5. The hypoglycemic effect was remarkable after taking Eudragit L-100 to prepare insulin microspheres. Eu-dragit L-100 insulin microspheres were released in the lower part of the small intestine in rabbits. And atropine promotes its absorption. Therefore, an acrylic resin can be used as a carrier to bring insulin to a specific absorption site in the intestine, and oral insulin can be administered.
7. Enteric Huiban materials
In order to reduce the side effects of the drug on gastric irritation, acrylic resin can be used as a microcapsule material to release the drug in the small intestine. Ibuprofen microcapsules were prepared using Eudragit L-100-55 to slowly release the drug in the small intestine, reducing side effects.
8. Solid dispersion material
Acrylic resins are also widely used in the preparation of slow release solid dispersions. There are two preparation methods for such dispersions: (1) solvent evaporation, and (2) coprecipitation. Ibuprofen solid dispersion In this method, ibuprofen and Eudragit L-100, Eu-dragit S-100 are first dissolved in acetone, and the acetone solution is poured into 100 ml of distilled water with gentle agitation at 10 ° C. The dissolution test showed that ibuprofen released 50% in Eudragit L-100 and Eudragit S-100 co-precipitate for 5 h, and the drug release was nearly complete at 8 h.
9. Pellet material
The rifampicin pellets were prepared using Eudragit RS-100, and the pellet size was affected by the ratio of the drug and Eudragit RS-100 and the stirring speed. The release time was affected by the size of the pellet and the ratio of the drug to the Eudragit ratio.
Source: China Pharmacy Author: Affiliated Hospital of Hubei Medical University, Department of Pharmacy, Rowan
They have a continuous hydrocarbon chain structure, are stable in the stomach, are not destroyed by digestive enzymes, and swell in body fluids; but they are not absorbed and do not participate in human physiological metabolism. After oral administration, it is quickly discharged by constant molecular formation and is harmless to the human body. It is widely used in solid preparations such as tablets, pills, granules and traditional Chinese medicine preparations, and is an excellent new auxiliary material. This article provides an overview of its application in this area.
Enteric film coating material
No. 1 resin emulsion liquid is used as enteric film coating material, water is dispersion. It is not solvent. Therefore, water can be evaporated quickly when the film is dry; 30% (W/W) film-forming material can be added. A human 3% (W/W) triacetin is used as a plasticizer, and it can be used by diluting with a certain amount of water, or it can be made into a colored film. The basic prescription of II, III resin coating liquid is shown in the attached table (omitted).
The resin No. II has a poor appearance, but the coating is not easy to adhere; the No. III resin is easy to form a film, and the gloss is good, but it is easy to stick. The practical application is a mixture of a certain proportion of the two. Applying the mixture of II and III to the full film coating of the sylvestre tablets, the results show that the film is tightly wrapped, the coat layer is solid, the appearance is ideal, and it is excellent in moisture resistance, heat resistance, friability and disintegration. In the case of enteric coated sugar tablets. There is also an enteric coating material which uses No. II resin as a traditional Chinese medicine extract sheet.
2. Gastric film coating material
Resin II quickly dissolved at pH 1-4 and swelled at pH 5%. It does not affect the efficacy of patients with too little gastric acid; the product is stable in nature, inert to the enzyme system, and does not cause prolongation of disintegration. It has good film forming properties, good gloss, toughness and moisture resistance. The film coating of the daning tablets is carried out by mixing the resin No. II with HPMC, and has the advantages of light weight, short coating time and good moisture resistance, which is unmatched by ordinary sugar-coated tablets. Resin II can be coated separately or in combination, and mixed with HPMC can increase film formability, disintegration degree and bioavailability; mixing with corn can improve moisture resistance.
3. Protective clothing material
Generally, the tablet has a slightly bitter taste or odor, and can be coated into a thin protective coat layer by appropriately adjusting the ratio of the II and III resin formulations. It can not only dissolve quickly but also make one-side light, no smell, easy to swallow. Prescription No. II: III resin (1:1) 3g; PEG-6 000 6g; Tween-80 1m1; castor oil 2m1; phthalic acid diethyl vinegar 7m1; ethanol 100m1; silicone oil 0. 5m1. Prescription 2, II resin 5 0r6 20m1 (ethanol solution); HPMC3 46100m1 (ethanol solution); phthalic acid diethyl vinegar 1m1; castor oil lml; Tween lml; talc powder 2-4g; PEG-6 000.1g; Moderate amount.
4. Adhesive material
Different concentrations of polyacrylic resin can be used as a binder for granulation. It has the ability to increase the compressibility of the particles, isolate the particle components and reduce the moisture absorption of the particles and tablets. The acetaminophen tablets are prepared by using 10% concentration II resin, which improves the compressibility, reduces the brittleness, and has no change in the absorption rate; The sodium granules reduce the wettability. The preparation of the sputum hepatic granules and the chloroacetic granules respectively improve the compressibility and stability.
5. Skeletal sustained release sheet material
The polyacrylic resin and the drug are made into an insoluble skeleton sustained-release tablet. After the tablet is taken, the drug is gradually released in the gastrointestinal tract, and the skeleton is discharged without change. The skeleton can form intricate pores with extremely fine pores, and the drug slowly diffuses into the body fluid through the pores to achieve sustained release. The type of acrylic resin and its amount can affect the release rate, select the appropriate type of acrylic resin, and determine the appropriate drug and resin ratio is the key to the speed of controlled release drugs. Different types of resins have different penetrating properties, and the use of different penetrating properties resins can achieve the desired release rate. In the poorly penetrating resin, some water-soluble substances such as PVP can be added to increase the penetration. Aspirin tablets are prepared with Eudragit S-100, and the drug release lasts for 8 hours.
6. Hui ball material
Insulin microspheres were prepared with Eudragit L-100 and Eudragit S-100, releasing more than 90% insulin in 60 minutes at pH 7.5. The hypoglycemic effect was remarkable after taking Eudragit L-100 to prepare insulin microspheres. Eu-dragit L-100 insulin microspheres were released in the lower part of the small intestine in rabbits. And atropine promotes its absorption. Therefore, an acrylic resin can be used as a carrier to bring insulin to a specific absorption site in the intestine, and oral insulin can be administered.
7. Enteric Huiban materials
In order to reduce the side effects of the drug on gastric irritation, acrylic resin can be used as a microcapsule material to release the drug in the small intestine. Ibuprofen microcapsules were prepared using Eudragit L-100-55 to slowly release the drug in the small intestine, reducing side effects.
8. Solid dispersion material
Acrylic resins are also widely used in the preparation of slow release solid dispersions. There are two preparation methods for such dispersions: (1) solvent evaporation, and (2) coprecipitation. Ibuprofen solid dispersion In this method, ibuprofen and Eudragit L-100, Eu-dragit S-100 are first dissolved in acetone, and the acetone solution is poured into 100 ml of distilled water with gentle agitation at 10 ° C. The dissolution test showed that ibuprofen released 50% in Eudragit L-100 and Eudragit S-100 co-precipitate for 5 h, and the drug release was nearly complete at 8 h.
9. Pellet material
The rifampicin pellets were prepared using Eudragit RS-100, and the pellet size was affected by the ratio of the drug and Eudragit RS-100 and the stirring speed. The release time was affected by the size of the pellet and the ratio of the drug to the Eudragit ratio.
Source: China Pharmacy Author: Affiliated Hospital of Hubei Medical University, Department of Pharmacy, Rowan
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