The composition of coated compressed tablets uses a coating mixture of chitosan or chitosan salts with a hydrophobic polymer for drug delivery to facilitate action or absorption in the large intestine.

Abstract

DC60 (18 / 06 / 51) Compressed tablets coated with chitosan or chitosan salts, such as chitosan acetate, are examples of tablets containing chitosan. Chitosan aspartate, chitosan lactate, chitosan hydrochloride, chitosan glutamate, or chitosan glycolate. And ethyl cellulose is used as a coating to deliver the drug for release in the large intestine, with the following steps: Preparation of chitosan salts by spray drying technique using chitosan of specific molecular weight and degree of Various deacetylation processes are used to prepare core tablets weighing approximately 100-200 mg with a diameter of approximately 6 cm. Using 5-aminosalicylic acid as a drug model, the core of the tablet was coated by compression molding with a coating substance. It is a mixture of chitosan or chitosan salt and ethyl cellulose in a percentage EC weight ratio:chitosan salt. The dosage of Xan is between 95:5 and 5:95, using approximately 200-300 mg of coating agent, with an overall tablet weight of approximately 300 mg. The 500mg tablet, approximately 10mm in diameter, features a controlled-release mechanism. At least four mechanisms involve drug release through mediators that mimic gastric and intestinal digestive juices in 5-6 stages. Within the first hour, no more than 10% of the drug is released into the digestive medium of the large intestine, and more than 90% is released within the time frame. 24 hours Compressed tablets coated with chitosan or chitosan salts, such as chitosan acetate, are examples of tablets containing chitosan. Chitosan aspartate, chitosan lactate, chitosan hydrochloride, chitosan glutamate, or chitosan chlorate. And ethyl cellulose is used as a coating to deliver the drug for release in the large intestine, with the following steps: Preparation of chitosan salts by spray drying technique using chitosan of specific molecular weight and degree of Various deacetylation processes are used to prepare core tablets weighing approximately 100-200 mg with a diameter of approximately 6 cm. Using 5-aminosalicylic acid as a drug model, the core of the tablet was coated by compression molding with a coating substance. It is a mixture of chitosan or chitosan salt and ethyl cellulose in a percentage EC weight ratio:chitosan salt. The dosage of Xan is between 95:5 and 5:95, using approximately 200-300 mg of coating agent, with an overall tablet weight of approximately 300 mg. The 500mg tablet, approximately 10mm in diameter, features a controlled-release mechanism. At least four mechanisms involve drug release through mediators that mimic gastric and intestinal digestive juices in 5-6 stages. Within the first hour, no more than 10% of the drug is released into the digestive medium of the large intestine, and more than 90% is released within the time frame. 24 hours;

Claims

1. The composition of coated compressed tablets consists of a core tablet containing 5-70% by weight of the compressed tablet components and a hydrophobic coating mixture capable of delivering the active ingredient or substances absorbed in the large intestine at a rate of 30-95% by weight of the compressed tablet components. The coating mixture contains a ratio of hydrophobic coating to chitosan or chitosan salts in a ratio of 95:5 to 5:95 by weight of the coating mixture. Such compressed tablets have at least four controlled-release mechanisms, with drug release in the gastric or intestinal simulated medium in the first 5-6 hours not exceeding 10%, and drug release in the gastric or intestinal simulated medium within 24 hours exceeding 90%.

2. The composition of coated compressed tablets as per claim 1, where the core tablet consists of a mixture of the active ingredient, a superdissolving agent, a diluent, and a lubricant. 3.The composition of coated compressed tablets under patent 2 where the active ingredient can be selected from the group of 5-aminosalicylic acid, therapeutic agents for colitis, and agents intended for transcolonization; 4. The composition of coated compressed tablets under either patent 2 or 3 where the aforementioned active ingredient is present at 5-70% by weight of the composition; 5. The composition of coated compressed tablets under either patent 2 or 4 where the superdissolving agent is sodium starch glycolate; 6. The composition of coated compressed tablets under...

7. Any one of the coating compressed tablet components under claims 2 to 6 where the diluent is directly compressed.

8. Any one of the coating compressed tablet components under claims 2 to 6 where the diluent is prepared in granule form.

9. Any one of the coating compressed tablet components under claims 2 to 8 where the diluent is selectable from the alpha-lactose monohydrate and dicalcium phosphate groups. 10.

10. The composition of coated compressed tablets under any one of Patents 2 to 9 where the said diluent is present at 0-60% by weight of the compressed tablet composition.

11. The composition of coated compressed tablets under any one of Patents 2 to 10 where the lubricant is magnesium stearate.

12. The composition of coated compressed tablets under any one of Patents 2 to 11 where the said lubricant is present at 0-10% by weight of the core tablet.

13. The composition of coated compressed tablets under any one of Patents 1 to 12 where the said lubricant is present at 0-10% by weight of the core tablet.

14. A pharmaceutical ingredient pursuant to any one of the claims 1-13 in which chitosan salts are selectable from the group of chitosan acetate, chitosan aspartate, chitosan lactate, chitosan hydrochloride, chitosan glutamate, and chitosan glucocholate.

15. A pharmaceutical ingredient pursuant to claim 14 in which chitosan salts are obtained by spray drying of a mixed solution of chitosan and acid of that chitosan salt, which can be selected from the group of acetic acid, aspartic acid, hydrochloric acid, glutamic acid, glycolic acid, and lactic acid. 16.

17. The composition of coated compressed tablets under any one of Patents 1 to 13 where the chitosan salt is chitosan acetate.

18. The composition of coated compressed tablets under any one of Patents 1 to 16 where the coating mixture is a mixture of chitosan or chitosan salt:ethyl cellulose in a ratio of 90:10 to 85:15, respectively.

19. The composition of coated compressed tablets under any one of Patents 1 to 16 where the coating mixture is a mixture of chitosan or chitosan salt with ethyl cellulose in a ratio... Ratio 87.5:12.

519. Composition of any coated compressed tablet under patents 1-18 in which chitosan and such chitosan salts have a molecular weight of 10-2000 kDa.

20. Composition of any coated compressed tablet under patents 1-19 which has a controlled-release mechanism which is time-controlled system, pH-controlled system, enzyme-controlled system, or tablet disintegration effect. 21.

21. Any component of a coated compressed tablet under claims 1-20 which has a release of more than 90% of the drug in the colonic digestive medium within 12 hours; 22. Any component of a coated compressed tablet under claims 1-21 which is a coated compressed tablet with a hardness of 5-30k;