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Details for Patent: 6,436,441

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Details for Patent: 6,436,441

Title: Hydrogel-forming sustained-release preparation
Abstract:The invention provides a hydrogel-type sustained-release preparation comprising (1) at least one drug, (2) an additive which insures a penetration of water into the core of the preparation and (3) a hydrogel-forming polymer, wherein said preparation is capable of undergoing substantially complete gelation during its stay in the upper digestive tract such as stomach and small intestine and is capable of releasing the drug in the lower digestive tract including colon. By the preparation of the invention, the drug is efficiently released and absorbed even in the colon so that a steady and sustained release effect can be achieved.
Inventor(s): Sako; Kazuhiro (Shizuoka, JP), Nakashima; Hiroshi (Shizuoka, JP), Sawada; Toyohiro (Shizuoka, JP), Okada; Akira (Shizuoka, JP), Fukui; Muneo (Shizuoka, JP)
Assignee: Yamanouchi Pharmaceutical Co., Ltd. (Tokyo, JP)
Filing Date:Mar 20, 1995
Application Number:08/403,752
Claims:1. A method for providing drug-release not only in the upper digestive tract including stomach and small intestine but also in the lower digestive tract including the colon, comprising the steps of: (A) orally administering a preparation having a gelation index of 70% or more, said preparation comprising: (1) a drug, wherein the amount of said drug is not more than 85% by weight based on the total preparation, (2) an additive which has a solubility such that the volume of water required for dissolving 1 gram of said additive is not more than 5 ml, wherein the amount of said additive is from 5 to 80% by weight based on the total preparation, and (3) a hydrogel-forming polymer having a viscosity of not less than 1000 cps as measured at 1% concentration in water at 25.degree. C., wherein the amount of said hydrogel-forming polymer is from 10 to 95% by weight based on the total preparation and not less than 70 mg per one preparation; (B) substantially complete gelling of the preparation in the upper digestive tract including stomach and small intestine; (C) through travelling in gel-form to the lower digestive tract, releasing the drug not only in the upper digestive tract including stomach and small intestine but also in the lower digestive tract including the colon.

2. The method as claimed in claim 1, wherein said preparation has a gelation index of 80% or more.

3. The method as claimed in claim 1, wherein said additive has a solubility such that the volume of water required for dissolving 1 gram of said additive is not more than 4 ml.

4. The method as claimed in claim 1, wherein the amount of said drug is not more than 80% by weight based on the total preparation.

5. The method as claimed in claim 1, wherein the amount of said additive is from 5 to 60% by weight based on the total preparation.

6. The method as claimed in claim 1, wherein the amount of said hydrogel-forming polymer is from 10 to 90% by weight based on the total preparation.

7. The method as claimed in claim 1, wherein the amount of said drug is not more than 80% by weight based on the total preparation, the amount of said additive is from 5 to 60% by weight based on the total preparation, and the amount of said hydrogel-forming polymer is from 10 to 90% by weight based on the total preparation.

8. The method as claimed in claim 1, wherein the amount of said hydrogel-forming polymer is not less than 100 mg per one preparation.

9. The method as claimed in claim 1, wherein said drug is nicardipine hydrochloride.

10. The method as claimed in claim 1, wherein said drug is tamusulosin hydrochloride.

11. The method as claimed in claim 1, wherein said additive is selected from the group consisting of a highly hydrophilic polymer, a sugar alcohol, a sugar, a surfactant, a salt, an organic acid, an amino acid and an amino sugar.

12. The method as claimed in claim 11, wherein said additive is selected from the group consisting of polyethylene glycol, polyvinylpyrrolidone, D-sorbitol, xylitol, sucrose, anhydrous maltose, D-fructose, dextran, polyoxyethylene-hydrogenated castor oil, polyoxyethylene-polyoxypropylene glycol, polyoxyethylene-sorbitan higher fatty acid ester, sodium chloride, magnesium chloride, citric acid, tartaric acid, glycine, .beta.-alanine, lysine hydrochloride and meglumine.

13. The method as claimed in claim 12, wherein said additive is selected from the group consisting of polyethylene glycol, polyvinylpyrrolidone, and D-sorbitol.

14. The method as claimed in claim 1, wherein said additive is polyethylene glycol.

15. The method as claimed in claim 1, wherein said additive is selected from the group consisting of polyethylene oxide, hydroxypropylmethylcellulose sodium carboxymethylcellulose, hydroxyethylcellulose and carboxyvinyl polymers.

16. The method as claimed in claim 15, wherein said hydrogel-forming polymer is polyethylene oxide.

17. The method as claimed in claim 1, wherein said additive is polyethylene glycol and said hydrogel-forming polymer is polyethylene oxide.

18. The method as claimed in claim 1, wherein drug-release is provided in the upper digestive tract and also in the lower digestive tract including the colon.

19. The method as claimed in claim 1, wherein said preparation is a tablet.

20. The method as claimed in claim 1, wherein said gelation index is defined by the equation

21. The method as claimed in claim 1, wherein said gelation index is defined by the equation

22. A method for providing drug-release not only in the upper digestive tract including stomach and small intestine but also in the lower digestive tract including the colon, comprising the steps of: (A) orally administering a preparation having a gelation index of 70% or more, said preparation comprising: (1) a drug, wherein the amount of said drug is not more than 85% by weight based on the total preparation, (2) an additive which has a solubility such that the volume of water required for dissolving 1 gram of said additive is not more than 5 ml, wherein the amount of said additive is from 5 to 80% by weight based on the total preparation, and (3) a hydrogel-forming polymer having a viscosity of not less than 1000 cps as measured at 1% concentration in water at 25.degree. C., wherein the amount of said hydrogel-forming polymer is from 10 to 95% by weight based on the total preparation and not less than 70 mg per one preparation; and (B) absorbing water before the preparation is in the low-water lower digestive tract including the colon.

23. A method for delivering a gel to the lower digestive tract including the colon for drug-release, comprising the steps of: (A) orally administering a preparation having a gelation index of 70% or more, said preparation comprising: (1) a drug, wherein the amount of said drug is not more than 85% by weight based on the total preparation, (2) an additive which has a solubility such that the volume of water required for dissolving 1 gram of said additive is not more than 5 ml, wherein the amount of said additive is from 5 to 80% by weight based on the total preparation, and (3) a hydrogel-forming polymer having a viscosity of not less than 1000 cps as measured at 1% concentration in water at 25.degree. C., wherein the amount of said hydrogel-forming polymer is from 10 to 95% by weight based on the total preparation and not less than 70 mg per one preparation; (B) substantially complete gelling in the upper digestive tract including stomach and small intestine; and (C) releasing the drug not only in the upper digestive tract including stomach and small intestine but also in the lower digestive tract including the colon.

24. A method for maintaining a steady blood level of a drug, comprising the steps of: (A) orally administering a preparation having a gelation index of 70% or more, said preparation comprising: (1) a drug, wherein the amount of said drug is not more than 85% by weight based on the total preparation, (2) an additive which has a solubility such that the volume of water required for dissolving 1 gram of said additive is not more than 5 ml, wherein the amount of said additive is from 5 to 80% by weight based on the total preparation, and (3) a hydrogel-forming polymer having a viscosity of not less than 1000 cps as measured at 1% concentration in water at 25.degree. C., wherein the amount of said hydrogel-forming polymer is from 10 to 95% by weight based on the total preparation and not less than 70 mg per one preparation; (B) substantially complete gelling in the upper digestive tract including stomach and small intestine; and (C) releasing the drug not only in the upper digestive tract including stomach and small intestine but also in the lower digestive tract including the colon.

25. A method for maintaining a steady blood level of a drug, comprising the steps of: (A) solubilizing a drug to provide a preparation having a gelation index of 70% or more, said solubilizing comprising combining the drug, in an amount not more than 85% by weight based on the total preparation, with (i) an additive which has a solubility such that the volume of water required for dissolving 1 gram of said additive is not more than 5 ml, wherein the amount of said additive is from 5 to 80% by weight based on the total preparation, and (ii) a hydrogel-forming polymer having a viscosity of not less than 1000 cps as measured at 1% concentration in water at 25.degree. C., wherein the amount of said hydrogel-forming polymer is from 10 to 95% by weight based on the total preparation and not less than 70 mg per one preparation; (B) orally administering the solubilized drug preparation of step (A); and (C) substantially complete gelling in the upper digestive tract including stomach and small intestine; followed by drug-release in the lower digestive tract including the colon.

26. The method of claim 1, wherein the method comprises oral administration to a human and the substantially complete gelation is about 4 to 5 hours after administration.

27. The method of claim 26, wherein the method comprises a portion of the preparation having undergone gelation still remaining in the colon 6 hours after administration.

28. The method of claim 27, wherein the method comprises a portion of the preparation having undergone gelation still remaining in the colon 8 hours after administration.

29. The method of claim 27, wherein the method comprises a portion of the preparation having undergone gelation still remaining in the colon 12 hours after administration.

30. A method for providing drug-release not only in the upper digestive tract including stomach and small intestine but also in the lower digestive tract including the colon, comprising the steps of: (A) orally administering a preparation having a gelation index of 70% or more, said preparation comprising: (1) a drug, wherein the amount of said drug is not more than 85% by weight based on the total preparation, (2) an additive which has a solubility such that the volume of water required for dissolving 1 gram of said additive is not more than 5 ml, wherein the amount of said additive is from 5 to 80% by weight based on the total preparation, and (3) a hydrogel-forming polymer, wherein the amount of said hydrogel-forming polymer is from 10 to 95% by weight based on the total preparation; (B) substantially complete gelling of the preparation in the upper digestive tract including stomach and small intestine; (C) through travelling in gel-form to the lower digestive tract, releasing the drug not only in the upper digestive tract including stomach and small intestine but also in the lower digestive tract including the colon.
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