Hydrogel-forming sustained-release preparation
AssigneeYamanouchi Pharmaceutical Co., Ltd.
InventorsKazuhiro Sako, Hiroshi Nakashima, Toyohiro Sawada, Akira Okada, Muneo Fukui
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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.
Claims30
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° 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.
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° 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.
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° 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.
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° 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.
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° 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.
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.
Dependencies are inferred from the claim text.