Multi-stage oral drug controlled-release system
First Claim
1. A controlled-release oral preparation characterized in that release of granules from matrix and drug release from the granules are conducted in stepwise way, wherein the preparation comprises:
- (a) granules comprising a drug and a carrier material in size of 0.1˜
1 mm, said carrier material is hydrophobic material in case of drug with water-solubility of 1 mg/ml or more and said carrier material is hydrophilic material in case of drug with water-solubility of less than 1 mg/ml;
(b) a matrix in which the granules are embedded, comprising swelling and erodible polymer and swelling-regulating material; and
(c) a release-modifying layer comprising hydrophobic release-modifying polymer, hydrophilic release-modifying polymer, pH-dependent release-modifying polymer or a mixture thereof.
1 Assignment
0 Petitions
Accused Products
Abstract
A multi-stage oral drug controlled-release system is disclosed, as well as a preparation for maintaining the drug blood concentration at a desired level for a prolonged time. The system operates by releasing the drug at a constant rate through stepwise control of drug release following administration of the preparation. More specifically, the multi-stage oral drug controlled-release system involves the stepwise release of drug-containing granules from an inner matrix, which is surrounded by a coating or release-modifying layer. The granules contain an active drug and a carrier material in size of 0.1˜1 mm. The carrier material is hydrophobic when the drug has a water-solubility of 1 mg/ml or more, and is hydrophilic when the drug has a water-solubility of less than 1 mg/ml. The inner matrix, in which the drug-containing granules are embedded, is formed from swelling and erodible polymer(s) and swelling-regulating material(s). The release-modifying layer is composed of a hydrophobic release-modifying polymer, a hydrophilic release-modifying polymer, pH-dependent release-modifying polymer or mixtures thereof.
149 Citations
15 Claims
-
1. A controlled-release oral preparation characterized in that release of granules from matrix and drug release from the granules are conducted in stepwise way, wherein the preparation comprises:
-
(a) granules comprising a drug and a carrier material in size of 0.1˜
1 mm, said carrier material is hydrophobic material in case of drug with water-solubility of 1 mg/ml or more and said carrier material is hydrophilic material in case of drug with water-solubility of less than 1 mg/ml;
(b) a matrix in which the granules are embedded, comprising swelling and erodible polymer and swelling-regulating material; and
(c) a release-modifying layer comprising hydrophobic release-modifying polymer, hydrophilic release-modifying polymer, pH-dependent release-modifying polymer or a mixture thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15)
-
Specification