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US 7,022,342 B2Granted
Controlled release oral dosage form of beta-adrenergic blocking agents
AssigneeAndrx Corporation
InventorsChih-Ming Chen, Xiu Xiu Cheng
Life of this patent
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Abstract
A sustained release beta-adrenergic receptor blocking agent, preferably propranolol, formulation.
Claims8
A controlled release pharmaceutical dosage form comprising a plurality of pellets wherein the pellets consists essentially of:
- (a) a core consisting essentially of:
- (i) propranolol or a pharmaceutically acceptable derivative thereof;
- (ii) sugar spheres;
- (iii) microcrystalline cellulose;
- and
- (iv) ethylcellulose;
- and
- (b) a coating applied directly to the core consisting essentially of a mixture of:
- (i) ethylcellulose;
- (ii) hydroxypropyl methylcellulose;
- (iii) acetyl tributyl citrate;
- and
- (iv) talc, wherein the viscosity of the core ethylcellulose is 8–12 cps and the viscosity of the coating ethylcellulose is above 8 cps wherein the dosage form exhibits the following dissolution profile when tested in a USP type 1 apparatus at 100 rpm in 900 ml of simulated intestinal fluid (pH 6.8 phosphate buffer) at 37° C.:
- after 2 hours 15–40% of the propranolol or a pharmaceutically acceptable derivative thereof is released;
- after 4 hours 35–65% of the propranolol or a pharmaceutically acceptable derivative thereof is released;
- after 8 hours 40–80% of the propranolol or a pharmaceutically acceptable derivative thereof is released;
- not less than 70% of the propranolol or a pharmaceutically acceptable derivative thereof is released after 12 hours;
- and
- not less than 80% of the propranolol or a pharmaceutically acceptable derivative thereof is released after 16 hours.
16 more elements
A controlled release pharmaceutical dosage form comprising a plurality of pellets wherein the pellets consists essentially of:
- (a) a core consisting essentially of:
- (i) propranolol or a pharmaceutically acceptable derivative thereof;
- (ii) sugar spheres;
- (iii) miuocrystalline cellulose;
- and
- (iv) ethylcellulose;
- and
- (b) a coating applied directly to the core consisting essentially of a mixture of:
- (i) ethylcellulose;
- (ii) hydroxypropyl methylcellulose;
- (iii) acetyl tributyl citrate;
- and talc, wherein the viscosity of the core ethylcellulose is 8–12 cps and the viscosity of the coating ethylcellulose is above 8 cps wherein the dosage form exhibits the following dissolution profile when tested in a USP type II apparatus at 75 rpm in 900 ml of simulated gastric fluid and at 37° C.:
- after 2 hours 10–40% of the propranolol or a pharmaceutically acceptable derivative thereof is released;
- after 4 hours 30–60% of the propranolol or a pharmaceutically acceptable derivative thereof is released;
- after 8 hours 50–80% of the propranolol or a pharmaceutically acceptable derivative thereof is released;
- not less than 70% of the propranolol or a pharmaceutically acceptable derivative thereof is released after 12 hours;
- and
- not less than 85% of the propranolol or a pharmaceutically acceptable derivative thereof is released after 20 hours.
15 more elements
Dependencies are inferred from the claim text.