EP0149920A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Pharmaceutical formulation
Assignee: Elan Corp PLC
•
Filing: 1984-12-21
•
Granted: —
•
Expires: 2004-12-21
Abstract
Abstract A controlled absorption diltiazem formulation for oral administration comprises a pellet having a core of diltiazem or a pharmaceutically acceptable salt thereof in association with an organic acid and a lubricant, and an outer membrane which permits release of diltiazem in an aqueous medium at a controlled rate which is substantially pH independent. The pellet has a dissolution rate in vitro, which when measured according to the Paddle Method of U.S. Pharmacopoeia XX, is not more than 10% of the total diltiazem after 2 hours of measurement in a buffered medium. Not more than 30% of the total diltiazem is released after a total of 4 hours measurement and not more than 40% of the total diltiazem is released after a total of 6 hours. 100% release is achieved after 12 hours, with a maximum of 80% of the total diltiazem being released after 8 hours.
Inventors
- 👤 Donald Eugene Panoz
- 👤 Edward James Geoghegan
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-04 10:21
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5073; A61K9/5078; A61K31/00; A61K31/33; A61K31/395; A61K31/55; A61K31/554; A61P; A61P3/00; A61P9/00; A61P9/08; A61P9/10
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
172 words
A controlled absorption diltiazem formulation for oral administration, characterised in that it comprises a pellet having a core of diltiazem or a pharmaceutically acceptable salt thereof in association with an organic acid and a lubricant, and an outer membrane which permits release of diltiazem in an aqueous medium, said pellet having a dissolution rate which is substantially pH independent and which when measured according to the Paddle Method of U.S. Pharmacopoeia XX has the following characteristics: a) between 0 and 10% of the total diltiazem is released after a total of 2 hours of measurement; b) between 10 and 30% of the total diltiazem is released after a total of 4 hours of measurement; c) between 20 and 40% of the total diltiazem is released after a total of 6 hours of measurement; d) between 50 and 80% of the total diltiazem is released after a total of 8 hours of measurement; and e) between 85 and 100% of the total diltiazem is released after a total of 12 hours of measurement.
Claim 2
Dependent Claim
172 words
A controlled absorption diltiazem formulation for oral administration, characterised in that it comprises a pellet having a core of diltiazem or a pharmaceutically acceptable salt thereof in association with an organic acid and a lubricant, and an outer membrane which permits release of diltiazem in an aqueous medium, said pellet having a dissolution rate which is substantially pH independent and which when measured according to the Paddle Method of U.S. Pharmacopoeia XX has the following characteristics: a) between 0 and 10% of the total diltiazem is released after a total of 2 hours of measurement; b) between 10 and 30% of the total diltiazem is released after a total of 4 hours of measurement; c) between 20 and 40% of the total diltiazem is released after a total of 6 hours of measurement; d) between 50 and 80% of the total diltiazem is released after a total of 8 hours of measurement; and e) between 85 and 100% of the total diltiazem is released after a total of 12 hours of measurement.
Claim 3
Dependent Claim
48 words
A formulation according to Claim 1, characterised in that the core comprises diltiazem or a pharmaceutically acceptable salt thereof and the associated organic acid and lubricant embedded in a polymeric material in a multi-layer arrangement and in that it is built up in a manner known per se.
Claim 4
Dependent Claim
38 words
A formulation according to Claim 2, characterised in that the polymeric material in which the diltiazem is embedded is rapidly soluble in water, the water soluble polymer preferably being selected from polyvinyl, alcohol, polyvinylpyrrolidone, hydroxypropylmethylcellulose and Eduragit RL.
Claim 5
Dependent Claim
25 words
A formulation according to Claim 2, characterised in that the polymeric material in which the diltiazem is embedded is readily permeable to diltiazem and water.
Claim 6
Dependent Claim
64 words
A formulation according to Claim 2, characterised in that the polymeric material contains a major proportion of a water soluble polymer and a minor proportion of a water insoluble polymer, the ratio of water soluble to water insoluble polymer being determined by the inherent characteristics of the respective polymers, the water insoluble polymer preferably being selected from polyvinylchloride, Shellac, polyurethane, ethylcellulose and Eudragit RS.
Claim 7
Dependent Claim
51 words
A formulation according to any preceding claim, characterised in that the outer membrane has a major proportion of a water insoluble polymer and a minor portion of a water soluble polymer, the ratio of water insoluble to water soluble polymer being determined by the inherent solubility characteristics of the respective polymers.
Claim 8
Dependent Claim
38 words
A formulation according to Claim 6, characterised in that the water insoluble polymer is selected from polyvinylchloride, Shellac, polyurethane, ethylcellulose and Eudragit RS and the water soluble polymer is selected from polyvinyl alcohol, polyvinylpyrrolidone, hydroxypropylmethylcellulose and Eudragit RL.
Claim 9
Dependent Claim
52 words
A formulation according to any one of Claims 1 to 5, characterised in that the outer membrane is composed of a major proportion of a non-porous polymer and a minor proportion of a porous polymer, the ratio of non-porous to porous polymer being determined by the inherent porosity of the respective polymers.
Claim 10
Dependent Claim
13 words
A capsule comprising pellets according to any one of Claims 1 to 8.
Claim 11
Dependent Claim
61 words
A process for the production of a formulation according to any one of Claims 1 to 8, which comprises forming a core of diltiazem or a pharmaceutically acceptable salt thereof in association with an organic acid and a lubricant and enclosing the core in an outer membrane which permits release of the diltiazem in the manner set out in Claim 1.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
Maintenance schedule is calculated for granted US utility patents.