Patent EP0271193A2 successfully refreshed from Google Patents.
EP0271193A2
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Controlled release hydromorphone composition
Assignee: Euro Celtique SA
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Filing: 1987-10-22
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Granted: —
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Expires: 2007-10-22
Abstract
Abstract A solid controlled release, oral dosage form, the dosage form comprising a therapeutically effective amount of hydromorphone or a salt thereof in a matrix wherein the dissolution rate in vitro of the dosage form when measured by the USP Paddle Method at 100rpm in 900ml aqueous buffer (pH between 1.6 and 7.2) at 37°C is between 12.5% and 42.5% (by weight) hydromorphone released after 1 hour, between 25% and 55% (by weight) hydromorphone released after 2 hours, between 45% and 75% (by weight) hydromorphone released after 4 hours and between 55% and 85% (by weight) hydromorphone released after 6 hours, the in vitro release rate being independent of pH between pH 1.6 and 7.2 and chosen such that the peak plasma level of hydromorphone obtained in vivo occurs between 2 and 4 hours after administration of the dosage form.
Inventors
- 👤 Robert Stronech Goldie
- 👤 Sandra Therese Antoinette Malkowska
- 👤 Stewart Thomas Leslie
- 👤 Ronald Brown Miller
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-03 13:26
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2004; A61K9/2013; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/47; A61K31/485; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1652; A61K9/2022; A61K9/205; A61K9/2054; A61K9/48; A61K9/50; A61K9/5005; A61K9/5021; A61K9/5036; A61K9/5042; A61K9/5047
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
144 words
A process for the preparation of a solid, controlled release, oral dosage form characterised by incorporating a therapeutically effective amount of hydromorphone or a salt thereof in a matrix wherein the dissolution rate in vitro of the dosage form when measured by the USP Paddle Method at 100rpm in 900ml aqueous buffer (pH between 1.6 and 7.2) at 37°C is between 12.5% and 42.5% (by weight) hydromorphone released after 1 hour, between 25% and 55% (by weight) hydromorphone released after 2 hours, between 45% and 75% (by weight) hydromorphone released after 4 hours and between 55% and 85% (by weight) hydromorphone released after 6 hours, the in vitro release rate being independent of pH between pH 1.6 and 7.2 and chosen such that the peak plasma level of hydromorphone obtained in vivo occurs between 2 and 4 hours after administration of the dosage form.
Claim 2
Dependent Claim
144 words
A process for the preparation of a solid, controlled release, oral dosage form characterised by incorporating a therapeutically effective amount of hydromorphone or a salt thereof in a matrix wherein the dissolution rate in vitro of the dosage form when measured by the USP Paddle Method at 100rpm in 900ml aqueous buffer (pH between 1.6 and 7.2) at 37°C is between 12.5% and 42.5% (by weight) hydromorphone released after 1 hour, between 25% and 55% (by weight) hydromorphone released after 2 hours, between 45% and 75% (by weight) hydromorphone released after 4 hours and between 55% and 85% (by weight) hydromorphone released after 6 hours, the in vitro release rate being independent of pH between pH 1.6 and 7.2 and chosen such that the peak plasma level of hydromorphone obtained in vivo occurs between 2 and 4 hours after administration of the dosage form.
Claim 3
Dependent Claim
106 words
A process according to claim 1 characterised in that the in vitro dissolution rate is between 17.5% and 37.5% (by weight) hydromorphone released after 1 hour, between 30% and 50% (by weight) hydromorphone released after 2 hours, between 50% and 70% (by weight) hydromorphone released after 4 hours and between 60% and 80%, (by weight) hydromorphone released after 6 hours, preferably between 22.5% and 32.5% (by weight) hydromorphone released after 1 hour, between 35% and 45% (by weight) hydromorphone released after 2 hours, between 55% and 65% (by weight) hydromorphone released after 4 hours and between 65% and 75% (by weight) hydromorphone released after 6 hours.
Claim 4
Dependent Claim
55 words
A process according to either claim 1 or claim 2 characterised in that the matrix comprises a controlled release matrix comprising at least one water soluble hydroxyalkyl, preferably C₁ to C₆ alkyl, cellulose, at least one C₁₂ to C₃₆, preferably C₁₄ to C₂₂, aliphatic alcohol and, optionally at least one polyalkylene glycol, preferably polyethylene glycol.
Claim 5
Dependent Claim
27 words
A process according to any one of claims 1 to 3 characterised in that the at least one hydroxyalkyl cellulose comprises hydroxypropyl cellulose, hydroxypropylmethylcellulose or, preferably hydroxyethylcellulose.
Claim 6
Dependent Claim
36 words
A process according to either claim 3 or claim 4 characterised in that the dosage form contains between 5% and 25% (by weight), especially between 6.25% and 15% (by weight), of the at least one hydroxyalkylcellulose.
Claim 7
Dependent Claim
31 words
A process according to any one of claims 3 to 5 characterised in that the aliphatic alcohol comprises lauryl alcohol, myristyl alcohol, stearyl alcohol or preferably, cetyl alcohol or cetostearyl alcohol.
Claim 8
Dependent Claim
51 words
A process according to any one of claims 3 to 6 characterised in that the dosage form contains between 20% and 50%, preferably between 25% and 45% (by weight) of the at least one fatty alcohol or of the at least one fatty alcohol and the at least one polyalkylene glycol.
Claim 9
Dependent Claim
49 words
A process according to claim 1 characterised by (a) wet granualting at least one water soluble hydroxyalkyl cellulose with hydromorphone or a salt thereof to form granules, (b) mixing the hydroxyalkyl cellulose containing granules with at least one C₁₂-C₃₆ aliphatic alcohol, and (c) optionally, compressing and shaping the granules
Claim 10
Dependent Claim
66 words
A process according to claim 8 characterised in that the at least one water soluble hydroxyalkyl cellulose and the hydromorphone or the salt thereof are wet granulated with water, the weight ratio of the water to the dry weight of the at least one water soluble hydroxyalkyl cellulose being between 1.5 to 1 and 5 to 1, especially between 1.75 and 1 and 3.5 to 1.
Claim 11
Dependent Claim
49 words
A process according to claim 1 characterised by blending a mixture comprising hydromorphone or a salt thereof and a non-water soluble spheronising agent, especially microcrystalline cellulose, extruding the blended mixture to give an extrudate, spheronising the extrudate until spheroids are formed and coating the spheroids with a film coat.
References Cited (Backward Citations)
No citation records indexed.
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