EP0368409A2
Expired / Lapsed
EP
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Compositions for the transdermal delivery of buprenorphine salts
Assignee: Warner Chilcott Pharmaceuticals Inc
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Filing: 1989-11-07
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Granted: —
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Expires: 2009-11-07
Abstract
Abstract Compositions for the transdermal delivery of buprenorphine salts comprising a safe and effective amount of a pharmaceutically-acceptable buprenorphine salt in a carrier comprising: (a) a polar solvent material selected from the group consisting of C₃-C₄ diols, C₃-C₆ triols, and mixtures thereof; and (b) a polar lipid material selected from the group consisting of fatty acids, fatty alcohols, fatty alcohol esters, fatty acid esters, and mixtures thereof; wherein said polar solvent material and said polar lipid material are present in a weight ratio of solvent material:lipid material of from about 60:40 to about 99:1. Preferably, the polar solvent material is propylene glycol, and the polar lipid material is a C₁₂- C₁₈ fatty alcohol, a C₁₂-C₁₈ fatty acid, or an ester of a C₈-C₁₂ fatty alcohol or fatty acid. Particularly preferred polar lipid materials include oleic acid, lauryl alcohol, methyl laurate and methyl caprylate. The ratio of polar solvent material to polar lipld material is preferably from about 90:10 to about 98:2.
Inventors
- 👤 Joan Bolduc Szuktak
- 👤 Gary Lee Manring
- 👤 Ronald Lee Smith
- 👤 Eugene George Drust
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-26 21:02
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/70; A61K9/7023; A61K9/703; A61K9/7084; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/47; A61K31/485; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/12; A61K47/14; A61K9/0012; A61K9/0014; A61P; A61P25/00; A61P25/04
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
91 words
A composition for the transdermal delivery of buprenorphine, comprising a safe and effective amount of a pharmaceutically-acceptable buprenorphine salt in a carrier comprising: (a) a polar solvent material selected from the group consisting of C₃-C₄ diols, C₃-C₆ triols, and mixtures thereof; and (b) a polar lipid material selected from the group consisting of fatty acids, fatty alcohols, fatty alcohol esters, fatty acid esters, and mixtures thereof; wherein said polar solvent material and said polar lipid material are present in a weight ratio of solvent material:lipid material of from 60:40 to 99:1.
Claim 2
Dependent Claim
91 words
A composition for the transdermal delivery of buprenorphine, comprising a safe and effective amount of a pharmaceutically-acceptable buprenorphine salt in a carrier comprising: (a) a polar solvent material selected from the group consisting of C₃-C₄ diols, C₃-C₆ triols, and mixtures thereof; and (b) a polar lipid material selected from the group consisting of fatty acids, fatty alcohols, fatty alcohol esters, fatty acid esters, and mixtures thereof; wherein said polar solvent material and said polar lipid material are present in a weight ratio of solvent material:lipid material of from 60:40 to 99:1.
Claim 3
Dependent Claim
84 words
A composition for the transdermal delivery of buprenorphine, according to Claim 1, wherein said polar lipid material is selected from the group consisting of: C₁₂-C₁₈ fatty acids, C₁₂-C₁₈ fatty alcohols, monoesters of a C₈-C₁₂ fatty alcohol, monoesters of a C₈-C₁₂ fatty acid, diesters of C₂-C₈ dicarboxylic acids with C₁-C₆ alcohols, diesters of C₂-C₈ dihydroxy alcohols with C₂-C₆ acids, and mixtures thereof; preferably methyl caprylate, propyl caprylate, octyl acetate, methyl caproate, propyl caproate, methyl laurate, C₁₂-C₁₅ alcohols lactate, diisopropyl adipate, diisobutyl adipate, and mixtures thereof.
Claim 4
Dependent Claim
38 words
A composition for the transdermal delivery of buprenorphine, according to Claim 2, wherein said polar solvent material is selected from the group consisting of: 1,2-butane diol, 1,2-propane diol, glycerol and 1,2,6-hexane triol, and mixtures thereof; preferably 1,2-propane diol.
Claim 5
Dependent Claim
30 words
A composition for the transdermal delivery of buprenorphine, according to Claim 3, wherein said polar lipid material is methyl laurate, and the weight ratio of solvent material:lipid material is 97:3.
Claim 6
Dependent Claim
33 words
A composition for the transdermal delivery of buprenorphine, according to Claim 3, wherein said polar lipid material is methyl caprylate, and the weight ratio of solvent material:lipid material is from 90:10 to 95:5.
Claim 7
Dependent Claim
39 words
A composition for the transdermal delivery of buprenorphine, according to Claim 3, wherein said polar lipid material is selected from the group consisting of lauryl alcohol, myristyl alcohol, oleyl alcohol, lauric acid, oleic acid, linoleic acid and mixtures thereof.
Claim 8
Dependent Claim
30 words
A composition for the transdermal delivery of buprenorphine, according to Claim 1, wherein said buprenorphine salt comprises buprenorphine and a pharmaceutically-acceptable acid, preferably citric acid, lactic acid, and mixtures thereof.
Claim 9
Dependent Claim
31 words
A composition for the transdermal delivery of buprenorphine, according to Claim 2, additionally comprising a solvent material which enhances the solubility of said polar lipid material in said polar solvent material.
Claim 10
Dependent Claim
16 words
A composition for the transdermal delivery of buprenorphine, according to Claim 2, additionally comprising a thickener.
Claim 11
Dependent Claim
144 words
A composition in unit dosage form, for the transdermal delivery of buprenorphine, comprising: (a) from 1.0 mg to 40 mg, preferably from 3.0 mg to 10 mg, of buprenorphine as a pharmaceutically-acceptable buprenorphine salt; and (b) a carrier comprising (i) propylene glycol, and (ii) a polar lipid material selected from the group consisting of oleic acid, lauryl alcohol, myristyl alcohol, oleyl alcohol, methyl caprylate, propyl caprylate, octyl acetate, methyl caproate, propyl caproate, methyl laurate, C₁₂-C₁₅ alcohols lactate, diisopropyl adipate, diisobutyl adipate, and mixtures thereof; preferably methyl laurate, methyl caprylate, or lauryl alcohol; wherein said polar solvent material and said polar lipid material are present at a combined level of from 70% to 99.5%, preferably from 80% to 99.5%; and wherein said polar solvent material and said polar lipid material are present in a weight ratio of solvent material:lipid material of from 60:40 to 99:1.
Claim 12
Dependent Claim
144 words
A composition in unit dosage form, for the transdermal delivery of buprenorphine, comprising: (a) from 1.0 mg to 40 mg, preferably from 3.0 mg to 10 mg, of buprenorphine as a pharmaceutically-acceptable buprenorphine salt; and (b) a carrier comprising (i) propylene glycol, and (ii) a polar lipid material selected from the group consisting of oleic acid, lauryl alcohol, myristyl alcohol, oleyl alcohol, methyl caprylate, propyl caprylate, octyl acetate, methyl caproate, propyl caproate, methyl laurate, C₁₂-C₁₅ alcohols lactate, diisopropyl adipate, diisobutyl adipate, and mixtures thereof; preferably methyl laurate, methyl caprylate, or lauryl alcohol; wherein said polar solvent material and said polar lipid material are present at a combined level of from 70% to 99.5%, preferably from 80% to 99.5%; and wherein said polar solvent material and said polar lipid material are present in a weight ratio of solvent material:lipid material of from 60:40 to 99:1.
References Cited (Backward Citations)
No citation records indexed.
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