申请人:Norwich Eaton Pharmaceuticals, Inc.
公开号:EP0368409A2
公开(公告)日:1990-05-16
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.
用于经皮给药丁丙诺啡盐的组合物,该组合物包含安全有效量的药学上可接受的丁丙诺啡盐在载体中,载体包括
(a) 选自 C₃-C₄ 二醇、C₃-C₆ 三醇及其混合物组成的组的极性溶剂材料;和
(b) 选自脂肪酸、脂肪醇、脂肪醇酯、脂肪酸酯及其混合物的极性脂质材料;
其中,极性溶剂材料和极性脂质材料的重量比为 60:40 至 99:1。优选地,极性溶剂材料为丙二醇,极性脂质材料为 C₁₂- C₁₈ 脂肪醇、C₁₂-C₁₈ 脂肪酸或 C₈-C₁₂ 脂肪醇或脂肪酸的酯。特别优选的极性脂质材料包括油酸、月桂醇、月桂酸甲酯和辛酸甲酯。极性溶剂材料与极性脂质材料的比例最好为约 90:10 至约 98:2。