公开(公告)号：EP0368406B1

公开(公告)日：1993-07-28

申请号：EP89202795.4

申请日：1989-11-07

申请人： Norwich Eaton Pharmaceuticals, Inc.

发明人： Drust, Eugene George ,  Smith, Ronald Lee ,  Kasting, Gerald Bruce ,  Szkutak, Joan Bolduc

IPC分类号： A61K31/485 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14

CPC分类号： A61K9/7084 ,  A61K9/0014 ,  A61K31/485 ,  A61K47/10 ,  A61K47/14 ,  Y10S514/947

公开(公告)号：EP0368409A2

公开(公告)日：1990-05-16

申请号：EP89202799.6

申请日：1989-11-07

申请人： Norwich Eaton Pharmaceuticals, Inc.

发明人： Szuktak, Joan Bolduc ,  Manring, Gary Lee ,  Smith, Ronald Lee ,  Drust, Eugene George

IPC分类号： A61K31/485 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14

CPC分类号： A61K9/7084 ,  A61K9/0014 ,  A61K31/485 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14

摘要： 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.

摘要翻译： 用于透皮递送丁丙诺啡盐的组合物，其包含在载体中包含安全有效量的药学上可接受的丁丙诺啡盐，其包含：（a）极性溶剂材料，其选自C 3 -C 4二醇，C 3 -C 6三醇和 其混合物; 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; 其中所述极性溶剂材料和所述极性脂质材料以约60:40至约99:1的溶剂材料：脂质材料的重量比存在。 优选地，极性溶剂材料是丙二醇，极性脂质材料是C 12 -C 18脂肪醇，C 12 -C 18脂肪酸或C 8 -C 12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胶体材料的比率优选为约90:10至约98:2。

公开(公告)号：EP0368409A3

公开(公告)日：1990-12-19

申请号：EP89202799.6

申请日：1989-11-07

申请人： Norwich Eaton Pharmaceuticals, Inc.

发明人： Szuktak, Joan Bolduc ,  Manring, Gary Lee ,  Smith, Ronald Lee ,  Drust, Eugene George

IPC分类号： A61K31/485 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14

CPC分类号： A61K9/7084 ,  A61K9/0014 ,  A61K31/485 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14

摘要： 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.

公开(公告)号：EP0368406A3

公开(公告)日：1990-12-19

申请号：EP89202795.4

申请日：1989-11-07

申请人： Norwich Eaton Pharmaceuticals, Inc.

发明人： Drust, Eugene George ,  Smith, Ronald Lee ,  Kasting, Gerald Bruce ,  Szkutak, Joan Bolduc

IPC分类号： A61K31/485 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14

CPC分类号： A61K9/7084 ,  A61K9/0014 ,  A61K31/485 ,  A61K47/10 ,  A61K47/14 ,  Y10S514/947

摘要： Compositions for the transdermal delivery of buprenorphine comprising a safe and effective amount of buprenorphine 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 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 an ester of a C₈-C₁₂ fatty alcohol or fatty acid. Particularly preferred polar lipid materials include methyl laurate and methyl caprylate. The ratio of polar solvent material to polar lipid material is preferably from about 90:10 to about 98:2.

公开(公告)号：EP0368406A2

公开(公告)日：1990-05-16

申请号：EP89202795.4

申请日：1989-11-07

申请人： Norwich Eaton Pharmaceuticals, Inc.

发明人： Drust, Eugene George ,  Smith, Ronald Lee ,  Kasting, Gerald Bruce ,  Szkutak, Joan Bolduc

IPC分类号： A61K31/485 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14

CPC分类号： A61K9/7084 ,  A61K9/0014 ,  A61K31/485 ,  A61K47/10 ,  A61K47/14 ,  Y10S514/947

摘要： Compositions for the transdermal delivery of buprenorphine comprising a safe and effective amount of buprenorphine 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 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 an ester of a C₈-C₁₂ fatty alcohol or fatty acid. Particularly preferred polar lipid materials include methyl laurate and methyl caprylate. The ratio of polar solvent material to polar lipid material is preferably from about 90:10 to about 98:2.

摘要翻译： 用于透皮递送丁丙诺啡的组合物，其在载体中包含安全有效量的丁丙诺啡，其包含：（a）选自C 3 -C 4二醇，C 3 -C 6三醇及其混合物的极性溶剂材料; 和（b）选自脂肪醇酯，脂肪酸酯及其混合物的极性脂质材料; 其中所述极性溶剂材料和所述极性脂质材料以约60:40至约99:1的溶剂材料：脂质材料的重量比存在。 优选地，极性溶剂材料是丙二醇，极性脂质材料是C8-C12脂肪醇或脂肪酸的酯。 特别优选的极性脂质材料包括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率优选为约90:10至约98:2。