公开(公告)号：US20030086948A1

公开(公告)日：2003-05-08

申请号：US09935277

申请日：2001-08-22

申请人： GATTEFOSSE S.A.

发明人： Hassan Benameur ,  Vincent Jannin ,  Delphine Roulot

IPC分类号： A61K031/366 ,  A61K031/225 ,  A61K009/20

CPC分类号： A61K9/4858 ,  A61K9/1075 ,  A61K31/366

摘要： A pharmaceutical composition for oral use is disclosed. It includes, as active principle, a drug liable to undergo a strong first intestinal passage effect and a carrier which is self-micro-emulsifying on contact with an aqueous phase. The carrier includes: a therapeutically effective amount of the active principle; a lipophilic phase, which is a mixture of glycerol mono-, di- and triesters and of PEG mono- and diesters with at least one fatty acid chosen from the group comprising C8-C18 fatty acids; a surfactant phase which is a mixture of glycerol mono-, di- and triesters and of PEG mono- and diesters with caprylic acid (C8) and capric acid (C10); a co-surfactant phase which is an ester of a polyvalent alcohol with at least one fatty acid chosen from the group comprising caprylic esters of propylene glycol, lauric esters of propylene glycol and oleic esters of polyglycerol. A method of decreasing the effect of intestinal metabolism on a drug using the composition is also disclosed.

摘要翻译： 公开了口服用药物组合物。 作为活性成分，作为活性成分，含有易于经受强烈的第一次肠通过作用的药物和与水相接触时自乳化的载体。 载体包括：治疗有效量的活性成分; 亲脂相，其是甘油单酯，二酯和三酯的混合物，以及PEG单酯和二酯与至少一种选自C8-C18脂肪酸的脂肪酸的混合物; 甘油单酯，二酯和三酯和PEG单酯和二酯与辛酸（C8）和癸酸（C10）的混合物的表面活性剂相; 辅助表面活性剂相，其是多元醇与至少一种脂肪酸的酯，所述脂肪酸选自丙二醇的辛酸酯，丙二醇的月桂酸酯和聚甘油的油酸酯。 还公开了使用该组合物降低肠代谢对药物的作用的方法。