公开(公告)号：US4525339A

公开(公告)日：1985-06-25

申请号：US434452

申请日：1982-10-15

申请人： Charanjit Behl ,  George Beskid ,  Navnit Shah ,  Jacques Tossounian ,  Joel Unowsky

发明人： Charanjit Behl ,  George Beskid ,  Navnit Shah ,  Jacques Tossounian ,  Joel Unowsky

IPC分类号： C07D477/00 ,  A61K9/36 ,  A61K9/48 ,  A61K9/62 ,  A61K31/397 ,  A61K31/40 ,  A61K31/43 ,  A61K31/535 ,  A61K31/545 ,  A61K47/14 ,  A61K47/26 ,  C07D499/46 ,  C07D499/64 ,  C07D499/68 ,  C07D499/893 ,  C07D499/897

CPC分类号： A61K47/14 ,  A61K31/40 ,  A61K31/43 ,  A61K31/545 ,  A61K9/4891

摘要： There is presented a method, in the form of a dosage formulation, for transforming substantially orally inactive .beta.-lactam antibiotics or their pharmaceutically acceptable salts or the esters, ethers, or hydrates of said antibiotics or their salts into orally active compounds by combination of the chosen .beta.-lactam antibiotic with an enhancer comprising an aliphatic, preferably a C.sub.2 to C.sub.18, straight- or branched-chain, saturated or unsaturated, fatty acid or an aliphatic, preferably a C.sub.2 to C.sub.12, straight- or branched-chain, saturated or unsaturated, fatty acid mono-, di- or triglyceride or mixtures thereof, partial or total esters of propylene glycol, polyethylene glycol and carbohydrates of C.sub.2 to C.sub.12 fatty acids, as well as the pharmaceutically acceptable esters and ethers of said glycerides. The antibiotic and enhancer mixture may be administered orally as a solid dosage form with the .beta.-lactam antibiotic above or, optionally, with the enhancer protected by an enteric coating.

摘要翻译： 呈现剂型制剂形式的方法，用于将基本上口服无活性的β-内酰胺抗生素或其药学上可接受的盐或所述抗生素或其盐的酯，醚或水合物转化为口服活性化合物，通过 选择的具有增强剂的β-内酰胺抗生素，其包含脂族，优选C2至C18直链或支链饱和或不饱和脂肪酸或脂族，优选C2至C12直链或支链饱和或 不饱和脂肪酸单 - ，二 - 或甘油三酸酯或其混合物，丙二醇，聚乙二醇和C2至C12脂肪酸的碳水化合物的部分或全部酯，以及所述甘油酯的药学上可接受的酯和醚。 抗生素和增强剂混合物可以作为固体剂型口服施用，其中β-内酰胺抗生素在上面，或任选地与由肠溶衣保护的增强剂一起使用。