大多数多肽药物(包括胰岛素)口服后,人体的生物利用度极低。作者开发了一种新型油包水的口服胰岛素微乳剂,水相中含胰岛素,用蛋白酶抑制剂——抑肽酶保护起来。油相中含胆固醇、卵磷脂和非酯化脂肪酸,其比例为1:2:14。微乳剂喷洒到隋性载体——羟甲基纤维素钙上,然后装入硬的明胶胶囊中。口服后该制剂通过吸附在乳糜微 The body’s bioavailability is extremely low when most peptide drugs, including insulin, are taken orally. The authors developed a novel water-in-oil oral insulin microemulsion that contains insulin in the aqueous phase and is protected by a protease inhibitor, aprotinin. Oil phase contains cholesterol, lecithin and non-esterified fatty acids in a ratio of 1: 2: 14. The microemulsion is sprayed onto the inert carrier, hydroxymethylcellulose calcium, and then filled into hard gelatin capsules. After oral administration the formulation is absorbed on the chylomicrons