口服胰岛素毫微球的特性及降血糖作用  

PROPERTIES AND HYPOGLYCEMIC EFFECT OFTHE INSULINLOADED NANOPARTICLES FOR ORAL ADMINISTRATION

作　　者：张强[1] 丁继军[1] 魏树礼[1] 

机构地区：[1]北京医科大学药剂研究室

出　　处：《北京医科大学学报》1998年第3期239-241,共3页Journal of Peking University(Health Sciences)

基　　金：国家"九五"重点科技攻关项目

摘　　要：目的：研究口服胰岛素毫微球（ＩＮＳＮＰ）的理化性能及对大鼠的降血糖作用。方法：测定ＩＮＳＮＰ的粒径、包封率和体外释放度，以糖尿病大鼠或正常大鼠为模型，通过测定血糖的浓度评价口服ＩＮＳＮＰ的降血糖效果。结果：ＩＮＳＮＰ的体外释药符合双指数动力学方程；给糖尿病大鼠口服５ｕ／ｋｇ的两种配方的ＩＮＳＮＰ（Ⅰ，Ⅱ）后，１～１２ｈ平均血糖值分别下降了３５．０％和３５．５％；而给与１０ｕ／ｋｇ的ＩＮＳＮＰ（Ⅰ）后，１～２４ｈ平均血糖值下降了６０．８４％；正常大鼠口服给与１０ｕ／ｋｇ的ＩＮＳＮＰ（Ⅰ）后，血糖下降不明显；口服给与两个配方的ＩＮＳＮＰ后，相对生物利用度分别达到２７．８６％和２８．５６％。结论：适当配方的毫微球能增加胰岛素对糖尿病大鼠的降血糖作用。Objective: To investigate the physicochemical properties and hypoglycemic effect of insulinloaded nanoparticles (INSNP) upon rats after oral administration. Methods: The mean diameter, associating ratio and invitro release kinetics of INSNP were investigated. The hypoglycemic effect of the two formulations of INSNP (Ⅰ,Ⅱ) was evaluated on the normal and diabetic rats by measuring the blood glucose levels. Results: The release profiles of INSNP were be well modelled using a biexponential function. The hypoglycemic effect was not significant after oral administration of 10 u/kg INSNP to the normal rats. The average blood glucose levels within 1～12 h dropped 35.0% and 35.5%, respectively, after 5 u/kg of INSNP (Ⅰ,Ⅱ) 　was orally administered to the diabetic rats, while it decresed 60.8% when 10 u/kg of INSNP (Ⅰ) was administered. In comparison with subcutaneous injection of the insulin solution, the pharmacological bioavailability calculated by the timeblood glucose decreased (%) profiles was 27.9% and 28.6%, respectively, for the INSNP Ⅰ and INSNP Ⅱ after oral administration. Conclusion: The hypoglycemic effect of insulin upon diabetic rats could be improved through the proper formulation of nanoparticles.

关 键 词：胰岛素 剂量 微球 降血糖作用 

分 类 号：R977.15[医药卫生—药品]