摘要
目的：研究口服胰岛素毫微球（ＩＮＳＮＰ）的理化性能及对大鼠的降血糖作用。方法：测定ＩＮＳＮＰ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ＩＮＳＮＰ的降血糖效果。结果：ＩＮＳＮＰ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ＩＮＳＮＰ（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ＩＮＳＮＰ（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ＩＮＳＮＰ（Ⅰ）后，血糖下降不明显；口服给与两个配方的ＩＮＳＮＰ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 insulinloaded nanoparticles (INSNP) upon rats after oral administration. Methods: The mean diameter, associating ratio and invitro release kinetics of INSNP were investigated. The hypoglycemic effect of the two formulations of INSNP (Ⅰ,Ⅱ) was evaluated on the normal and diabetic rats by measuring the blood glucose levels. Results: The release profiles of INSNP were be well modelled using a biexponential function. The hypoglycemic effect was not significant after oral administration of 10 u/kg INSNP 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 INSNP (Ⅰ,Ⅱ) was orally administered to the diabetic rats, while it decresed 60.8% when 10 u/kg of INSNP (Ⅰ) was administered. In comparison with subcutaneous injection of the insulin solution, the pharmacological bioavailability calculated by the timeblood glucose decreased (%) profiles was 27.9% and 28.6%, respectively, for the INSNP Ⅰ and INSNP Ⅱ after oral administration. Conclusion: The hypoglycemic effect of insulin upon diabetic rats could be improved through the proper formulation of nanoparticles.
出处
《北京医科大学学报》
CSCD
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
关键词
胰岛素
剂量
微球
降血糖作用
Insulin/admin Microspheres Blood glucose/drug eff
