口服胰岛素毫微球的特性及降血糖作用

• 作 者: 张强 丁继军 魏树礼
• 机 构: 北京医科大学药剂研究室
• 出 处: 北京医科大学学报
• 发表日期: 1998年03期
• 关键词: 降血糖作用 口服胰岛素 血糖值 糖尿病大鼠 血糖／药物作用 微球 理化性能 相对生物利用度 体外释放度 体外释药

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 study the physicochemical properties of oral insulin nanospheres (INSNP) and its hypoglycemic effect on rats. Methods: The particle size, encapsulation efficiency and in vitro release of INSNP were measured. The diabetic rats or normal rats were used as models to evaluate the hypoglycemic effect of oral administration of INSNP by measuring the concentration of blood glucose. RESULTS: The in vitro release of INSNP was in accordance with the double-exponential kinetics equation. After oral administration of 5u / kg INSNP (Ⅰ, Ⅱ) to diabetic rats, the average blood glucose value decreased by 35% in 1 ~ 12h respectively. 0%, and 35.5% respectively. However, the average blood glucose value decreased by 60.84% ​​after 1 ~ 24h of administration of 10 ng / kg INS  NP (Ⅰ) Ⅰ), there was no obvious drop of blood glucose. After oral administration of INSNP with two formulas, the relative bioavailability reached 27.86% and 28.56% respectively. Conclusion: The proper formula of nanospheres can increase the hypoglycemic effect of insulin on diabetic rats.