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目的 以胰岛素为模型药物 ,评价PEG包裹胰岛素脂质体的降血糖药效学作用。方法 采用逆相蒸发法制备PEG包裹的胰岛素脂质体。正常Wistar大鼠分别静脉注射给予胰岛素溶液、胰岛素脂质体及PEG包裹的胰岛素脂质体。采用葡萄糖还原酶法测定血清中的血糖浓度。以梯形法计算血糖 -时间曲线上面积 (AAC) ,采用胰岛素溶液的AAC为对照 ,分别计算胰岛素脂质体和PEG包裹的胰岛素脂质体的药理相对生物利用度。结果 PEG包裹的胰岛素脂质体的包封率为 18 3 3 % ,平均粒径为 58 4nm。静脉注射给予胰岛素溶液、胰岛素脂质体和PEG包裹的胰岛素脂质体后 ,其血糖降低的最低百分率(Cmin% )分别为 :2 5 2 6± 5 75% ,3 3 92± 12 42 %和 42 3 9± 10 5% ;达到最低百分率的时间 (Tmin)分别为 :0 7± 0 3 ,1 2± 0 4和 2 3± 0 7h。胰岛素脂质体和PEG包裹的胰岛素脂质体的药理相对生物利用度分别为 :98 0 3 %和 99 70 %。结论 PEG包裹的胰岛素脂质体具有相对的缓释作用 ,降血糖作用更为明显
Objective To evaluate the hypoglycemic pharmacodynamic effects of PEG-encapsulated insulin liposomes using insulin as a model drug. Methods PEG encapsulated insulin liposomes were prepared by reverse phase evaporation. Normal Wistar rats were given intravenous insulin solution, insulin liposomes and PEG-coated insulin liposomes. Serum glucose concentration was measured by glucose reductase method. The AAC was calculated by the trapezoidal method and the AAC of the insulin solution was used as a control to calculate the pharmacological relative bioavailability of insulin liposomes and PEG-encapsulated insulin liposomes, respectively. Results The encapsulation efficiency of PEG-encapsulated insulin liposomes was 18 3 3% with an average particle size of 58 4 nm. After intravenous administration of insulin solution, insulin liposomes and PEG-encapsulated insulin liposomes, the lowest percentage of blood glucose (Cmin%) were 2562 ± 5 75%, 3392 ± 12 42% and 42 3 9 ± 10 5%. The time to reach the lowest percentage (Tmin) were 0 7 ± 0 3, 1 2 ± 0 4 and 2 3 ± 0 7 h, respectively. The pharmacological relative bioavailability of insulin liposomes and PEG-coated insulin liposomes were 98 0 3% and 99 70%, respectively. Conclusion The PEG-encapsulated insulin liposomes have relatively sustained release effect, and the hypoglycemic effect is more obvious