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目的研究壳聚糖和CEC双层包覆胰岛素脂质体的吸收状况,并验证其有效性。方法采用逆相蒸发制备胰岛素脂质体;用酶-苯酚法测定血糖值;用放射免疫法测定血清胰岛素含量,并采用Pkanalyst程序进行拟合。结果 Ch-CEC双层包覆的胰岛素脂质体对负载葡萄糖的正常大鼠的血糖升高具有抑制作用;以皮下注射胰岛素(Ins)为对照,Ch-CEC双层包覆的胰岛素脂质体经糖尿病模型大鼠和beagle犬给药后的相对药理生物利用度均大于9%,具有较好的降血糖作用。另外,在beagle犬降血糖实验中,根据血清胰岛素浓度-时间曲线的曲线下面积(AUC)计算Ch-CEC双层包覆的胰岛素脂质体灌胃给药的相对生物利度为12.67%。结论壳聚糖-CEC双层包覆胰岛素脂质体有利于改善胰岛素口服生物利用度。
Objective To study the absorption status of double-coated insulin liposomes of chitosan and CEC and verify its effectiveness. Methods The liposomes were prepared by reverse phase evaporation. The blood glucose level was measured by enzyme-phenol method. The serum insulin level was determined by radioimmunoassay and was fitted by Pkanalyst program. Results Ch-CEC double-coated insulin liposomes could inhibit the increase of blood glucose in normal glucose-loaded rats. Insulin liposomes were subcutaneously injected with insulin (Ins) The relative pharmacological bioavailability of diabetic model rats and beagle dogs after administration is more than 9%, which has a good hypoglycemic effect. In addition, in the beagle dog hypoglycemic experiment, the relative bioavailability of Ch-CEC double-coated insulin liposome administered by gavage was 12.67% based on the area under the curve of serum insulin concentration-time curve (AUC). Conclusion Chitosan-CEC double-coated insulin liposomes is beneficial to improve oral bioavailability of insulin.