【摘要】 目的制备胰岛素壳聚糖巯基醋酸微球,并对该剂型的降血糖作用进行验证。方法选用巯基含量983μmol.g-1的壳聚糖巯基醋酸偶合物为载体,利用油相干燥法,将胰岛素包封制备成微球;通过体外释药试验和高血糖大白鼠的降血糖试验,对胰岛素壳聚糖巯基醋酸微球的降血糖作用进行评价。结果所制备胰岛素壳聚糖巯基醋酸微球的平均粒径为13μm,粒径在5~20μm的微球占95%以上;高血糖大白鼠十二指肠内和回肠内给予该微球,4h内均能明显降低大白鼠的血糖水平,回肠内给药的效果更为明显,其相对于皮下注射给药的生物利用度为29.9%。结论胰岛素壳聚糖巯基醋酸微球能提高胰岛素的口服生物利用度,回肠给药具有良好的生物有效性。更多还原

【Abstract】 Objective To prepare insulin-containing chitosan-thioglycollic acid conjugates microspheres and evaluate their hypoglycemic effect.Methods The insulin-containing chitosan-thioglycollic acid conjugates microspheres were prepared by the dry-in-oil method using the chitosan-thioglycollic acid conjugates which the content of thiol group was 983μmol·g-1.The hypoglycemic effect of the microsphere was evaluated by drug release test in vitro and hypoglycemic test on hyperglycemic rats.Results The insulin-containing chitosan-thioglycollic acid conjugates microspheres with an average diameter of 13μm were administered by intraduodenal and intraileal application,and gave visible decrease in plasma glucose level in 4h at a dose of 20IU·kg-1.The relative bioavailability of the latter compared to hypodermic injection was 29.9%.Couclusion The results showed that the bioavailability of oral insulin could be facilitated by insulin-containing chitosan-thioglycollic acid conjugates microspheres,and good biological availability was obtained when the microspheres were administered by intraileal application.更多还原