壳聚糖及其衍生物包覆脂质体对胰岛素肠道吸收的影响  

Effects of the liposomes coated by chitosan and its derivatives on the gastrointestinal transit of insulin

作　　者：吴正红[1] 平其能[1] 雷晓敏[1] 李建英[1] 蔡鹏[1] 

机构地区：[1]中国药科大学药剂教研室,江苏南京210009

出　　处：《药学学报》2005年第7期618-622,共5页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金(39930200).

摘　　要：目的考察壳聚糖及其衍生物包覆脂质体对胰岛素肠道吸收的影响。方法采用逆相蒸发制备胰岛素脂质体;采用在体肠灌流法研究壳聚糖及其衍生物包覆胰岛素脂质体的肠道吸收;用酶-苯酚法测定血糖值;用放射免疫法测定血清和肠组织中胰岛素含量。结果壳聚糖(CH)、壳聚糖-EDTA 轭合物(CEC)包覆胰岛素脂质体和CH-CEC 双层包覆胰岛素脂质体的最佳吸收部位均集中在十二指肠,胰岛素溶液的最佳吸收部位在结肠,而未包覆胰岛素脂质体和 N-三甲基壳聚糖盐酸盐(TMC)包覆胰岛素脂质体的最佳吸收部位尚不能确定。在各肠段中,以CH-CEC 双层包覆胰岛素脂质体的吸收最佳。结论壳聚糖及其衍生物包覆脂质体能促进胰岛素经肠道吸收,并可提高其在肠道中的稳定性。Aim To study the effect of the liposomes coated by chitosan and its derivatives as oral dosage form for peptide drugs on the gastrointestinal(GI)transit of drugs.Methods Insulin-liposomes were prepared by reversed-phase evaporation.The in situ perfusion experiment was used to investigate the enteral absorption of insulin.The hypoglycemic effects of insulin were investigated using the glucose oxidase method after administration in rats.The insulin concentrations of serum and enteral tissues were determined by radio-immunoassay in rats.Results In in situ local intestinal perfusion experiment,the duodenum was the best segment for the absorption of the insulin liposomes coated by chitosan(CH)or chitosan-EDTA conjugates(CEC),and double-coated by CH-CEC;the colon was the best segment for the absorption of the insulin solution from rat intestine;but the best segment for the absorption of the uncoated and N-trimethyl chitosan chloride(TMC)coated insulin liposomes was unclear.In all segments,the enteral absorption of the insulin liposomes double-coated by CH-CEC was superior to that of other insulin liposomes.Conclusion The insulin-liposomes coated by chitosan and its derivatives can enhance enteral absorption of insulin and increase stability of insulin in GI tract.

关 键 词：胰岛素 脂质体 壳聚糖 在体肠灌流法 

分 类 号：R943.4[医药卫生—药剂学]