聚乙二醇维生素E琥珀酸酯修饰的姜黄素脂质体的药代动力学及在体肠吸收

发布时间：2018-08-23 12:25

【摘要】：目的考察聚乙二醇维生素E琥珀酸酯(TPGS)修饰的姜黄素脂质体的药代动力学和在体肠吸收。方法大鼠灌胃给药,高效液相色谱法测定各时间点的血药浓度,应用DAS软件处理数据;采用大鼠在体单向灌流模型,考察TPGS修饰的姜黄素脂质体在不同肠段的吸收情况。结果 TPGS修饰的姜黄素脂质体的血药浓度-时间曲线下面积(AUC),最大血药浓度(Cmax)分别为游离药物的2.13、2.61倍;其十二指肠、空肠、回肠、结肠各肠段的吸收速率常数(Ka)相对于游离药物分别提高了0.84、1.77、1.48、4.99倍,有效渗透率(Peff)相对于游离药物分别提高了1.56、2.06、2.82、7.17倍。结论 TPGS修饰的姜黄素脂质体有良好的促吸收效果,并能提高姜黄素的生物利用度。
[Abstract]:Objective to investigate the pharmacokinetics and in vivo absorption of curcumin liposomes modified with polyethylene glycol vitamin E succinate (TPGS). Methods Rats were given intragastric administration of curcumin liposomes at different time points by high performance liquid chromatography (HPLC). The data were processed by DAS software and the absorption of curcumin liposomes modified by TPGS in different intestinal segments was investigated by unilateral perfusion model in vivo. Results the area of TPGS modified curcumin liposome was 2.13 ~ 2.61 times higher than that of free curcumin liposome, and the area under the curve of concentration and time of (AUC), was 2.13 ~ 2.61 times of that of free drug, respectively, and its duodenum, jejunum, ileum, jejunum and ileum were also increased. Compared with free drugs, the absorption rate constant (Ka) of colon and the effective permeability (Peff) of colon were increased by 0.84 ~ 1.77 ~ 1.484.99 times and 1.56 ~ 2.206 ~ 2.82 ~ 7.17 times higher than those of free drugs, respectively. Conclusion TPGS modified curcumin liposomes has a good absorption effect and can improve the bioavailability of curcumin.
【作者单位】：重庆医科大学药物高校工程研究中心;
【基金】：重庆市教育委员会首批高等学校优秀人才资助项目(KJ120321)
【分类号】：R965

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