姜黄素壳聚糖盐酸盐脂质体大鼠药代动力学和在体肠吸收研究

Pharmacokinetics and Intestinal Absorption of Curcumin Chitosan Hydrochloride Coated Liposome in Rats

目的:考察姜黄素壳聚糖盐酸盐脂质体(CCLP)的药代动力学和在体肠吸收特征。方法:SD大鼠灌胃给药后,定时采血,采用DAS软件分析处理数据,并建立大鼠在体肠吸收模型,利用单向灌流法考察CCLP体肠道吸收行为。结果:CCLP的AUC0-t、AUC0-∞、t1/2、Cmax较游离药物分别为CUR的1.73、1.95、1.56、1.91倍;CCLP在十二指肠、空肠、回肠、结肠4个肠段的药物吸收速率常数分别为CUR的1.48、1.28、1.17、4.01倍,有效渗透率分别为CUR的1.58、1.33、1.30、4.55倍,CCLP在结肠段的吸收有显著提高。结论:CCLP能明显提高姜黄素的生物利用度,延长其作用时间,并促进其在各肠段的吸收,特别是结肠段的吸收。

Objective： To investigate the pharmacokinetics and intestinal absorption characteristic of curcumin chitosan hydrochloride coated liposome（CCLP） in SD rats. Methods： Blood samples were collected after oral administration. Pharmacokinetic parameters were analyzed by DAS program. Rat single pass intestinal perfusion method was employed to investigate the absorption mechanism. Results： The AUC0-t,AUC0-∞,t1 /2、and Cmaxof CCLP were 1. 73-fold,1. 95-fold,1. 56-fold and 1. 91-fold of the free drug. The intestinal absorption rate constant（Ka） of CCLP in duodenum,jejunum,ileum and colon were 1. 48,1. 28,1. 17,and 4. 01 times as much as the free drug and the effective permeability（Peff） of CCLP were 1. 58,1. 33,1. 30 and 4. 55 times of the free drug,respectively. Conclusion： The bioavailability of CCLP in rats is increased remarkably and Kais increased in various intestinal segments by CCLP,especially in colon,as well as Peff.