盐酸小檗碱脂质纳米粒的药代动力学及生物等效性研究  

Pharmacokinetics and bioequivalence of berberine hydrochloride lipidic nanoparticles in rats

作　　者：袁誉铭 徐靖鑫 张景勍[1] YUAN Yu-ming;XU Jing-xin;ZHANG Jing-qing(Chongqing Research Center for Pharmaceutical Engineering,Chongqing Medical University of Pharmacy,Chongqing 400016,China)

机构地区：[1]重庆医科大学药学院重庆药物高校工程研究中心,重庆400016

出　　处：《中国临床药理学杂志》2022年第11期1251-1254,共4页The Chinese Journal of Clinical Pharmacology

基　　金：重庆市社会事业与民生保障科技创新专项基金资助项目(cstc2017shmsA130028)。

摘　　要：目的研究盐酸小檗碱(BH)和盐酸小檗碱脂质纳米粒(BHLN)在大鼠体内的药代动力学及其生物等效性。方法采用溶剂蒸发法制备盐酸小檗碱脂质纳米粒,并测定其粒径与电位。将大鼠随机分组给予相同药量,于不同的时间点采集血样,用HPLC法测定血药浓度,用DAS(2.1.1版)软件分析主要的药代动力学参数及计算生物等效性。结果BHLN的平均粒径和电位分别为(128.32±2.55)nm和(-30.34±0.83)mV。BHLN和盐酸小檗碱的T_(max)分别为0.75和1.50 h,AUC_(0-72) h分别为1192.35和353.47μg·h·L^(-1),C_(max)分别是537.21和157.92μg·L^(-1)。BHLN的C_(max)较盐酸小檗碱增大了3.40倍,AUC_(0-72) h是盐酸小檗碱的3.37倍,AUC_(0-72) h,C_(max)和T_(max)差异均有统计学意义(均P<0.05)。结论将盐酸小檗碱制备为BHLN显著提高其口服生物利用度,延长了盐酸小檗碱的体内作用时间,且BHLN和盐酸小檗碱不具有生物等效性。Objective To study the pharmacokinetics of Berberine hydrochloride(BH)in rats and to compare the bioavailability and bioequivalence of the berberine hydrochloride lipidic nanoparticles(BHLN).Methods Berberine hydrochloride lipidic nanoparticles was prepared by the solvent evaporation methods.The particle size and zeta potential of berberine hydrochloride lipidic nanoparticles were measured by dynamic light scattering analysis.The rats were randomly divided into two groups and given the same dose.Blood samples were collected at different time points and the blood concentration was determined by HPLC.The DAS(version 2.1.1)software was used to calculate the main pharmacokinetic parameters and bioequivalence.Results The particle size of BHLN was(128.32±2.55)nm and the zeta potential was(-30.34±0.83)mV.The T_(max) of BHLN and BH were 0.75 and 1.50 h,AUC_(0-72) h were 1192.35 and 353.47μg·h·L^(-1),C_(max) were 537.21 and 157.92μg·L^(-1),respectively.The C_(max) of BHLN was 3.40 times larger than that of BH,and the AUC_(0-72) h was 3.37 times that of BH.The results of AUC_(0-72) h,C_(max) and T_(max) were statistically different(all P<0.05)by analysis of variance and wilconxon rank sum test.Conclusion The preparation of BH into BHLN significantly improves its oral bioavailability and prolongs the in vivo action time of BH,and BHLN and BH are not bioequivalent.

关 键 词：盐酸小檗碱 脂质纳米粒 药代动力学 生物利用度 生物等效性 

分 类 号：R28[医药卫生—中药学]