甘草酸二铵胶囊人体相对生物利用度研究  

Study on the Relative Bioavailability of Diammonium Glycyrrhizinate Capsule in Healthy Volunteers by HPLC-MS

作　　者：金悠[1] 杨俊[2] 魏磊[2] 吴鹏飞[2] 龙利红[1] 陈建国[1] 

机构地区：[1]华中科技大学同济医学院临床药理研究所,武汉430030 [2]华中科技大学同济医学院药理系,武汉430030

出　　处：《医药导报》2008年第8期915-917,共3页Herald of Medicine

摘　　要：目的建立甘草酸二铵的活性代谢产物甘草次酸血药浓度的液-质联用色谱测定法(LC-MS),并对甘草酸二铵胶囊在健康受试者体内的生物等效性进行研究。方法采用两制剂双周期随机交叉试验设计,20例男性健康受试者先后分别单剂量口服甘草酸二铵受试制剂或参比制剂150 mg,采用液-质联用色谱法,以熊果酸为内标,测定血浆中其活性代谢产物甘草次酸的浓度。采用DAS 2.0药动学软件进行数据处理。结果试验制剂与参比制剂的AUC0-t分别为(1648.49±230.55)和(1609.27±265.59)ng.mL-1.h;Cmax分别为(95.97±14.99)和(93.05±17.91)ng.mL-1;tmax分别为(12.00±1.30)和(11.80±1.44)h。结论两种制剂人体内血药浓度变化符合二室模型,两药的平均生物利用度为(103.5±12.7)%(AUC0-t),具有生物等效性。Objective To develop a LC-MS assay for determination of glycyrrhetic acid in human plasma and to estimate the relative bioavailability of diammonium glycyrrhizinate capsules in 20 healthy volunteers. Methods According to a randomized two-period crossover design, 20 healthy volunteers were orally administered with 150 mg diammonium glycyrrhizinate capsules or reference ones, respectively. Glycyrrhetic acid in plasma was determined by LC-MS with ursolic acid used as internal standard, and the data were processed with DAS 2.0 pharmacokinetic program. Results The pharmacokinetic parameters of the two tablets were as follows： AUC0-t were （1 648.49±230.55） and （1 609.27 ± 265.59） ng· mL^-1 · h, Cmax were （95.97±14.99） and （93.05 ±17.91） ng ·mL^-1, tmax were （12.00 ±1.30） and （11.80±1.44） h, respectively. ConcLusion The concentration-time curves of two tablets arc consistent with a two-compartment model. The mean relative bioavailability is （ 103.5 ± 12.7 ） % （AUC0-t ）, both of which are bioequivalent.

关 键 词：甘草酸二铵 甘草次酸 液-质联用色谱法 生物等效性 

分 类 号：R286[医药卫生—中药学] R965[医药卫生—中医学]