Study on pharmacokinetics of silibinin capsule in Chinese healthy volunteers / 中国药理学通报

ABSTRACT

Aim To investigate the pharmacokinetic characteristics of silibinin in Chinese healthy volunteers.Methods Nine Chinese male healthy volunteers were divided into receiving orally a single dose of silibinin capsule corresponded 70,140 and 280 mg of silibinin,respectively,in Latin square design study.After administration of silibinin capsule,the plasma concentrations were determined by HPLC with UV detection.The pharmacokinetic parameters were analyzed by Topfit 2.0 program.Results The linearity of this method was found to be from 3.125 to 10 000 μg·L~(-1) with a lower limit of quantitation(LLOQ) of 3.125 μg·L~(-1) for silibinin.The pharmacokinetic parameters were calculated as the followsat the three different dosages(70,140 and 280 mg),T_(1/2) was 2.44,2.38 and 2.47 h;C_(max) was 1135.6,2841.1 and 3946.9 μg·L~(-1);T_(max) was 1.35,1.26 and 1.39 h;AUC_(0-11 h) was 1287.2,3337.8 and 5398.5 μg·h·L~(-1);AUC_(0-∞)was 1300.7,3377.1 and 5453.9 μg·h·L~(-1);CL/F was 1062.1,824.7 and 943.2 ml·min~(-1);And V_d was 219.9,167.1 and 212.0 L,respectively.Conclusions The developed method is shown to be sensitive,accurate and simple,and can satisfy the requirement of pharmacokinetic study of silibinin in human.The C_(max),AUC_(0-11 h) and AUC_(0-∞) of silibinin in Chinese healthy volunteers(in ranges of 40～120 mg)are fitted with non-linear kinetic model,while there are no significant differences in T_(1/2) at the three different dosages.