Evaluation of pharmacokinetics and bioequivalence of valacyclovir hydrochloride tablets by HPLC-MS/MS / 中国药学杂志

ABSTRACT

OBJECTIVE: To establish a simple, sensitive method of high performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS) for the determination of valaciclovir in human plasma, and to evaluate the pharmacokinetics and bioequiva-lence of valaciclovir hydrochloride tablets in healthy volunteers. METHODS: A single oral dose of reference and test tables was given to 24 healthy male volunteers according to randomized crossover design. The plasma samples were precipitated by 30% trifluoroacetic acid, and the supernatant was neutralized by 50% ammonia and injected into the LC-MS/MS system directly. Then internal standard method was used to calculate the concentrations of valaciclovir in plasma. The pharmacokinetic parameters were calculated using SAS 9.1. RESULTS: The main pharmacokinetic parameters of valaciclovir test and reference preparations were as follows ρmax (3457.92 ± 783.83) and(4181.25 ± 1130.19) μ · L-1, t1/2 (3.04 ± 0.41) and (3.13 ± 0.52) h, AUC0-tn(10 624.29 ± 2007.05) and (12 607. 30 ± 2 808.07) μg · h · L-1, respectively. F0-tn was (95.25 ± 15.72), and F0-∞ was (95.32 ± 15.76)%. CONCLUSION: The HPLC-MS/MS method established in this study is simple, sensitive and accurate, and it is suitable for the study of pharmacokinetics of valaciclovir in human plasma. The test tablets are bioequivalent to the reference tablets. Copyright 2012 by the Chinese Pharmaceutical Association.