单次口服盐酸伐昔洛韦缓释片在健康人体的药代动力学

Pharmacokinetics of valaciclovir hydrochloride sustained-release tablets after a single oral administration

目的研究盐酸伐昔洛韦缓释片(抗病毒药)在健康人体内的药代动力学特征。方法12名健康志愿者按拉丁方设计分别口服3种单剂量(600,1200,1800mg)盐酸伐昔洛韦缓释片,用高效液相色谱-紫外检测法测定血浆中盐酸伐昔洛韦活性代谢物阿昔洛韦浓度,用DAS1.0软件计算药代动力学参数。结果12名受试者血药浓度随其单次给药剂量的增加而呈现升高趋势,口服盐酸伐昔洛韦缓释片600,1200,1800mg的AUC0～24分别为(6.61±1.38),(13.38±3.76)和(20.62±8.20)mg.h.L-1;Cmax分别为(1.67±0.37),(3.10±0.87)和(4.73±2.15)mg.L-1,不同剂量组的AUC0-24/dose、Cmax/Dose比值间无显著性差异。结论在600～1800mg内,盐酸伐昔洛韦缓释片在健康人体内过程呈线性药代动力学特征。

Objective To study the pharmacokinetics of valaciclovir hydrochloride sustained -release tablets in healthy volunteers after oral administration of different dosages. Methods Twelve healthy volunteers were divided into 3 groups receiving orally a single dose of 600,1200, 1800 mg valaciclovir hydrochloride sustained -release tablets respectively, in latinsquare design study. The plasma concentration of acyclovir, an active metabolism of valaciclovir was determined by HPLC with ultraviolet detection. The pharmacokinetic parameters were analyzed by DAS 1.0 program. Results It was found that plasma levels of acyclovir increased after orally increased dosage of valaciclovir hydrochloride sustained - release tablet in the healthy volunteers. The pharmacokinetic parameters were as follows ： AUC0-24 of three different dosages （600,1200, 1800 mg） were （6.61±1.38）,（13.38±3.76） and （20.62±8.20） mg·h·L^-1;Cmax were （1.67 ±0.37 ） , （3.10±0.87） and （.4.73± 2.15） mg·L^-1. There were no significant differences in AUC0-t/dose, Cmax/dose between the groups. Conchsion The pharmacokinetic char- acteristics of valaciclovir hydrochloride sustained - release tablets in healthy volunteers in the dosage rang of 600 ～ 1800 mg were fitted with linear kinetic model.