摘要
目的研究缬更昔洛韦片剂(抗病毒药)在健康人体内的原药缬更昔洛韦及其活性代谢产物更昔洛韦的药代动力学过程。方法20名健康男性受试者单次口服缬更昔洛韦片900mg,用LC-MS/MS测定给药后不同时间血浆中缬更昔洛韦及其活性代谢产物更昔洛韦的浓度,研究缬更昔洛韦与更昔洛韦的药代动力学特征。结果主要药代动力学参数如下。缬更昔洛韦:AUC0-t为(606.83±245.53)μg·h·L-1;AUC0-∞为(616.52±247.89)μg·h·L-1;Cmax为(423.56±178.20)μg·L-1;tmax为(1.15±0.41)h;t1/2为(0.82±0.25)h;MRT0-t为(1.58±0.37)h;MRT0-∞为(1.66±0.38)h;Ka为(2.57±2.53)h-1;Ke为(0.91±0.24)h-1;V/F为(1963.85±920.05)L;CL/F为(1688.77±636.77)L·h-1。更昔洛韦:AUC0-t为:(24.99±7.78)mg·h·L-1,AUC0-∞为(26.37±7.80)mg·h·L-1;Cmax为(7.11±1.96)mg·L-1;tmax为(1.76±0.59)h;t1/2为(3.49±0.96)h;MRT0-t为(4.04±0.80)h;MRT0-∞为(4.81±0.84)h;Ka为(1.13±1.20)h-1;Ke为(0.21±0.07)h-1;V/F为(178.55±44.82)L;CL/F为(37.33±11.92)L·h-1。结论本文建立的测定方法,简单、快速、无干扰,适合人体内血药浓度监测和药代动力学研究。
Objective To study the pharmacokinetics of valganciclovir and its active metabolite ganciclovir of valganciclovir tablet in healthy volunteers. Methods Nine hundreds mg single oral dose of valganciclovir tablet was given to 20 healthy volunteers. The plasma concentrations of unaltered valganciclovir and its active metabolite ganciclovir were determined by LC -MS/MS method. The pharmacokinetic parameters were measured. Results The main pharmacokinetic parameters of valganciclovir were as follow： AUC0-t was （606. 83 ± 245. 53）μg · h · L^-1; AUC0-∞ was（616.52 ±247.89）μg · h · L^-1; Cmax was（423.56 ± 178.20）μg · L^-1; tmax was（1.15 ±0.41）h; t1/2 was（0.82 ±0.25）h; MRT0-t was（1.58 ±0.37） h; MRT0-∞ was（1.66 ±0.38） h; Ka was （2.57±2.53） h^-1;Ke was （0.91 ±0.24） h^-1; V/F was （1963.85 ± 920.05） L; CL/F was （1688.77±636.77） L · h^-1. The main pharmacokinetic parameters of ganciclovir were as follow ： AUC0-t was（ 24.99 ± 7.78）μg · h · L^-1; AUC0-∞ was （26.37±7.80） μg · h · L^-1; Cmax,was（7.11 ± 1.96） mg · L^-1; tmax was（ 1.76 ±0.59） h; t1/2 was（3.49±0.96） h; MRT0-t was（4.04 ±0.80） h; MRT0-∞ was（4.81 ±0.84） h; Ka was （1.13±1.20） h^-1;Ke was （0.21 ±0.07） h^-1; V/Fwas （178.55±44.82） L; CL/F was （37.33 ± 11.92） L · h^-1. Conclusion The method to determinate the concentrations of valganciclovir and ganciclovir is simple, quick and not inferfering, which is suitablele for the monitor of plasma concentration and the pharmacokinetic study.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2007年第3期205-208,共4页
The Chinese Journal of Clinical Pharmacology
