盐酸伐昔洛韦片人体生物等效性研究

Bioequivalence of Valaciclovir Hydrochlordide Tablets in Healthy Volunteers

目的研究盐酸伐昔洛韦片在健康人体内的生物等效性。方法20名受试者单剂量、交叉口服盐酸伐昔洛韦片受试制剂和参比制剂后,采用高效液相色谱-荧光检测法测定其体内代谢转化物阿昔洛韦的血药浓度,以BAPP2.0程序计算药动学参数和生物等效性数据。结果受试制剂和参比制剂的阿昔洛韦,其Cmax分别为(2.04±0.48)、(1.94±0.37)μg·mL-1,tmax分别为(1.3±0.6)、(1.4±0.6)h,t1/2分别为(2.53±0.42)、(2.55±0.43)h,AUC0～12分别为(5.82±0.99)、(5.54±0.84)μg·h·mL-1,AUC0～∞分别为(6.04±1.04)、(5.76±0.94)μg·h·mL-1。经方差分析和配对t检验,受试制剂与参比制剂的药动学参数无显著性差异(P>0.05),受试制剂的相对生物利用度为(105.7±13.9)%。结论2种制剂具有生物等效性。

OBJECTIVE：To study the bioequivalence of valaciclovir hydrochlordide tablets in healthy volunteers.METHODS： A total of 20 subjects were administered with single dose of test and reference preparations of valaciclovir hydrochlordide tablets by a cross- over way.The blood concentration of valacilovir and the metabolite in vivo were determined by HPLC- fluoremetry, and the pharmacokinetic parameters and the bioequivalence were computed using BAPP2.0 pharmacokinetic program .RESULTS：The main pharmacokinetic parameters of the test preparation vs. the reference preparation of aciclovir tablets were as follows： Cmax were（2.04±0.48） vs.（1.94±0.37） μg . mL^-1, tmax were（1.3±0.6） vs.（1.4±0.6） h, t 1/2 were（2.53± 0.42） vs.（2.55±0.43） h, AUC0-12 were（5.82±0.99） vs.（5.54±0.84） μg . h . mL^-1, AUC0-∞ were（6.04± 1.04）, （5.76± 0.94） μg . h . mL^-1.No significant difference was found in pharmacokinetic parameters between two preparations by method analysis and paired t test（P 〉 0.05） .The bioequivalence of test tablets was （105.7± 13.9）% .CONCLUSION： The results of statistics analysis show that the test and reference tablets were bioequivalent.