盐酸伐昔洛韦片人体生物等效性研究

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。

Bioequivalence of Valaciclovir Hydrochlordide Tablets in Healthy Volunteers

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,t1/2 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.