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目的观察伐昔洛韦缓释片在健康人体内的药代动力学情况。方法 2013年4月-2014年5月选择健康受试者16例,第1周,受试者禁食12 h后于次日晨空腹口服伐昔洛韦缓释片300 mg,温开水200 ml服下,服药后2 h方可饮水,服药后4 h统一进食;隔1周后进行第2周期单剂量600 mg给药,再间隔1周后进行第3周期单剂量900 mg给药,给药方法同第1周。各剂量组均于服药前及服药后0.5、1、1.5、2、2.5、3、4、6、8、10、12、24h抽取前臂静脉血。根据血药浓度-时间数据模拟确定模型,选择最佳药代动力学模型,对各个体的药代动力学参数进行计算,药时曲线下面积(AUC)按梯形面积法计算。结果本研究中阿昔洛韦的回收率高,日内和日间精密度变异小。受试者口服伐昔洛韦缓释片300、600、900 mg后,三个剂量间滞后时间(lag time)、分布半衰期(t1/2ka)、消除半衰期(t1/2ke)、达峰时间(tmax)、清除率(CL/F)经单因素方差分析,比较差异均无统计学意义(P>0.05)。而三个剂量间峰浓度(Cmax)[(0.50±0.16)、(1.05±0.25)、(1.36±0.20)μg·h/m L]、0~t药时曲线下面积(AUC0-t)[(7.00±1.13)、(13.64±2.60)、(18.60±2.49)μg·h/m L]经单因素方差分析比较差异均有统计学意(P<0.05)。结论盐酸伐昔洛韦缓释片在临床应用中具有明显的缓释作用。
Objective To observe the pharmacokinetics of valaciclovir sustained-release tablets in healthy volunteers. Methods From April 2013 to May 2014, 16 healthy subjects were selected. In the first week, the subjects were fasting for 12 hours and were dosed with 300 mg of valaciclovir sustained-release tablets and 200 ml of warm water 2 hours after taking the medication before drinking water, 4 h after taking the unified feeding; every other week after the second cycle of a single dose of 600 mg, and then one week after the third cycle of a single dose of 900 mg to give The same method of treatment with the first week. Each dose group were taken before taking and after taking 0.5,1,1.5,2,2.5,3,4,6,8,10,12,24 h forearm venous blood. Pharmacokinetic parameters of each individual were calculated according to the model of drug concentration-time data simulation, and the best pharmacokinetic model was selected. The area under the curve (AUC) was calculated by the trapezoidal area method. Results The recoveries of acyclovir in this study were high, and variation in intra- and inter-day precision was small. After oral administration of 300,600 and 900 mg of valaciclovir sustained-release tablets, the lag time, distribution half-life (t1 / 2ka), elimination half-life (t1 / 2ke), and peak time tmax), clearance rate (CL / F) by one-way analysis of variance, the difference was not statistically significant (P> 0.05). (Cmax) [(0.50 ± 0.16), (1.05 ± 0.25), (1.36 ± 0.20) μg · h / m L], and the area under the curve of 0 ~ t drug dose (AUC0-t) (7.00 ± 1.13), (13.64 ± 2.60) and (18.60 ± 2.49) μg · h / m L, respectively. The difference was statistically significant by one-way ANOVA (P <0.05). Conclusion Valaciclovir Hydrochloride Sustained Release Tablets have obvious sustained release effect in clinical application.