阿昔洛韦片剂人体相对生物利用度研究

The Relative Bioavailability of Acyclovir Tablet in Normal Volunteers

选用8名健康男性自愿受试者,随机交叉口服深圳海王药业有限公司生产的阿昔洛韦片剂及湖北省医药工业研究所科益制药厂生产的阿昔洛韦（参比制剂）片剂各400mg,采用高效液相色谱（HPLC）法测定血药浓度,进行相对生物利用度研究。结果表明,本品药代动力学过程符合线性—房室模型特征.受试片剂及参比片剂的达峰时间（Tmax）分别为（0.968±0.224）h和(1.157±O.336）h,峰浓度（Cmax）分别为（O.555±0.221)μg/ml和（O.496±0.149)μg/ml,消除半衰期（T_(1/2)kc）分别为（1.426±0.486）h和(1.630±0.405）h,药—时曲线下面积（AUC）分别为（1.844±0.535）μg/（ml·h）和（1.934±0.483)μg/（ml·h）,受试片剂与参比片剂比较的相对生物利用度为（95.18±12.48）%,变异系数:13.11％。两种口服片剂的达峰时间、峰浓度、消除半衰期和药—时曲线下面积说明两种片剂的吸收速度及吸收程度无明显统计学差异.表明该药品相对生物利用度符合临床应用的要求。

The pharmacokinelics and relative bioavailability of two kinds of acyclovir tablet were determined following 400 mg oral dose of acyclovir given to 8 normal volunteers in an open randomized crossover study. A sensitive high performance liquid chromatographic method was used to determine the serum concenfration of acyclovir. The results indicated that the pharmacokinetics of this drug exhibited a linear 1-compartmant model. The Tmax values werc(0. 968±0. 224) h and (1. 157±0. 336) h, the Cmax values were (0. 555±0. 221) μg/ml and (0. 496±0. 149) μg/ml, the T1/2 ke values were (1. 426±0. 486) h. and (1. 630±0. 405) h, and the areas under the drug concentratio n-time curves (AUC) were (1. 844±0. 535) μg/(mg. h) and (1. 934±0. 483) μg/ (mg. h) for the tested and reference tablet, respectively. The relative bioavailability of acyclovir of tested tablet vs reference tablet was (98. 18±12. 48) % and the CV % was (13. 11) %. The results in Tmax. Cmax, T1/2 Ke, and AvC high performance liguid chromatography showed that there is no evidence for statistical differences between the two kinds of tablet and they were bioequivalence.