摘要
目的评价2种恩替卡韦制剂在健康人体的生物等效性。方法 20例男性健康志愿受试者随机分成2组,分别交叉单剂量口服试验制剂(恩替卡韦分散片)或参比制剂(恩替卡韦片)0.5 mg,2周后交叉服药,采用高效液相色谱-串联质谱法测定血浆中药物浓度,以DAS 3.2.7软件计算药动学参数,进行生物等效性评价。结果 2种制剂的峰浓度(Cmax)分别为(4.41±1.02)μg/L和(4.36±0.89)μg/L;达峰时间(tmax)为(0.66±0.19)h和(0.70±0.29)h;半衰期(t1/2)为(46.11±32.32)h和(61.28±93.69)h;曲线下面积(area under curve,AUC)0~72h为(13.31±2.63)μg·h^(-1)·L^(-1)和(13.10±2.20)μg·h^(-1)·L^(-1)。结论 2种恩替卡韦制剂生物等效,相对生物利用度为(103.3±14.0)%。
Objective To evaluate the bioequivalence of 2kinds of entecavir preparations in human bodies.Methods The randomized,crossed-over study was conducted in 20 healthy volunteers.After A single oral dose of entecavir hydrochloride test and reference preparations（containing 0.5 mg entecavir）,the drug levels in plasma were determined by high performance liquid chromatography-tandem mass spectrometry.The pharmacokinetic parameters were calculated with DAS 3.2.7software,then bioequivalence of the two preparations was evaluated.Results The peak concentrations Cmax,tmax,t1/2and AUC0-72 h of the 2formulations were（4.41±1.02）μg/L and（4.36±0.89）μg/L,（0.66±0.19）h and（0.70±0.29）h,（46.11±32.32）h and（61.28±93.69）h,（13.31±2.63）μg·h^-1·L^-1 and（13.10±2.20）mg·h^-1·L^-1,respectively.Conclusion The results show that the two formulations are bioequivalent.The relative bioavailability of entecavir is（103.3±14.0）%.
出处
《河北医科大学学报》
CAS
2016年第12期1441-1444,共4页
Journal of Hebei Medical University
