【摘要】 目的评价自制非那雄胺片生物等效性。方法采用正交试验法确定制剂最佳配方,采用双交叉试验设计评价制剂的生物等效性;20例健康男性志愿者随机分为两组,各服用供试片或市售参比片,以HPLC-MS法测定血药浓度,并以3P97软件计算药动学参数和人体相对生物利用度。结果本剂配方合理、质量稳定,供试片和参比片的主要药动学参数分别为:药时曲线下面积(AUC_0～t):（334.19±117.94）、（364.51±155.99）ng·hr/mL;AUC_0～∞:（352.34±129.88）、（380.14±164.66）ng·hr/mL;C_max:（42.24±12.35）、（52.43±18.60）ng/mL;t_max:（2.60±0.91）、（2.20±0.86）h;消除半衰期(t_1/2):（5.34±0.97）、（5.16±1.13）h;MRT:（6.83±0.86）、（6.51±0.77）h。供试片的平均相对生物利用度为（94.31±12.31）%和（95.19±12.69）%(n=20,以AUC_0～t计算),参比片和供试片的AUC_0～t和AUC_0～∞无显著性差异。结论经配方优化的自制非那雄胺片质量稳定,与市售参比片具生物等效性。更多还原

【Abstract】 Objective To evaluate the clinical bioequivalence of self-made finasterides tablets.Methods The formula was optimized by orthogonal experiment.To evaluate bioequivalence of self-made and reference tablets of finasteride by a two way cross over trial.20 healthy male volunteers were randomly divided into two groups and take self-made or reference tablets of finasterides.The concentrations of finasterides plasma were determined by HPLC-MS method.The parameters of pharmacokinetics and relative bioavailability were calculated by 3P97 software.Result The self-made finasterides tablets have reasonable formula and good stability.The pharmacokinetic parameters of the tset tablets and reference tablets were as follows:AUC_0～t:（334.19±117.94）,（364.51±155.99）ng·hr/mL;AUC_0～∞:（352.34±129.88）,（380.14±164.66）ng·hr/mL;C_max:（42.24±12.35）,（52.43±18.60）ng/mL;t_max:（2.60±0.91）,（2.20±0.86）h;t_1/2:（5.34±0.97）,（5.16±1.13）h;MRT:（6.83±0.86）,（6.51±0.77）h.The relative bioavailability of test tablets was（94.31±12.31）% and（95.19±12.69）%(n=20,AUC_0～t).There were no notable differences of AUC_0～t and AUC_0～∞between test tablets and reference tablets.Conclusion The self-made finasterides tablets have good quality and it′s formula is optimistical.The two kinds of finasterides tablets are of bioequivalence.更多还原