两种枸橼酸坦度螺酮制剂的人体生物等效性

Study on Bioequivalence of Two Preparations of Citrate Tandospirone in Chinese Healthy Volunteers

目的研究枸橼酸坦度螺酮胶囊和片剂在健康志愿受试者中的药动学和人体生物等效性。方法 20例男性受试者交叉单剂量(10 mg)口服受试制剂枸橼酸坦度螺酮胶囊和参比制剂枸橼酸坦度螺酮片,用高效液相色谱法测定血药浓度。主要药动学参数峰浓度(Cmax)、平均血药浓度-时间曲线下面积(AUC0-12、AUC0-∞)对数转换后经方差分析,双向单侧t检验和[1-2α]%置信区间评价两制剂的生物等效性。结果受试制剂和参比制剂主要药动学参数:达峰时间(tmax)分别为(0.81±0.16)与(0.87±0.10)h,Cmax分别为(1.66±0.32)与(1.71±0.29)μg·mL-1,AUC0-12分别为(14.56±3.95)与(14.82±3.66)μg·mL-1.h,AUC0-∞分别为(15.05±3.90)与(15.31±3.61)μg·mL-1.h,半衰期(t1/2)分别为(1.24±0.21)与(1.29±0.17)h。与参比制剂相比,受试制剂相对生物利用度为(102.6±5.8)%。结论两种枸橼酸坦度螺酮制剂具有生物等效性。

Objective To study the pharmacokinetics and bioequivalence of citrate tandospirone capsules and tablets in healthy volunteers. Methods A single oral dose of 10 mg citrate tandospirone tested capsules or reference tablets were given to 20 healthy male volunteers in a randomized, two-way crossover study. Plasma drug concentration was determined by high performance liquid chromatography （HPLC）. Peak concentration （ Cmax ）, area under the plasma concentration time curve AUC0-12 and AUC0-∞ were determined. The bioequivalence of citrate tandospirone capsules and tablets was evaluated through variance analysis, two one-side T test and [ 1-2a ] % confidence interval. Results The main pharmacokinetic parameters of the tested （capsules） and reference （tablets） preparations were as follows： time to peak （tmax） was （0. 81±0. 16） and （0.87±0.10） h; Cmax was （1.66±0.32） and （1.71±0.29） μg ·mL-1; AUC0.12 was （14.56±3.95） and （14.82±3.66）μg ·mL-1· h; AUC0-∞ was （15.05±3.90） and （15.31±3.61） μg·mL-1 · h; half-time period （t1/2） was （1.24±0.21） and （1.29±0.17） h, respectively. The relative bioavailability of the tested preparations was （ 102.6± 5.8 ） %. Conclusion The results of the statistical analysis shows that the two tested formulations are bioequivalent.