头孢拉定分散片两种服药方法的相对生物利用度及生物等效性研究

The relative bioavailability and bioequivalence of cefradine dispersible tablets which were administrated in two kinds of ways

目的研究健康受试者两种服用方法服用头孢拉定分散片的人体相对生物利用度和生物等效性。方法在12例健康男性受试者中进行标签开放、随机、2×2交叉研究,分别分散后服、吞服头孢拉定分散片0.5 g。采用高效液相色谱(HPLC)法测定血浆中头孢拉定浓度。用DAS软件计算人体相对生物利用度并评价生物等效性。结果分散后服、吞服头孢拉定分散片的达峰时间(t_(max))分别为(46.3±17.5)和(51.3±21.7)min,峰浓度(C_(max))分别为(18.81±4.65)和(16.53±3.83)μg/mL,AUC_(O-t)分别为(1 620±268.2)和(1681±285.5)(μg·min)/mL,经方差分析均无显著性差异(P>0.05)。两种服药方法的相对生物利用度为(96.82±9.30)%。生物等效性检验显示,AUC_(O-t)90%置信区间为92.0%～101.1%,C_(max)90%置信区间为97.2%～130.0%。结论头孢拉定分散片两种服用方法具有生物等效性,临床应用时可分散后服,也可以吞服。

Objective To observe the relative bioavailability and bioequivalence of cefradine dispersible tablets which were administrated in two kinds of ways in healthy male volunteers. Methods According to an open-label, randomized, two-way crossover design, 12 male volunteers were administrated cefradine dispersible tablets （0.5 g）. The cefradine dispersible tablets were taken after dispersed in water or swallowed directly. The plasma concentration of cefradine was determined by a validated HPLC method. Results tmax was （46.34±17.5） and （51.3±21.7） min （P〉0.05） ; Cmax was （18.81±4.65） and （16.53±3.83） μg/mL（P〉0.05）; AUC0-t twas （1 620±268.2） and （1 6814±285.5） μg·min/mL（P〉0.05）. The 90% confidential interval of A UC0-t was 92.0%-101.1%, that of Cmax was 97.2%-130.0%. The relative bioavailability of the two kinds of administration was （96.824±9.30） %. Conclusion Cefradine dispersible tablets which administrated in two kinds of ways are bioequivalence.