头孢他美酯分散片在人体内的相对生物利用度及生物等效性

Relative bioavailability of Cefetamet pivoxil dispersible tablet in human plasma

目的建立HPLC法测定人血浆中头孢他美的浓度,并研究头孢他美酯分散片在人体内的相对生物利用度及生物等效性。方法18名受试者随机均分成两组,先后单剂量po受试制剂或参比制剂后,采用HPLC法测定血药浓度,计算药动学参数并进行生物等效性判定。结果单次服用0.5 g受试制剂或参比制剂后的药动学参数AUC0→14、AUC0→∞、Tm ax、Cm ax、t1/2分别为22.07±3.98μg.h.m l-1和21.31±4.37μg.h.m l-1,22.62±4.06μg.h.m l-1和21.99±4.54μg.h.m l-1,2.42±0.55 h和2.61±0.50 h,4.16±0.74μg.m l-1和3.95±0.87μg.m l-1,2.24±0.26 h和2.48±0.33 h。实验制剂对参比制剂的相对生物利用度为105.0%±14.6%。两种制剂的药动学参数无明显差异。结论受试制剂与参比制剂具有生物等效性。

OBJECTIVE To determine Cefetamet in human plasma by HPLC method, and study on its relative bioavailability and bioequivalence. METHODS Eighteen volunteers were randomly divided into 2 groups. And then, followed with administration of the trial preparation or reference preparation. The plasma concentration of Cefetamet was measured by HPLC method. Pharmacokinetie parameters and Bioequivalence was determined. RESULTS The pharmacokinetie parameters AUC0→4, AUC0→∞ , Tmax Cmax and t1/2 of the olunteers after taking a single dose of 60 mg of the trial preparation or the reference preparation were 22.07 ± 3.98μg· h·ml^-1 and 21.31 ±4.37 μg·h·ml^-1 , 22.62 ±4.06 μg·h·ml^-1and 21.99 ±4.54 μg·h·ml^-1, 2.42±0.55 h and 2.61±0.50 h, 4.16 ±0.74 μg·ml^-1 and 3.95 ±0.87 μg·ml^-1, 2.24± 0.26 h and 2.48 ± 0.33 h, respectively. The relative bioavailability was 105.0% ± 14. 6%. No significant differences were found among the main pharmacokinetic parameters. CONCLUSION The two preparations were equivalent.