盐酸头孢他美酯分散片人体药物动力学及生物等效性研究

Pharmacokinetics and bioequivalance of cefetamet pivoxil dispersible tablets in healthy volunteers

目的 研究盐酸头孢他美酯分散片在健康人体内的药物动力学，并评价其与同剂量的普通片剂的生物等效性。方法18名健康男性志愿者采用随机交叉自身前后对照口服盐酸头孢他美酯供试制剂或参比制剂500mg，用高效液相色谱法测定盐酸头孢他美血药浓度，计算药物动力学参数和相对生物利用度，评价两种制剂的生物等效性。结果供试制剂和参比制剂的AUC0～12分别为（16．61±6．68）、（15．58±7．25）μg·h·mL^-1，AUC0～∞分别为（18．00±7．01）、（16．93±7．55）μg·h·mL^-1，Cmax分别为（3．10±1．24）、（2．95±1．30）μg·mL^-1，tmax分别为（2．11±0．53）、（2．64±0．23）h，t1/2分别为（2．61±0．50）、（2．65±0．61）h。相对生物利用度为109．1％±14．0％。结论盐酸头孢他美酯分散片具有崩解快、吸收快的特点，相同剂量的分散片和普通片生物等效。

OBJECTIVE To study the pharmacokinetics of cefetamet pivoxil dispersible tablets, and to evaluate its bioequivalance to the ordinary tablets. METHODS A single oral dose of 500 mg of test or reference preparation was given to 18 healthy volunteers according to an open randomized crossover study. The plasma concentration of cefe tamet was determined by HPLC. The parameters of pharmacokinetics and relative bioavailitivity were calculated, the bioequivalance of the two preparations were analysed. RESULTS The main pharmacokinetic parameters of the test and the reference preparations were as follows： AUC0-12 was （16.61±6.68） and （15.58±7.25） μg · h · mL^-1 ;AUC0-∞ was （18.00±7.01） and （16.93±7.55） μg · h · mL^-1 ; Cmax was （3. 10±1.24） and （2.95±1.30） μg · mL^-1; tmax was （2.11±0.53） and （2.64±0.23） h; t1/2 was （2.61±0.50） and （2.65±0.61） h. The relative bioavailitivity of test to reference preparation was 109.1±14.0%. CONCLUSIONS The cefetamet pivoxil dispersible tablet has the characteristics of rapid disintegration and absorption and is bioequivalent to the ordinary cefetament pivoxil tablet.