克拉霉素分散片人体药物动力学及生物等效性研究

Pharmacokinetics and Bioequivalance of Clarithromycin Dispersed Tablet in Healthy Volunteers

目的 研究克拉霉素分散片在健康人体内的药物动力学，评价两种分散片的生物等效性。方法 采用随机自身交叉双周期设计方法，将18名健康男性受试者随机分为两组，分别单次交叉口服等剂量克拉霉索分散片供试制剂或参比制剂500mg，采用高效液相色谱-紫外检测法测定血浆中克拉霉素的浓度，计算其药代动力学参数和相对生物利用度，评价两制剂的生物等效性。结果 供试制剂和参比制剂克拉霉索实测AUC0-24分别为20．51±5．90和19．58±5．73vg／（mL·h），Cmax分别为3．34±1．24和3.31±1．27vg／（mL·h）．Tmax分别为1．6±0．5和1．4±0．3h，t1／2分别为7．06±1．45和6．93±1．20h。供试制剂相对于参比制剂的生物利用度为112．3％±43．3％。结论 两制剂具有生物等效性。

Objective To investigate pharmacokinetic of clarithromycin dispersed tablet and to evaluate the bioequivalance of the two dispersed tablets. Methods Eighteen volunteers were ran- domly divided into 2 groups. A single oral dose of 500 mg of test or reference dispersed tablet were given to each volunteer in an open crossover test. The plasma concentration of clarithromy- cin was determined by HPLC-UV. The parameters of pharmacokintic and relative bioavailability were calculated, the bioequivalance of two dispersed tablets were calculated too. Results The main pharmacokinetic parameters of test and reference Clarithromycin were as the followings： AUC0-24 was （20.51±5.90）μg/（mL · h） and（19.58±5.73）μg/（mL · h）;Cmax was （3. 34± 1.24）μg/（mL - h） and（3.31±1.27）μg/（mL - h） ;Tmax was （1.6±0.5）h and（1.4 ±0.3）h; t1/2 was （7.06±1.45）h and （6.93±1.20） h. The relative bioavailability of test to reference preparation was （112.3 ± 43.3）%. Conclusion The two preparations are bioequivalent.