盐酸克林霉素棕榈酸酯咀嚼片人体生物等效性研究

Bioequivalence study of clindamycin palmitate hydrochloride chewable tablets in healthy volunteers

目的:评价单剂量口服盐酸克林霉素棕榈酸酯咀嚼片与参比分散片在健康人体中药代动力学及其生物等效性特征。方法:20名男性健康志愿受试者,口服盐酸克林霉素棕榈酸酯受试制剂和参比制剂600mg,用双周期交叉设计自身对照试验方法,以液相色谱法测定服药后不同时刻的血药浓度。结果:按该方法测得的克林霉素血药浓度的最低定量限为0.125μg/mL(r=0.999)。受试制剂与参比制剂的主要药代动力学参数Cmax分别为(4.5±1.4)、(4.6±1.4)μg/mL;tmax分别为(0.83±0.33)、(0.90±0.29)h;t1/2分别为(2.3±0.7)、(2.3±0.7)h;AUC0→t分别为(16±6)、(17±6)μg·mL-1·h;AUC0→∞分别为(17±6)、(18±6)μg·mL-1·h,各参数间比较差异无统计学意义(P>0.05)。结论:等效性分析受试制剂的相对生物利用度(F)为96.3%,统计学结果显示两制剂具有生物等效性。

AIM： To compare the pharmacokineties and relative bioequivalenee of chewable tablet of clindamycin palmitate hydrochloride with that of dispersible tablet. METHODS： An open randomized and two-period crossover study with a one week washout interval was performed in 20 healthy volunteers. Concentrations of clindamycin in plasma were assayed by High Performance Liquid Chromatography method after a single oral dose of 600 mg of the tested or the reference tablets. RESULTS： Limit of quantification was accepted as 0. 125 μg/mL （ r = 0.999）. The main pharmacokinetic parameters of the test and the reference formulations were as follows ： Cmax, were （4.5 ± 1.4） and （4.6 ± 1.4） μg/mL; tmax were （0.83 ± 0.33） and （0.90 ± 0.29） h; t1/2 were （2.3 ± 0.7） and （2.3±0.7） h; AUC0→t were （16±6） and （17±6） μg·mL^-1·h; AUC0→∞ were （17 ± 6） and （18 ± 6） μg·mL^-1· h. There was no significant difference between the parameters of two tablets. CONCLUSION： The relative bioavailability of the test tablet to reference tablet was 96.3 %. The results of the statistical analysis show that the two formulations are bioequivalent.