克拉霉素软胶囊在中国健康人体的生物等效性研究

Bioequivalence of Clarithromycin soft capsules in healthy Chinese volunteers

目的:评价受试制剂克拉霉素软胶囊与参比制剂克拉霉素片在中国健康人体中的生物等效性。方法:采用双周期随机交叉试验设计,入选20名男性健康受试者单剂空腹口服参比制剂和受试制剂0.25g,采用液相色谱-串联质谱法(LC-MS/MS)测定血浆中克拉霉素的浓度,经BAPP2.0软件处理参数,并进行双单侧t检验确定是否生物等效。结果:主要药代动力学参数:受试制剂和参比制剂克拉霉素的达峰时间tmax分别为(2.1±0.6)、(2.0±0.8)h;Cmax分别为(815±191)、(800±200)ng/mL;t1/2分别为(4.0±0.4)、(3.9±0.5)h;AUC0-24h分别为(5612±1283)、(5246±1375)ng.h.mL-1;AUC0-∞分别为(5722±1313)、(5339±1402)ng.h.mL-1。受试制剂与参比制剂的相对生物利用度为(110.5±23.9)%。结论:受试制剂克拉霉素软胶囊与参比制剂克拉霉素片生物等效。

AIM： To evaluate the bioequivalence of Clarithromycin soft capsule in healthy Chinese volunteers.METHODS： A single oral doses of 0.25 g Clarithromycin soft capsule and tablet（test and reference） were given to 20 healthy volunteers according to an open randomized crossover design.The concentrations of Clarithromycin in plasma were determined by LC-MS/MS.With the aid of BAPP2.0,the bioequivalence of the test and reference preparation were calculated by analysis of variance,tow one sided t-test.RESULTS：The pharmacokinetic parameters of the two preparations were as follow： tmax of test drug and reference drug were（2.1±0.6）、（2.0±0.8）h,Cmax were（815±191）、（800±200） ng/mL,t1/2 were（4.0±0.4）、（3.9±0.5） h,AUC0-24 were（5612±1283）、（5246±1375） ng·h·mL-1,AUC0-∞ were（5722±1313）、（5339±1402） ng·h·mL-1,respectively.The relative bioavailability of the test formulation were（110.5±23.9）%.CONCLUSION： The tested preparation was of bioequivalence to the reference preparation.