阿奇霉素干混悬剂的人体药动学及生物等效性研究

目的:评价2种阿奇霉素干混悬剂的生物等效性。方法:20名男性健康志愿者随机交叉口服受试制剂或参比制剂10袋(含阿奇霉素1.0g)后,采用反相高效液相色谱法测定血浆中的药物浓度,并计算有关药动学参数,通过方差分析和双单侧t检验和1～2α置信区间法进行生物等效性评价。结果:受试制剂与参比制剂中阿奇霉素的Cmax分别为(29.651±5.600)、(29.256±6.382)μg·mL-1,tmax分别为(2.25±0.444)、(2.400±0.503)h,t1/2分别为(37.910±10.181)、(37.980±9.220)h,AUC0～120分别为(458.139±47.368)、(463.114±42.267)μg.h.mL-1,AUC0～∞分别为(519.217±57.262)、(522.980±48.267)μg.h.mL-1。受试制剂相对于参比制剂的生物利用度为(99.5±8.9)%。结论:2种制剂生物等效。

Pharmacokinetics and Relative Bioavailability of Azithromycin Dried Suspension in Human Body

OBJECTIVE： To evaluate the bioequivalence of two kinds of Azithromycin dried suspensions. METHODS： A randomized crossed- over study was conducted in 20 healthy volunteers. After a single dose of test and reference preparations （containing 1.0 g Azithromycin）, the plasma drug levels were determined by RP- HPLC. The related pharmacokinetic parameters were computed and the bioequiavailabilityof the two preparations were evaluated by variance analysis and two one side t test by 1--2α confidence interval method. RESULTS： The main pharmacokineties parameters of test and reference preparations were as follows： C were（29.651± 5.600）μg·mL^-1 and （29.256± 6.382）μg·mL^-1; t were（2.25± 0.444） h and （2.400±0.503）h; t1/2 were（37.910± 10.181） h and （37.980± 9.220）h; AUC0-120 were （458.139±47.368）μg·h·mL^-1 and （463.114± 42.267）μg·h·mL^-1 AUC0-∞were （519.217± 57.262）μg·h·mL^-1 and （522.980± 48.267）μg·h·mL^-1. The relative bioavailability of Azithromycin dried suspension is （99.5± 8.9）% as against the reference preparation. CONCLUSION： The results showed that the two formulations were bioequivalent.