琥乙红霉素干混悬剂的人体生物等效性研究

Study of Human Bioequivalence of Erythromycin Ethylsuccinate Suspension

目的研究琥乙红霉素干混悬剂的人体药代动力学和生物等效性。方法健康志愿者20名,用随机双交叉试验方法,单剂量口服试验制剂琥乙红霉素干混悬剂和参比制剂琥乙红霉素颗粒剂,剂量为800 mg,剂间间隔为2周。用微生物法测定血浆中红霉素的浓度。结果单剂口服试验和参比制剂后血浆红霉素的Cmax分别为1.56±0.33 mg/L和1.49±0.30 mg/L;Tmax分别为0.80±0.17 h和0.85±0.20 h;t1/2分别为2.37±0.63 h和2.37±0.54 h;AUC(0-10)分别为4.87±1.59 mg.h/L和4.58±1.19 mg.h/L;AUC(0-inf)分别为5.20±1.65 mg.h/L和4.91±1.22 mg.h/L;相对生物利用度为(107.2±25.2)%。结论试验制剂和参比制剂具有生物等效性。

Objective To study the human pharmaeokinetics and bioequivalenee of erythromyein ethylsuccinate suspension. Methods A single oral dose（800 mg of tested and reference formulations） was given to 20 healthy volunteers in a randornised crossover study. The concentrations of erythromycin in plasma were determined by microbiological analysis with baciUus subtilis as test strain. Results After a single dose, the pharmacokinetics parameters for erythromygin were as follows：Crux were 1.56 ± 0.33 mg/L and 1.49 ± 0.30 mg/ L; Tmax were 0.80 ± 0.17 h and 0.85 ± 0.20 h; h1/2 were 2.37 ± 0.63h and 2.37 ± 0.54 h; AUC（0-10） were 4.87 ± 1.59 mg· h/L and 4.58 ± 1. 194 mg· h/L; AUC（0-inf） were 5.20 ± 1.65 mg· h/L and 4.91 ± 1.22 mg·h/ L for T and R respectively; the relative bioavailability （ 107.2 ± 25.2） %. Conclusion The results of the statistical analysis show that the two formulations are bioequivalence.