琥乙红霉素口崩片在健康志愿者的生物等效性

Bioequivalence of erythromycin ethylsuccinate orally disintegrating tablet in healthy volunteers

目的 研究琥乙红霉素口崩片的人体相对生物利用度和生物等效性。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口崩片和参比制剂琥乙红霉素片,剂量为800 mg,交叉间隔为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(1.16±0.38)和(1.03±0.34) mg.L-1;tmax分别为(1.04±0.30 )和(1.02±0.35) h;t1/2分别为(2.48±0.51) h和(2.51±0.36) h;AUC(0-10)分别为(4.12±1.36)和(3.80±1.17) mg.h.L-1;AUC(0-inf)分别为(4.43±1.38)和(4.12±1.20) mg.h.L-1;相对生物利用度为(109.3 ± 22.1)%。结论 试验和参比制剂具有生物等效性。

Objective To study the bioequivalence and relative bioavailability oferythromycin ethylsuccinate orally disintegrating tablet. Methods A single oraldose(800mg of test and reference formulation) were given to 20 healthy volunteersin a randomized crossover study. The concentrations of erythromycin in plasma weredetermined by microbiological analysis with bacillus subtilis as test strain. Thepharmacokinetic parameters were calculated and the bioavailability andbioequivalence of two formulations were evaluated. Results After a single dose, thepharmacokinetic parameters for erythromycin in plasma were as follows: Cmax were(1.16 ± 0.38) and (1.03 ± 0.34) mg.L-1; tmax were (1.04 ± 0.30) and (1.02 ± 0.35) h ;t1/2 were (2.48 ± 0.51) and (2.51 ± 0.36) h; AUC(0-10) were (4.12 ± 1.36) and (3.80 ±1.17)mg.L-1; AUC(0-inf) were (4.43 ± 1.38) and (4.12 ± 1.20) mg.h.L-1 for test andreference respectively; the relative bioavailability was (109.3 ± 22.1)%. ConclusionThe results of the statistic analysis showed that the two formulations werebioequivalence.