阿奇霉素胶囊人体生物等效性研究

Bioequivalence of Azihromycin Capsules in Healthy Volunteers

目的:研究阿奇霉素胶囊的人体生物等效性。方法:21名健康志愿者采用拉丁方设计,分为A、B、C3组,分别交叉单剂量口服阿奇霉素胶囊受试制剂1(规格:每粒0.25g)、受试制剂2(规格:每粒0.125g)及参比制剂(规格:每粒0.25g)后,用微生物法测定血药浓度,计算药动学参数,并进行生物等效性评价。结果:受试制剂1、受试制剂2、参比制剂的Cmax分别为(1.06±0.41)、(0.99±0.54)、(1.07±0.53)μg·mL-1,tmax分别为(2.38±0.86)、(1.86±0.85)、(2.52±1.40)h,AUC0～144分别为(11.00±6.15)、(10.65±5.17)、(10.49±5.17)μg·h·mL-1,AUC0～∞分别为(12.48±7.27)、(11.65±5.64)、(11.57±5.87)μg·h·mL-1;阿奇霉素胶囊受试制剂1、2的相对生物利用度分别为(102.73±15.63)%、(103.17±13.64)%。结论:2种规格的阿奇霉素胶囊与参比胶囊均具有生物等效性。

OBJECTIVE： To study the bioequivalence of azihromycin capsules in healthy volunteers. METHODS： 21 healthy volunteers designed by latin square were divided into group A, B and C. The three groups were given single dose of azihromycin capsules 1 （0.25 g in every capsule）, azihromycin capsules 2（0.125 g in every capsule） and reference preparation（0.25 g in every capsule）. The plasma concentrations of azihromycin were determined by microbiological assay and pharmacokinetic parameters were calculated and the bioequivalence was evaluated. RESULTS： Main pharmacokinetic parameters of three kinds of preparations were as follows： （1.06±0.41）μg·mL^-1（0.99±0.54）μg·mL^-1（1.07±0.53）and （1.07± 0.53） μg·mL^-1; tmax（2.38 ±0.86）h, （1.86 ±0.85）h and （2.52±1.40）h; AUC0-144（11.00 ±6.15）μg·mL^-1, （10.65 ± 5.17） μg·mL^-1 and （10.49 ± 5.17）μg·mL^-1 ;AUC0-∞（12.48 ± 7.27） μg·mL^-1, （11.65 ± 5.64） μg·mL^-1 and （11.57 ± 5.87） μg·mL^-1. The relative bioavailabitity of azihromycin capsules 1 and azihromycin capsules 2 were （102.73 ± 15.63）% and （103.17 ± 13.64）%. CONCLUSION： The results suggest that two specifications of azihromycin capsules are bioequivalent to reference preparation.