国产红霉素肠溶胶囊在健康志愿者的相对生物利用度

Bioequivalence of erythromycin enteric-coated capsules in healthy volunteers

目的:研究国产红霉素肠溶胶囊与进口红霉素肠溶胶囊相对生物利用度.方法:20名健康男性志愿者双周期随机交叉口服单剂量(500 mg)国产和进口红霉素肠溶胶囊两种制剂,分别于服药前及服药后1、2、2.5、3、3.5、4、4.5、5、6、8、10 h采集血样.用微生物法测定血清中红霉素的浓度,并对试验数据进行统计处理.结果:单次口服国产及进口红霉素肠溶胶囊的cmax分别为(2.14±0.75)和(2.11±0.77) mg/L;tmax分别为(3.10±0.58)和(3.30±0.64) h;AUC0～10 h分别为(6.63±2.08)和(6.64±2.18) mg·h/L; AUC0～∞分别为(7.38±2.34)和(7.46±2.41) mg·h/L;国产红霉素肠溶胶囊与进口品相比的相对生物利用度为(100.59±19.47) %;用方差分析及双单侧t检验对国产和进口红霉素肠溶胶囊的生物等效性进行评价,两制剂间差异无显著性.结论:两种红霉素制剂具有生物等效性.

To study relative bioavailability of domestic and imported erythromycin enteric-coated capsules in healthy vol-unteers.A single oral administration of 500mg domestic and imported erythromycin enteric-coated capsules were given to 20healthy male volunteers in randomized crossover study. The washout peried is one week. Microbiological assay was used to determinethe concentrations of erythromycin in human serum. The data were analyzed by 3p97 program.The pharmacokinetic param-eters after a sing1e oral administration of 500 mg domestic and imported erythromycin enterc-coated capsu1es were as follows: cmax(2.14 ±0.75) and (2.11 ±0.77) mg/L; tmax(3.10 ±0.58) and (3.30 ±0.64)h;AUC0-l0h(6.63 ±2.08) and (6.64 ±2.18)mg.h/L;AUC0-∞(7.38 ±2.34) and (7.46 ±2.41 ) mg.h/L; F0-∞(100.59 ±19.47)% respectively. Variance analysis and twoone-sided test were performed to parameters: cmax , AUC0-l0h,AUC0-∞. There was no significant difference. The twopreparations of erythromycin are of bioequivalence.