罗红霉素无味颗粒剂人体生物等效性研究

Study on bioequivalence of roxithromycin tasteless granules in healthy volunteers

目的测定罗红霉素无味颗粒剂生物等效性。方法采用随机双周期、双交叉实验设计,18名健康志愿者分别单剂空腹口服罗红霉素受试和参比颗粒剂300mg,于不同时间采集血样,以高效液相色谱(HPLC)法测定血浆中药物浓度,并进行生物等效性评价。结果受试和参比颗粒剂的达峰时间分别为2.00±0.34(h)和2.00±0.00(h),达峰时血中药物浓度分别为14.87±2.14(μg·mL-1)和15.18±2.90(μg·mL-1),两种制剂的消除相半衰期分别为12.57±1.30(h)和12.03±1.87(h),药时曲线下面积(AUC0→48)分别为140.26±26.47μg/(mL·h)和146.11±29.93μg/(mL·h),(AUC0→∞)分别为152.74±27.66μg/(mL·h)和157.11±33.51μg/(mL·h)。将主要药动学参数经方差分析、双单侧t检验、90%置信区间分析表明结果差异无统计学意义。结论罗红霉素受试颗粒剂与参比颗粒剂具生物等效性。

OBJECTIVE To determine the bioequivalence of roxithromycin （RM）tasteless granules. METHODS On an empty stomach, 18 healthy volunteers were randomly administrated with an oral single crossover dose of 300 mg test preparation or reference preparation. Blood samples were collected at different interval, and the plasma concentration of RM was measured by HPLC, then the results were used to evaluate the bioequivalence. RESULTS The pharmacokinetic parameters for the test and reference preparation were as follows： Tmax were（2.00 ± 0.34）h and（2.00 ± 0.00）h;Cmax were（14.87 ± 2.14）μg· mL^-1 and（15.18 ± 2.90）μg· mL^-1 ; t1/2 were（12.57 ± 1.30）h and（12.03 ± 1.87）h;AUC0→48 were（140.26 ± 26.47）μg· （mL· h）^-1 and（146.11 ± 29.93）μg· （mL· h）^-1 ; AUC0→∞ were（152.74 ± 27.66） μg· （mL· h）^-1 and（ 157.11 ± 33.51） μg· （mL· h）^-1, respectively. There were no significant differences in main pharmacokinetic parameters of the two preparations according to the results Of ANOVA and two-one-sided t-test with 90 % confidence interval. CONCLUSION The test granules is bioequivalent to the reference granules.