进食对美欧卡霉素药代动力学和生物利用度的影响

 目的 比较研究空腹、餐后单剂量 po 美欧卡霉素的药代动力学和生物利用度。方法 采用交叉给药方案，10名健康受试者空腹或餐后单剂量 po 600 mg美欧卡霉素，用HPLC测定血药浓度，SCIENTIST程序拟合药代动力学参数，t 检验比较组间差异，双单侧 t 检验评价生物等效性。结果 空腹和餐后单剂量给药的药时曲线均符合单室模型，达峰时间 t_max分别为(0.63±0.11)，(1.02±0.31) h，峰浓度 c_max分别为(2.36±0.35)，(1.82±0.32) μg·ml^-1，消除半衰期 t_1/2分别为(1.31±0.11)，(2.03±0.19) h，药时曲线下面积 AUC 分别为(6.20±1.28)，(6.88±1.46) μg·h·ml^-1。结论 进食使美欧卡霉素的吸收速度减慢、消除半衰期延长，但对吸收总量无显著影响，以 AUC 为指标进行评价，两者生物等效。

Influence of food on pharmacokinetics and bioavailability of miocamycin in normal volunteers after single oral administration

OBJECTIVE To compare the pharmacokinetics and bioavailability of miocamycin under conditions of fasting and after meal. METHODS A single oral dose of miocamycin 600 mg was given to 10 healthy volunteers under the conditions of fasting and after meal in a crossover study.Serum miocamycin concentration was determined by HPLC. RESULTS The concentration-time profile of miocamycin fitted to one compartment model and the pharmacokinetic parameters were:t_max=(0.63±0.11) and (1.02±0.31) h，c_max=(2.36±0.35) and (1.82±0.32) μg·ml^-1，t_1/2=(1.31±0.11) h and (2.03±0.19) h，AUC=(6.20±1.28) and (6.88±1.46) μg·h·ml^{-1/sup>in fasting and after meal conditions,respectively.The absorption rate of miocamycin was delayed and the peak concentration was reduced,with a long elimitration half-time after meal.But the bioavailability of miocamycin had no significant difference. CONCLUSION Miocamycin was bioequivalence between the conditions of fasting and after meal.in terms of AUC.}