Johnson K I, Hoppe H J, Schatton W
Arzneimittelforschung. 1984;34(12):1785-7.
The relative bioavailability of 2-(p-chlorophenoxy)-2-methylpropionic acid [2-(nicotinyloxy)-ethyl]-ester (etofibrate) from Lipo-Merz retard (500 mg) with respect to Lipo-Merz (600 mg) has been determined in 10 health volunteers in a crossover study. Etofibrate was determined in plasma after hydrolysis to clofibrinic acid. Pharmacokinetic parameters were derived to describe the plasma concentration-time profiles using a minimisation of least squares technique. The absorption was apparently delayed following the sustained release formulation with a longer time to maximum plasma concentration, which was significantly lower following the retard form. No significant differences were found in the mean apparent elimination half-lives nor areas under the plasma concentration-time curves indicating that the two formulations can be considered bioequivalent.
在一项交叉研究中,对10名健康志愿者测定了Lipo-Merz缓释片(500毫克)中2-(对氯苯氧基)-2-甲基丙酸[2-(烟酰氧基)-乙酯](益多酯)相对于Lipo-Merz(600毫克)的相对生物利用度。水解为氯贝酸后测定血浆中的益多酯。使用最小二乘法技术得出药代动力学参数以描述血浆浓度-时间曲线。采用缓释制剂后吸收明显延迟,达到最大血浆浓度的时间更长,缓释剂型后的最大血浆浓度显著更低。平均表观消除半衰期和血浆浓度-时间曲线下面积未发现显著差异,表明这两种制剂可视为生物等效。