氟苯尼考在大鼠肠内吸收特征试验

Studies on Florfenicol absorption characteristics in rat intestine

考察氟苯尼考的溶解度及在大鼠肠内吸收行为,为研究高效快速吸收氟苯尼考制剂提供参考。高效液相色谱法测定药物的浓度,紫外分光光度法测定酚红浓度,以饱和法测定氟苯尼考的溶解度,在肠内循环模型考察氟苯尼考在大鼠体内吸收行为。结果显示,氟苯尼考在蒸馏水、乙醇、丙酮中的饱和溶解度分别为1.224、26.88、78.91mg/mL。低、中、高浓度大鼠肠吸收的吸收速率常数分别为0.221h-1、0.221h-1、0.235h-1,半衰期分别为3.135 7h、3.135 7h、2.961 5h,2h吸收率分别为为35.75%、36%、36.6%。表明氟苯尼考的吸收为一级动力学吸收过程,以被动扩散为主;提示在进行氟苯尼考药物剂型时应该充分考虑到药物的低溶解度、低吸收速度特性。

This study was designed to determine the solubility of florfenicol and its absorption behavior in rat. The concentration of florfenicol was determined by High Performance Liquid Chromatography, and the concentration of phenol red was measured by UV spectrophotometric, the solubility of florfenicol was measured by saturation method,investigated the absorption of florfenicol in rats by in vivo intestinal loop model. The solubility of florfenicol was 1. 224 mg/mL in water, 26.88 mg/mL in ethanol, and 78.92 mg/ mL in acetone. Low medium high concentrations of rat intestinal absorption rate constants were 0. 221 h^-1 ,0. 221 h^-1 and 0. 235 h^-1. The half-life was 3. 135 7 h, 3. 135 7 h and 2. 961 5 h. The absorption rate at 2 h was 35. 750.,4, 36% and 36.6% . The absorption of florfenicol for the first-order kinetics was passive diffusion. So when florfenicol dosage forms are designed, the low drug solubility, low permeability and low absorption rate characteristics should be fully taken into account.