辛伐他汀大鼠在体小肠吸收动力学

Study on the absorption kinetics of simvastatin in rat small intestine

目的:研究辛伐他汀大鼠在体小肠的吸收情况。方法:采用大鼠在体小肠回流实验装置,利用UV分光光度法测定肠循环液中酚红的含量和HPLC法测定辛伐他汀的含量。结果:辛伐他汀在低、中、高3种不同浓度下,吸收速率常数分别为0.756,0.795,0.783h-1。结论:吸收动力学为一级吸收。在低、中、高3种不同浓度下,吸收速率常数差异无显著性,其吸收机制为被动扩散。

OBJECFIVE To explore the absorption mechanism of simvastatin from various intestinal segments. METHODS The absorption kinetics and permeability rate constant s（ka） were investigated by the in situ perfusing method in rats, the concentration of Phenol red was determined using UV and the concentration of simvastatin was determined by HPLC. RESULTS It was shown that the small intestine was the best absorption segment. The permeability rate constants of simvastatin were 0, 756,0. 795, 0, 783h 1 respectively at different concentration such as low, medium, high concentration. No saturation phenomenon occurred and at the same time, ka was kept unchanged. CONCLUSION the absorption of simvastatin compilies with the passive transport mechanism and first order kinetics. The results indicates that simvastatin can be prepared and processed into sustained release dosage form for once a day.