普伐他汀大鼠在体肠吸收动力学

Study on the absorption kinetics of pravastatin in rat small intestine

目的:研究普伐他汀在大鼠小肠的吸收情况。方法:采用大鼠在体小肠回流实验装置,利用HPLC紫外检测的方法测定肠循环液中酚红和普伐他汀的含量。采用XTerra@MS C-18色谱柱(5μm,150mm×2.1 mm.ID),流动相为3.5 mmol/L磷酸二氢钠溶液—乙腈(70:30,用磷酸调至pH 3.0),流速为0.2ml/min;结果:普伐他汀在大鼠小肠全肠段的吸收速率常数和吸收百分率分别为0.110±0.023(h^(-1))和18.21±2.50%。普伐他汀在小肠中吸收量与时间呈线性关系,但吸收速率较低。结论:普伐他汀可以通过增加药物的脂溶性,进而提高药物的生物利用度。

Objective： To explore the absorption ofpravastatin in rats＇ small intestine. Methods： The absorption kinetics and absorption rate constants （ka） were investigated by the in situ perfusing method in rats, and the concentration of Phenol red and pravastatin were determined by HPLC. The chromatography was employed with an XTerra MS C-18 reverse-phase column （5 μm, 150 mm× 2.1 mm.ID）, analytical column and mixture of phosphate buffer solution （3.5 mmol/L NaH2PO4, pH adjusted to 3.0 with phosphoric acid） -acetonitrile （70：30）, the mobile phase with the flow rate of 0.2 ml/min. Results： The absorption rate constants and the uptake rate of pravastatin were 0.110± 0.023 （h^-1） and 18.21 ± 2.50 %, respectively. The linear correlation of the absorption of pravastatin and the time is good, but the absorption rate is low. Conelusion： The bioavailability of pravastatin can be increased by increasing the liposolubility of the drug.