【摘要】 目的考察川芎嗪在不同浓度甘油中的大鼠体内药动学参数和生物利用度。方法采用HPLC检测大鼠灌胃给予川芎嗪甘油溶液和川芎嗪水混悬液后血药浓度的变化。计算其房室模型药动学参数,根据药-时曲线下面积AUC(0～∞)和给药剂量,分别计算其绝对生物利用度。结果川芎嗪血浆样品在0.1919～30.6977μg.mL-1范围内线性关系良好,最低检测限为25.1ng.mL-1,高、中、低三个浓度的提取回收率分别为107%、109%、103%。大鼠灌胃给予20%、40%、60%、80%、100%川芎嗪甘油溶液及川芎嗪水混悬液后,川芎嗪的达峰时间分别为45min、15min、15min、30min、15min、30min,AUC(0～∞)分别为(110.23±15.94)、(101.37±11.79)、(343.72±12.06)、(468.86±63.40)、(411.64±83.11)、(173.03±0.81)μg.min.mL-1,其绝对生物利用度分别为23.02%、21.22%、71.94%、98.12%、86.15%、36.21%。结论 60%、80%、100%的甘油能显著提高川芎嗪的绝对生物利用度。更多还原

【Abstract】 OBJECTIVE To investigate the pharmacokinetics and bioavailability of ligustrazine in different concentrations of glycerol in rats.METHODS Pharmacokinetics study was conducted by determinating the serum concentrations of ligustrazine and calculating the pharmacokinetics parameters after i.g.administration ligustrazine glycerol solution and ligustrazine water suspension.RESULTS The calibration curve of ligustrazine was linear at a range of 0.1919~30.6977μg·mL-1.The lowest detectable limit was 25.1ng·mL-1.The extracted recoveries were 107%,109%,103% at high,middle and low concentrations,respectively.Rats were orally administered the 20%,40%,60%,80%,100% ligustrazine glycerol solution and ligustrazine water suspension,respectively.The peak time of ligustrazine were 45min,15min,15min,30min,15min,30min.AUC(0~∞)were(110.23±15.94),(101.37±11.79),(343.72±12.06),(468.86±63.40),(411.64±83.11),(173.03±0.81)μg·min·mL-1,respectively.The absolute bioavailability were 23.02%,21.22%,71.94%,98.12%,86.15%,36.21%,respectively.CONCLUSION 60%,80%,100% glycerol can significantly improve absolute bioavailability of Ligustrazine.更多还原