异绿原酸A在大鼠体内的生物利用度和药物代谢动力学

发布时间：2018-05-23 09:46

  本文选题：异绿原酸A + 静脉给药　； 参考：《中国实验方剂学杂志》2015年16期

【摘要】：目的:研究异绿原酸A在大鼠体内的生物利用度和药代动力学,为该制剂的临床应用提供参考。方法:建立大鼠血浆中异绿原酸A的HPLC检测,检测波长300 nm,流动相甲醇-0.1%磷酸水(50∶50)。考察大鼠经静脉注射(32 mg·kg-1)与灌胃(90 mg·kg-1)给予异绿原酸A后的血药浓度变化,利用3P97软件计算药动学参数,根据药时曲线下面积AUC0-∞和给药剂量,计算异绿原酸A的绝对生物利用度。结果:异绿原酸A在0.16~110.00 mg·L-1线性良好(R2=0.998);质量浓度分别为0.43,6.88,55.00 mg·L-1的异绿原酸A的提取回收率分别为(89.43±2.84)%,(93.16±3.95)%,(85.91±2.04)%;日内精密度RSD分别为11.8%,4.0%,4.0%,日间精密度RSD分别为6.5%,5.8%,5.8%。大鼠静脉注射和灌胃异绿原酸A后,异绿原酸A在大鼠体内的代谢过程均符合二室模型,消除半衰期分别为(29.49±0.75),(44.48±0.13)min,AUC0-∞分别为(355.40±32.58),(319.91±51.00)mg·min-1·L-1。异绿原酸A在大鼠体内的绝对生物利用度30.71%。结论:异绿原酸A在大鼠体内的过程符合线性动力学过程,且代谢快、半衰期短。
[Abstract]:Aim: to study the bioavailability and pharmacokinetics of Lv Yuan A in rats and to provide reference for its clinical application. Methods: HPLC detection of isophosphate A in rat plasma was established. The detection wavelength was 300nm.The mobile phase consisted of methanol-0.1% phosphoric acid water (50: 50). The changes of plasma concentration of isobaric acid A in rats after intravenous injection of 32 mg kg-1 and intragastric administration of 90 mg kg-1) were investigated. Pharmacokinetic parameters were calculated by 3P97 software. According to the area under the drug time curve, AUC0- 鈭，

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