摘要
目的:研究牡荆素在大鼠体内的药代动力学。方法:大鼠静注牡荆素后,采用HPLC法测定大鼠血浆、组织、粪便、胆汁及尿液中的牡荆素。色谱系统:C18柱(250mm×4.6mm,5μm),流动相为乙腈-10mmol/L磷酸氢二钾溶液(22∶78,含10mmol/L四丁基溴化铵,pH7.8),检测波长340nm。结果:血浆样品中,牡荆素的线性范围为0.2～25.0μg/mL(r=0.9996);各浓度的提取回收率均大于80%;最低定量限为0.2μg/mL。牡荆素在大鼠体内的平均t1/2约为25min。AUC与给药剂量呈现良好的线性相关性。静脉注射给药后牡荆素广泛分布于各组织,其中肝和肾组织中浓度最高。牡荆素主要通过肝脏和肾脏代谢排泄,在大鼠尿、粪和胆汁中的总排泄量约为给药量的30%。牡荆素平均血浆蛋白结合率为64.8%。结论:静注给药后,牡荆素迅速从大鼠体内消除,并可在体内广泛分布,有约30%的以原型形式从胆汁和尿液排泄。
Aim： To study the pharmacokinetics of vitexin in rats. Methods： Following iv administration to rats, HPLC was used to determine vitexin concentration in plasma, tissues, bile, feces and urine. The analysis was carried out on a C18 column（250 mm × 4.6 mm,5 μm）at 340 nm. The mobile phase consisted of acetonitrile-10 mmol/L dipotassium hydrogen phosphate（22：78）containing 10 mmol/L tetrabutyl ammonium bromide（pH 7.8）. Results：The linear range of ritexin in plasma was 0.2 - 25.0μg/mL（ r = 0.999 6）and quantitative limit of vitexin was 0.2 μg/mL with the recovery more than 80%. Mean elimination half life time（ t1/2）of vitexin in rats plasma was about 25 min. The relationship between dose and AUC showed excellent linearity, suggesting that there was linear disposition of vitexin in rats in the dose range. Following iv administration to rats, vitexin mainly distributed in liver and kidney. Vitexin was mainly excreted through bile, and urine, and the total percentage of the corresponding cumulative excretion was found to be nearly 30% in the bile, urine and feces. Moreover, the mean plasma protein bounding ratio of vitexin was 64.8%. Conclusion：Vitexin can be rapidly eliminated from the rat plasma, extensively distributed in rats after iv administration. Following iv administration, vitexin is mainly excreted in the bile and urine in 30% parent forms.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2007年第1期65-68,共4页
Journal of China Pharmaceutical University
基金
国家中医药管理局基金资助项目(No.02-032p32)~~
