大鼠血浆中的新藤黄酸HPLC测定及其药代动力学研究  

Determination of Gambogenic acid and its pharmacokinetics in rat plasma by HPLC

作　　者：汪电雷[1,2,3] 张瑞[1] 陶秀华[1] 张弦[1] 陈卫东[1] 王效山[1] 李庆林[1,2,3] 彭代银[1] 

机构地区：[1]安徽中医学院,安徽合肥230031 [2]安徽省中药研究与开发重点实验室,安徽合肥230031 [3]省部共建新安医学教育部重点实验室,安徽合肥230031

出　　处：《中国药理学通报》2012年第8期1164-1167,共4页Chinese Pharmacological Bulletin

基　　金：国家重大新药创制资助项目(No 2009ZX09103-399);国家自然科学基金资助项目(No 81001592);教育部科学技术重点项目(No 210101);安徽高校省级自然科学研究重点项目资助(No KJ2010A210,KJ2012A186)

摘　　要：目的建立测定大鼠血浆中新藤黄酸浓度的HPLC方法,并用于新藤黄酸在大鼠体内的药代动力学研究。方法以藤黄酸为内标,建立大鼠血浆中新藤黄酸的HPLC测定方法。采用该方法测定大鼠单剂量静脉注射1、2、4 mg.kg-1新藤黄酸后不同时间点大鼠血浆中的新藤黄酸的浓度,对其血药浓度-时间采用BABP 3.0软件拟合,计算药动学参数。结果血浆中新藤黄酸在0.07～18.0 mg.L-1浓度范围,其线性关系良好(r=0.999),定量下限为0.07 mg.L-1,提取回收率分别为大于70%,其日内、日间RSD均小于10%。新藤黄酸以1、2和4 mg.kg-1静脉给药后,在大鼠体内的T12分别为(43.61±0.61)、(46.07±2.11)和(46.73±1.14)min,AUC0-t分别为(158.52±6.27)、(211.13±9.33)和(361.37±14.97)min.mg.L-1。结论所建立的HPLC法样品前处理简便、操作简便、能满足新藤黄酸在大鼠体内的药代动力学研究。Aim To develop a HPLC method for the determination of plasma concentration of Gambogenic acid （GNA） and study the pharmacokinetics of GNA in rat plasma. Methods A HPLC method was established for the determination of GNA in rat plasma using gambogic acid as the internal standard. The plasma concentration of GNA in rats was determined by HPLC after intravenous administration of GNA at a dose of 1, 2 and 4 mg · kg- 1, and the pharmacokinetic parame- ters were calculated by BABP 3.0. Results Calibra- tion curve was linear over the range of 0. 07 - 18.00 mg· L-1. The lower limit of quantification was 0.07 mg · L-1. The extraction recoveries were higher than 70%. The intra- and inter-day precision （RSD%）was lower than 10%. This validated method was suc- cessfully applied to a pharmacokinetic study after iv administration of GNA in rats at a dose of 1, 2 and 4 mg · kg-1. The T1/2 was（43.61 ±0.61）,（46. 07 ±2. 11） and （46.73± 1.14） rain, respectively, and the AUC0-t was （158.52 ± 6.27）, （211.13 ± 9.33） and （361,37 ± 14.97） min·mg·L-1, respectively. Conclusion A simple, rapid, accurate and precise HPLC method for the analysis of GNA in rat plasma is successfully developed and validated and successfully applied to a pharmacokinetic study of GNA in rats.

关 键 词：新藤黄酸 大鼠 血药浓度 HPLC 测定 药代动力学 

分 类 号：R332[医药卫生—人体生理学] R282.71[医药卫生—基础医学]