淫羊藿苷单体及淫羊藿总黄酮提取物大鼠药动学特征比较  

Comparison of the pharmacokinetic characteristics of icariin and icarisideⅡafter administration of icariin monomer and Epimedium flavonoids in Wistar rats

作　　者：刘晓燕[1] 王本杰[1] 魏春敏[1] 袁桂艳[1] 张蕊[1] 郭瑞臣[1] 

机构地区：[1]山东大学齐鲁医院临床药理研究所,山东济南250012

出　　处：《中国医院药学杂志》2011年第22期1858-1863,共6页Chinese Journal of Hospital Pharmacy

摘　　要：目的:进行大鼠灌胃淫羊藿苷单体及淫羊藿总黄酮提取物后大鼠淫羊藿苷和淫羊藿次苷Ⅱ的药动学特征比较研究。方法:16只大鼠随机分为2组,分别给予相同剂量的淫羊藿苷单体及淫羊藿总黄酮提取物(以淫羊藿苷计),留取血浆样本,采用液相-串联质谱法(HPLC-MS/MS)检测淫羊藿苷及淫羊藿次苷Ⅱ药物浓度,采用非房室模型药动学程序计算淫羊藿苷及淫羊藿次苷Ⅱ药动学参数,评价淫羊藿苷单体及淫羊藿总黄酮提取物大鼠药动学差异。结果:大鼠灌胃相同剂量(50 mg.kg-1,以淫羊藿苷计)淫羊藿苷单体及淫羊藿总黄酮提取物后淫羊藿苷和淫羊藿次苷Ⅱ的药时曲线呈双峰现象。淫羊藿苷单体组和淫羊藿总黄酮提取物组大鼠淫羊藿苷的主要药动学参数分别为t1/2(3.6±1.1)h和(6.0±3.4)h,tmax(1.0±0.7)h和(1.2±1.1)h,Cmax(21.0±9.1)ng.mL-1和(14.9±4.5)ng.mL-1,AUC0-12(78.5±42.6)ng.mL-1.h和(42.5±13.8)ng.mL-1.h,AUC0-∞(87.0±45.4)ng.mL-1.h和(51.2±13.0)ng.mL-1.h。淫羊藿次苷Ⅱ的主要药动学参数分别为t1/2(3.0±1.4)h和(17.2±10.2)h,tmax(3.9±2.3)h和(0.9±0.5)h,Cmax(20.9±8.6)ng.mL-1和(5.4±2.4)ng.mL-1,AUC0-12(87.1±24.8)ng.mL-1.h和(18.8±10.2)ng.mL-1.h,AUC0-∞(96.3±22.9)ng.mL-1.h和(35.2±8.4)ng.mL-1.h。结论:大鼠灌胃淫羊藿苷单体和淫羊藿总黄酮提取物后,单体组大鼠淫羊藿苷及淫羊藿次苷Ⅱ血药浓度均高于总黄酮组,经统计学分析二者主要药动学参数具有显著差异。OBJECrlVE To compare the pharmacokinetics of icariin and icariside 11 in Wistar rats after administration of icariin monomer and Epimedium flavonoids. METHODS 16 Wistar rats were divided into two groups randomly and received an intragastric administration of 50 mg·kg^-1icariin monomer （5 mL·kg^-1 ） and 0. 2 g Epimedium flavonoids （containing 50 mg icariin）kg^-1 body weight, respectively. The plasma samples were collected as scheduled, and icariin and icariside Ⅱ were analyzed by HPLC-MS/MS. The pharmacokinetic parameters of icariin and icariside Ⅱ were calculated and evaluated by non-compartment model. RFNULTS The plasma concentration of icariin and icariside Ⅱ after administration of icariin monomer were all higher than that after Epirnedium flavonoids. The main parameters of icariin after icariin monomer and Epirnedium flavonoids were shown as follows：t1/2 （3.6 ± 1.1）h and （6. 0 ±3.4）h,tmax（1.0 ± 0. 7）h and （1.2 ± 1.1）h,Cmax,（21.0 ± 9. 1）ng·mL^-1and （14. 9 ＋4. 5）ng·mL^-1 , AUG0-12 （78. 5 ± 42. 6）ng·mL^-1 .h and （42. 5±13.8） ng·mL^-1· h, AUC0-∞ （87. 0 ± 45.4） ng·mL^-1·h and （51.2 ± 13. 0） ng·mL^-1·h. The main parameters of ieariside Ⅱ after ieariin monomer and Epimedium flavonoids were shown as follows： t1/2 （3. 0 ± 1.4）h and （17. 2 ± 10. 2）h, tmax （3. 9 ± 2. 3）h and （0. 9 ±0. 5）h, Cmax. （20. 9 ± 8. 6）ng·mL^-1 and （5. 4 ±2. 4）ng ·mL^-1 , AUG0-12 （87. 1 ± 24. 8）ng·mL^-1 ·h and （18. 8 ± 10. 2）ng·mL^-1 .h,AUC0-∞ （96. 3± 22. 9） ng·mL^-1 .h and （35.2±8.4） ng·mL^-1. k CONCLUSION The plasma concentration of icariin and icarisidel]after administration of icariin monomer were all higher than that after Epirnedium flavonoids. Statistical analysis of main pharmacokinetic parameters of icariin showed that AUC0-2 and AUG0-∞ have statistical significance, while all of the main pharmacokinetic parameters of icarisideⅡhave statistical significane.

关 键 词：淫羊藿苷 淫羊藿次苷Ⅱ 淫羊藿总黄酮提取物 药动学 液相-串联质谱法 

分 类 号：R969.1[医药卫生—药理学]