萝芙木中育亨宾大鼠体内药物动力学Pharmacokinetics of yohimbine from Rauvolfia verticillata in rats in vivo
王曦,王淼,申长慧,王加,赵春杰
WANG Xi,WANG Miao,SHEN Chang-hui,WANG Jia,ZHAO Chun-jie(School of Pharmacy
摘要(Abstract)：
目的建立育亨宾在大鼠体内的高效液相色谱测定方法,测定萝芙木中育亨宾在静脉注射后大鼠体内的药物动力学行为。方法采用大连中汇达Hypersil-C18(250 mm×4.6 mm,5μm)色谱柱,以甲醇-体积分数为0.05%的三乙胺水溶液(体积比为75:25)为流动相,流速为1.0 mL.min-1,检测波长为280 nm。大鼠静脉注射育亨宾1 mg.kg-1后,于不同时间点眼眶采血,HPLC法测定其血药浓度,经DAS2.1.1版药动学软件处理得到药动学参数。结果大鼠血浆中育亨宾的线性范围为0.10～3.00 mg.L-1(r=0.995 2),定量下限为0.10 mg.L-1。tmax为0.083 h,ρmax为(2.095±0.302)mg.L-1,AUC0-t为(2.423±0.417)g.h.L-1,AUC0-∞为(2.634±0.412)g.h.L-1。Cl为(0.389±0.072)L.h-.1kg-1。结论建立的大鼠血浆中育亨宾含量的HPLC测定方法适合萝芙木中育亨宾大鼠体内的药物动力学研究;育亨宾静脉注射后消除较快。
Objective To establish an HPLC method for the determination of yohimbine in rat plasma and study the pharmacokinetics of yohimbine from Rauvolfia verticillata in rats.Methods A Zhonghuida Hypersil-C18(250 mm×4.6 mm,5 μm)column was adopted,the mobile phase was a mixture of methanol and 0.05%(w)triethylamine in water(V∶ V=75∶ 25)at the flow rate of 1.0 mL · min-1 and the UV detector was operated at 280 nm.After intravenous injection of yohimbine(1 mg · kg-1),take blood from orbit at different time points,the yohimbine concentrations in rat plasma were detected by HPLC.The pharmacokinetic parameters were calculated by DAS 2.1.1 program.Results In rat plasma,a good linearity between peak area ratio of yohimbine to the internal standard and the concentration was found in the range of 0.10-3.00 mg · L-1(r=0.995 2).The limit of test was 0.10 mg · L-1.The plasma yohimbine concentration-time curve could be evaluated by the two compartment mode.tmax,ρmax,AUC0-t,AUC0-∞ and Cl were 0.083 h,(2.095±0.302)mg · L-1,(2.423±0.417)g · h · L-1,(2.634±0.412)and(0.389±0.072)L · h-1 · kg-1,respectively.Conclusions The developed HPLC method for the pharmacokinetic study of yohimbine in rats after intravenous injection is precise and specific.It′s suitable for the pharmacokinetic study of yohimbine from Rauvolfia verticillata in rats in vivo.Yohimbine eliminates fast after intravenous injection.
关键词(KeyWords)：
高效液相色谱;萝芙木;育亨宾;药物动力学
HPLC;Rauvolfia verticillata;yohimbine;pharmacokinetics
基金项目(Foundation):
作者(Author):
王曦,王淼,申长慧,王加,赵春杰
WANG Xi,WANG Miao,SHEN Chang-hui,WANG Jia,ZHAO Chun-jie(School of Pharmacy
DOI: 10.14066/j.cnki.cn21-1349/r.2012.12.010
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