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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 a method for the determination of yohimbine in rats by HPLC and to determine the pharmacokinetics of yohimbine in rats after intravenous injection. Methods The chromatographic column was packed on a Hypersil-C18 (250 mm × 4.6 mm, 5 μm) column with a mobile phase of methanol-methanol 0.05% triethylamine (volume ratio 75:25) at a flow rate of 1.0 mL .min-1, the detection wavelength is 280 nm. Rats were intravenously injected with yohimbine 1 mg.kg-1, at different time points orbital blood sampling, HPLC determination of plasma concentration, pharmacokinetic software by DAS2.1.1 pharmacokinetic parameters. Results The linear range of yohimbine in rat plasma was 0.10-3.00 mg.L-1 (r = 0.995 2) and the lower limit of quantitation was 0.10 mg.L-1. tmax was 0.083 h, pmax was (2.095 ± 0.302) mg.L-1, AUC0-t was (2.423 ± 0.417) g.h.L-1 and AUC0-∞ was (2.634 ± 0.412) g.h.L-1. Cl was (0.389 ± 0.072) L.h-1kg-1. Conclusion The established method for the determination of yohimbine in rat plasma is suitable for the pharmacokinetics of yopecufum in yohimban rats. The yohimbine is rapidly eliminated after intravenous injection.