中文摘要：

目的建立微透析取样技术结合RP-HPLC分析方法同步研究附子中主要有效成分乌头碱、次乌头碱和新乌头碱在大鼠体内的药动学过程。方法大鼠十二指肠给予附子提取物1055mg·kg^-1,颈静脉微透析采样,RP-HPLC测定透析液中乌头碱、次乌头碱和新乌头碱的含量,以回收率校正实际药物浓度,并用3P97程序计算药动学参数。结果透析液中乌头碱、次乌头碱和新乌头碱分别在0.0112～0.56mg·L^-1（r=0.9999）,0.0106～0.53mg·L^-1（r=0.9997）和0.0114～0.57mg·L^-1（r=0.9998）内线性关系良好,方法回收率在93.12%以上。乌头碱、次乌头碱和新乌头碱的血药浓度-时间曲线均符合开放式二室模型。结论本实验建立的方法简便,专属灵敏,可用于附子提取物中乌头类生物碱的药动学研究。

英文摘要：

OBJECTIVE To investigate pharmacokinetics of aconitine, hypaconitine and mesaconitine, three main effective components of Fuzi in rats using microdialysis sampling technique coupled with RP-HPLC method. METHODS After a single duodenum administration of Fuzi extract of 1 055 mg·kg^-1 to SD rats, microdialysates from jugular vein were collected. Aconitine, hypaconitine and mesaconitine in dialysates were assayed by RP-HPLC simultaneously, and reverse microdialysis was used for recovery calibration to quantify the ＂true＂ concentration. The pharmacokinetic parameters were caculated by 3P97 pharmacokinetic program. RESULTS The linear range was 0.011 2 0.56 mg·L^-1 （r=0.999 9）, 0.010 6-0.53 mg·L^-1 （r=0.999 7） and 0.011 4-0.57 mg·L^-1（r=0.999 8） for aconitine, hypaconitine and mesaconitine in dialysate, respectively. The recovery of assay was above 93.12%.The concentration-time curves CONCLUSION The method in the extract of Fuzi. of aconitine, hypaconitine and is simple, specific and sensitive, mesaconitine were fitted to the two-compartment open model. and suitable for pharmacokinetic study on aconitine-type alkaloids