党参超微粉与细粉在大鼠体内的药动学比较研究

Comparative pharmacokinetics of ultramicro-powder and fine powder of Radix Codonopsis in rats

目的:对党参超微粉与细粉中的有效成分党参炔苷在大鼠体内的药动学进行比较。方法:采用高效液相质谱(HPLC)法分别测定灌服两种样品的大鼠体内党参炔苷的血药浓度,通过DAS 2.0药动学软件处理数据,比较党参超微粉及其细粉在大鼠体内的药动学参数和相对生物利用度。结果:党参炔苷在大鼠体内的血药浓度-时间数据符合单室模型;Cmax分别为1.408,1.932μg·mL^(-1);tmax分别为1,1.5 h;t1/2分别为0.243,0.674 h;V分别为34.701,50.745 L;CL分别为5.281,3.779 L·h^(-1)。党参超微粉相对于细粉,其生物利用度提高了39.7%。结论:党参经超微粉碎后可促进其党参炔苷在大鼠体内的吸收,提高生物利用度。

OBJECTIVE To compare pharmacokinetics of lobetyolin in ultramicro-powder and fine powder of Radix Codonopsis in rats.METHODS Plasma concentration of lobetyolin was determined by HPLC method after Radix Codonopsis were gavaged to rats.Pharmacokinetic parameters were analyzed using a DAS 2.0pharmacokinetic software package.The difference was then compared between ultramicro-powder and fine power of Radix Codonopsis and relative bioavailability was calculated.RESULTS Plasma concentration-time data of lobetyolin were both fitted to single compartment model.Cmaxvalues were separately 1.408μg·mL^-1 and 1.932μg·mL^-1;tmax1 h and 1.5 h;t1/20.243 h and 0.674 h;V 34.701 L and 50.745 L;and CL5.281 L·h^-1 and 3.779 L·h^-1.The relative bioavailability of lobetyolin in ultramicro-powder to fine podwer was increased by39.7%.CONCLUSION Ultramicro-powder can promote absorption of active ingredients compared to fine powder of Radix Codonopsis,and improve bioavailability of lobetyolin in rats.