醋蒸对南五味子木脂素类成分在大鼠体内药代动力学的影响

目的考察醋蒸对南五味子木脂素类化学成分在大鼠体内代谢规律的影响。方法给大鼠灌服相同原药材量的醋蒸前后南五味子提取物,于不同时间点采集血浆样本,采用高效液相色谱法测定不同时间点大鼠血浆样品中五味子酯甲和五味子甲素含量,绘制血药浓度-时间曲线,采用DAS2.0药代动力学分析软件计算药代动力学参数。结果五味子酯甲和五味子甲素在大鼠体内药代动力学模型均符合单房室模型。南五味子醋蒸前后样品中五味子酯甲血药浓度分别在给药后(4.250±1.523)、(5.750±1.784)h达到峰值,实测Cmax分别为(2.197±0.995)、(2.815±0.842)μg/mL,T1/2分别为(2.654±0.377)、(3.504±0.856)h;南五味子醋蒸前后样品中五味子甲素血药浓度分别在给药后(3.250±1.836)、(4.250±1.471)h达到峰值,实测Cmax分别为(1.922±0.773)、(2.307±0.602)μg/mL,T1/2分别为(2.111±1.185)、(3.242±2.126)h。南五味子醋蒸前后在大鼠体内主要药代动力学参数存在差异。结论从五味子酯甲和五味子甲素的药代动力学参数分析,醋制使南五味子木脂素类成分大鼠体内代谢明显减慢。

Effects of Steaming Orange Magnoliavine Fruit with Vinegar on Pharmacokinetics in Rats

Objective To study the effects of steaming Orange Magnoliavine Fruit with vinegar on the lignan metabolism in rats.Methods The rats were fed with same amount of extracts：Orange Magnoliavine Fruit before and after steaming processing with vinegar. Then plasma samples were collected at different times and determined contents of schisantherin A and deoxyschizandrin by HPLC to draw drug concentration in blood-time curve. The pharmacokinetic parameters were calculated with DAS2.0 analysis software.Results Pharmacokinetic model of schisantherin A and deoxyschizandrin in rats accorded with one compartment model. Plasma concentration in rats under the condition of Orange Magnoliavine Fruit samples before and after steaming processing with vinegar was：Tmax of schisantherin A was determined with （4.250±1.523）, （5.750±1.784）h respectively, Cmax with （2.197±0.995）, （2.815±0.842）μg/mL respectively, T1/2 with （2.654±0.377）, （3.504±0.856）h respectively. Tmax of deoxyschizandrin was determined with （3.250±1.836）, （4.250±1.471）h respectively, Cmax with （1.922±0.773）, （2.307±0.602）μg/mL, T1/2 with （2.111±1.185）, （3.242±2.126）h. Orange Magnoliavine Fruit before and after steaming processing with vinegar exhibited differences in pharmacokinetic parameters in rats.Conclusion The pharmacokinetic parameters of schisantherin A and deoxyschizandrin showed that the steaming processing with vinegar on Orange Magnoliavine Fruit can slow down lignan metabolism in vivo.