外感咳嗽方中白花前胡甲素的大鼠血浆药物代谢动力学研究  

Rat Plasma Pharmacokinetic Research of Praeruptorin A in WaiGan KeSou Formula

作　　者：何根祥 伍时惠 HE Gen-xiang;WU Shi-hui(Foshan Sanshui district maternal and children health hospital,Foshang 528100,China;Guangdong Second Provincial Hospital of T.C.M.(Guangdong Province Engineering Technology Research Institute of T.C.M.),Guangzhou 510095,China)

机构地区：[1]佛山市三水区妇幼保健院,广东佛山528100 [2]广东省第二中医院(广东省中医药工程技术研究院),广东广州510095

出　　处：《海峡药学》2021年第8期19-22,共4页Strait Pharmaceutical Journal

摘　　要：目的通过测定外感咳嗽方君药前胡指标性成分的药代动力学特征,研究生物体对该方的吸收和利用。方法使用超高效液相色谱-质谱联用仪,色谱柱为Waters ACQUITY BEH C 18(100×2.1 mm,1.7μm粒径),流动相为0.1%甲酸(A)-乙腈(B),梯度洗脱程序为:0~0.5 min,5%~5%B;0.5~1.0 min,5%~90%B;1.0~2.5 min,90%~90%B;2.5~3.0 min,90%~5%B;流速0.3 mL·min^(-1),测定指标为白花前胡甲素,内标为补骨脂素;实验动物为大鼠,服用临床剂量外感咳嗽方汤剂后,在各时间点取血,血浆经前处理后测定血药浓度并绘制血药浓度-时间曲线。结果给药后24 h内,白花前胡甲素的峰浓度C max=(172.697±17.254)ng·mL^(-1),达峰时间T max=1.50 h,消除半衰期T 1/2=1.02 h,平均驻留时间MRT=3.42 h,药-时曲线下面积AUC 0-τ=(504.866±50.317)h·ng·mL^(-1),AUC 0-∞=(514.401±36.950)h·ng·mL^(-1)。结论白花前胡甲素在大鼠体内生物利用度较好,能够发挥其药理活性。OBJECTIVE Through determination of pharmacokinetic parameters of Praeruptorin A-the index compound of Radix Peucedani,the monarch drug of WaiGan KeSou Formula,to investigate its absorption and exploitation by the body.METHODS An ultra-high performance liquid chromatography-tandem mass spectrometry method was established,the column used was Waters ACQUITY BEH C 18(100×2.1 mm,particle size 1.7μm),the mobile phase contained 0.1%formic acid(A)and acetonitrile(B),the gradient program was:0-0.5 min,5%-5%B;0.5-1.0 min,5%-90%B;1.0-2.5 min,90%-90%B;2.5-3.0 min,90%-5%B;the flowrate was 0.3 mL·min^(-1),the component being analyzed was Praeruptorin A,and Psoralen as internal standard;Rats were fed with clinical dosage of WaiGan KeSou Formula decoction,and blood was taken in different time points,the obtained plasma samples were pre-treated,analyzed,and the plasma concentration-time curve was drawn according to the result.RESULTS In 24 hours after administration,the peak concentration C max of Praeruptorin A was(172.697±17.254)ng·mL^(-1),peak time T max was 1.50 h,elimination half-life T 1/2 was 1.02 h,mean retention time MRT=3.42 h,area under the curve was AUC 0-τwas(504.866±50.317)h·ng·mL^(-1),AUC 0-∞was(514.401±36.950)h·ng·mL^(-1).CONCLUSION Praeruptorin A had relatively good bioavailability in the rat body,and was capable of taking therapeutic effects.

关 键 词：外感咳嗽方 白花前胡甲素 药物代谢动力学 

分 类 号：R965[医药卫生—药理学]