目的 探究紫辛鼻鼽顆粒主要入血成分木蘭花堿、水合氧化前胡素、木蘭脂素、五味子醇甲在大鼠體內(nèi)的藥動學(xué)特征。方法 采用UPLC-MS/MS技術(shù)，測定SD大鼠單次ig給予紫辛鼻鼽顆粒2.52、5.04、10.08 g·kg^-1，以及多次ig給予5.04 g·kg^-1后，上述4個(gè)成分在不同時(shí)間點(diǎn)的血藥濃度；利用DAS3.2.8軟件計(jì)算藥動學(xué)參數(shù)，分析其藥動學(xué)行為。結(jié)果 建立的UPLC-MS/MS分析方法可同時(shí)測定大鼠血漿中4種指標(biāo)成分，該方法專屬性、準(zhǔn)確度、精密度、提取回收率、基質(zhì)效應(yīng)和穩(wěn)定性結(jié)果均符合生物樣本定量分析要求。大鼠單次給藥后，水合氧化前胡素、木蘭脂素和五味子醇甲的藥時(shí)曲線下面積（AUC_0～t）與給藥劑量呈良好的線性關(guān)系（R²＞0.9）；與單次給藥相比，多次給藥后4個(gè)成分的藥動學(xué)行為基本一致，AUC_0～t和半衰期（t_1/2）均無顯著性差異。結(jié)論 大鼠單次ig紫辛鼻鼽顆粒后，水合氧化前胡素、木蘭脂素和五味子醇甲在體內(nèi)呈線性動力學(xué)特征，木蘭花堿則表現(xiàn)為非線性動力學(xué)過程；多次給藥后各成分在體內(nèi)無蓄積現(xiàn)象。

Objective To investigate the pharmacokinetic characteristics of the main blood components of Zixin Biqiu Granules, namely magnoflorine, hydrated oxypeucedanin, magnolin, and schisandrin, in rats. Methods UPLC-MS/MS technology was used to determine the blood concentrations of the four components at different time points after single oral administration of 2.52, 5.04, and 10.08 g·kg^-1 and multiple oral administration of 5.04 g·kg^-1 of the granules to SD rats. The pharmacokinetic parameters were calculated using DAS3.2.8 software, and their pharmacokinetic behaviors were analyzed. Results The established UPLC-MS/MS analytical method could simultaneously determine the four indicator components in plasma. The specificity, accuracy, precision, extraction recovery, matrix effect, and stability results of the method all met the requirements for quantitative analysis of biological samples. After single administration to rats, the area under the plasma concentration-time curve (AUC_0~t) of hydrated oxypeucedanin, magnolin, and schisandrin showed a good linear relationship with the dose (R² > 0.9). Compared with single administration, the pharmacokinetic behaviors of the four components after multiple administrations were basically the same, and there were no significant differences in AUC_0~t and half-life (t_1/2). Conclusion After single oral administration of Zixing Biqiu Granules to rats, hydrated oxypeucedanin, magnolin, and schisandrin showed linear pharmacokinetic characteristics in vivo, while magnoflorine exhibited nonlinear pharmacokinetic processes. There was no accumulation of the components in vivo after multiple administrations.

R969.1

國家工信部重點(diǎn)創(chuàng)新中藥/新型天然藥物項(xiàng)目（2440STCZB2614）