山楂消脂胶囊超微粉与细粉中大黄酸在大鼠体内药代动力学差异研究.docVIP

山楂消脂胶囊超微粉与细粉中大黄酸在大鼠体内药代动力学差异研究 　　[摘要] 目的 比较大鼠灌胃山楂消脂胶囊超微粉和细粉后大黄酸的药代动力学特征差异。 方法 大鼠分别灌胃给予超微粉混悬液或细粉混悬液，用高效液相色谱法测定大黄酸的血药浓度变化。色谱柱为Uranus C18（250 mm× 4.6 mm，5 μm），流动相为甲醇-0.1%磷酸水溶液（85∶15），流速为1 mL/min，检测波长为254 nm，血药浓度-时间数据采用PKSolver2.0药代动力学软件进行分析。 结果 大黄酸血药浓度在0.16～40.00 μg/mL线性关系良好。大鼠灌胃给予山楂消脂胶囊超微粉混悬液及细粉混悬液后大黄酸血浆-时间曲线均符合二房室模型，山楂消脂胶囊超微粉及山楂消脂胶囊细粉的主要药动学参数AUC分别为（4.08±4.96）μg/（mL?h）和（0.74±0.06）μg/（mL?h）（P 0.05），药峰浓度（Cmax）分别为（0.79±0.15）μg/mL和（0.17±0.02）μg/mL（P 0.05）。 结论 超微粉碎能使大黄酸在大鼠体内的吸收更完全，提高生物利用度。 　　[关键词] 山楂消脂胶囊；超微粉；细粉；大黄酸；药代动力学 　　[中图分类号] R284.1 [文献标识码] A [文章编号] 1673-7210（2017）11（a）-0027-04 　　Pharmacokinetic study of rhein from the ultra-micro and fine powder of Shanzha Xiaozhi Capsules in rats 　　LIANG Xiuqing1 SHEN Xiao2 LI Zihong1 LI Huaiguo1 LIU Dongwen1 WANG Lisheng2 　　1.Preparation Center， Foshan Hospital of TCM， Guangdong Province， Foshan 528000， China； 2.College of Traditional Chinese Medicine， Guangzhou University of Chinese Medicine， Guangdong Province， Guangzhou 510006， China 　　[Abstract] Objective To compare the differences of pharmacokinetic characteristics of rhein after rats received ultra-micro and fine powder of Shanzha Xiaozhi Capsules by gavage. Methods The experimental rats were given suspensions of the ultra-micro and fine powder of Shanzha Xiaozhi Capsules. The plasma concentration of rhein in rats was measured by high performance liquid chromatography. Uranus C18 （250 mm× 4.6 mm， 5 μm） was used as the analytical column. The mobile phase was methanol-water-0.1% phosphoric acid （85∶15）， the wavelength of detection was set at 254 nm， and the flow rate was 1.0 mL/min. Serum concentration-time data was processed by pharmacokinetics software PKSolver 2.0. Results The linear range of rhein was from 0.16 to 40.00 μg/mL. The concentration-time curves of rhein in rats fitted well into two compartment model. The main pharmacokinetic parameters of the AUC of rhein from the ultra-micro and fine powder of Shanzha Xiaozhi Capsules were （4.08±4.96） μg/（mL?h） and （0