| 摘要: |
| 目的 建立HPLC法测定吴茱萸碱新型纳米乳（evodiamine novel nano emulsion，ENNE）中吴茱萸碱（evodiamine，EVO）在大鼠体内的血药浓度，研究ENNE在大鼠体内的药代动力学行为，比较ENNE与EVO的生物等效性。方法 12只SD大鼠平均分为两组，分别灌胃给予ENNE（相当于EVO 100 mg/kg）与EVO（100 mg/kg），采用HPLC法测定5 min、10 min、15 min、30 min、45 min、1 h、2 h、5 h、8 h、12 h、24 h、48 h、72 h大鼠体内EVO的血药浓度。HPLC法色谱条件：流动相为甲醇-0.1%甲酸水溶液（66：34，体积比），流速为1.0 mL/min，进样体积为100 μL，检测波长为225 nm。绘制血药浓度-时间曲线，用DAS 2.1.1软件计算主要药代动力学参数与生物等效性。结果 建立的HPLC法线性关系良好，准确度与精密度符合分析方法学要求。ENNE与EVO的AUC0-∞分别为（8 248.88±69.92）μg·h·L-1、（884.82±83.52）μg·h·L-1，半衰期分别为（1.70±0.60）h、（1.05±0.45）h。ENNE的相对生物利用度约为EVO的9倍，半衰期约为EVO的1.62倍，ENNE与EVO不具有生物等效性。结论 ENNE较EVO更能促进药物的吸收，提高生物利用度；ENNE与EVO不具生物等效性。 |
| 关键词: 吴茱萸碱 纳米乳 药代动力学 肠吸收 生物利用度 半衰期 |
| DOI：10.16781/j.0258-879x.2016.10.1256 |
| 投稿时间：2016-01-16修订日期：2016-03-19 |
| 基金项目: |
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| Pharmacokinetics and bioequivalence of evodiamine novel nano emulsion in rats |
| LEI Ting-ting,ZHANG Jing-qing,CHEN Jing,ZHANG Yan-fang,ZHAO Hua* |
(Medicine Engineering Research Center in University, Chongqing Medical University, Chongqing 400016, China
*Corresponding author) |
| Abstract: |
| Objective To establish an HPLC approach for determining the plasma drug concentration of evodiamine (EVO) in evodiamine novel nano emulsion (ENNE) in rats, and to investigate the pharmacokinetics and bioequivalence of ENNE in rats. Methods Twelve SD rats were evenly randomized into two groups and were administered intragastrically with ENNE (containing EVO 100 mg/kg) or EVO (100 mg/kg). The plasma drug concentrations of EVO were measured at 5 min, 10 min, 15 min, 30 min, 45 min, 1 h, 2 h,5 h, 8 h, 12 h, 24 h, 48 h and 72 h after administration of ENNE or EVO by HPLC. The chromatographic conditions were as following:the mobile phase was methanol and 0.1% of formic acid-water solution (66:34,V/V), the flow rate was 1 mL/min, the injection volume was 100 μL, and the detection wavelength was 225 nm. The concentration-time curve was drawn by excel software, and the main pharmacokinetic parameters and bioequivalence were calculated by DAS 2.1.1 software. Results The established method was fast, accurate, and had good linear correlation. The AUC0-∞ of ENNE and EVO were (8 248.88±69.92) μg·h·L-1 and (884.82±83.52) μg·h·L-1, and the t1/2 of ENNE and EVO were (1.70±0.60) h and (1.05±0.45) h, respectively. The AUC0-∞ of ENNE was 9 times that of EVO, and the t1/2 of ENNE was 1.62 times that of EVO.ENNE and EVO were not bioequivalent. Conclusion Bioavailability and absorption of ENNE are higher than EVO, and ENNE and EVO are not bioequivalent. |
| Key words: evodiamine nano emulsion pharmacokinetics intestinal absorption biological availability half-life |
