| 摘要: |
| 目的 研究吴茱萸碱（EVO）羟丙基-β-环糊精包合物（EHD）的大鼠在体肠吸收特征。方法 制备EHD并测定其理化性质。将健康雄性SD大鼠随机分为2组，运用单向肠灌流模型对大鼠各肠段EVO的吸收情况进行考察，使用HPLC法测定EVO的含量：Lichrospher C18柱（250 mm×4.6 mm，5 μm），流动相为甲醇：水=75：25（体积比），流速1.0 mL/min，检测波长225 nm，柱温35℃，并对吸收速率常数（Ka）及有效渗透系数（Peff）进行计算。结果 EHD的傅里叶红外扫描图谱中，EVO特征吸收峰减弱；差示扫描量热图谱中，EVO的吸热峰明显减小；EHD的电镜下形态与EVO和羟丙基-β-环糊精的物理混合物明显不同；肠灌流液中EVO的回收率与精密度均符合要求。EHD在十二指肠、空肠、回肠、结肠中的Ka值分别为EVO的9.07、16.22、11.04、28.86倍，差异有统计学意义（P<0.05）；Peff值分别为EVO的2.41、1.52、1.82、1.09倍，在十二指肠处差异有统计学意义（P<0.05），在其他肠段处差异均无统计学意义。结论 EHD能使EVO在大鼠体内的肠吸收得到明显改善。 |
| 关键词: 吴茱萸碱 包合物 高效液相色谱法 在体肠吸收 |
| DOI：10.16781/j.0258-879x.2016.11.1387 |
| 投稿时间：2016-01-25修订日期：2016-06-21 |
| 基金项目:重庆市科委资助项目（csct2015jcyjBX0027）. |
|
| Intestinal absorption characteristics of evodiamine hydroxypropyl-β-cyclodextrin inclusion complex in rats |
| ZHANG Xue,LIU Hong-ming,LEI Ting-ting,DENG Luo-wen,ZHANG Jing-qing |
(Chongqing Medicine Engineering Research Center, Chongqing Medical University, Chongqing 400016, China
*Corresponding author.) |
| Abstract: |
| Objective To study the intestinal absorption characteristics of evodiamine (EVO) hydroxypropyl-β-cyclodextrin inclusion complex (EHD) in rats. Methods EHD was prepared and its physicochemical properties were determined. Healthy male SD rats were randomly divided into two groups. One-way intestinal perfusion rat model was employed to investigate the intestinal absorption of EVO in each segment. The concentrations of the EVO were determined by HPLC (Lichrospher C18 column[250 mm×4.6 mm, 5 μm]), with the mobile phase being methanol-water (75:25), flow rate being 1.0 mL/min, the detection wavelength being set at 225 nm, and the column temperature being 35℃. The absorption rate constants (Ka) and effective permeability coefficients (Peff) were calculated. Results The characteristic endothermal peak of EVO was decreased in the fourier transform infrared spectroscopy of EHD, and differential scanning calorimetry (DSC) of EHD showed that the endothermic peak of EVO was greatly reduced. The morphological character of EHD under electron microscope was obviously different from that of the physical mixture of EVO and hydroxypropyl-β-cyclodextrin. The coefficient of recovery and precision of EVO in the intestinal perfusion liquid met the requirement. The Ka values of EHD in the duodenum, jejunum, ileum, and colon were 9.07, 16.22, 11.04, and 28.86 folds that of the free EVO, respectively, showing significant differences between the two groups (P<0.05). The Peff values of EHD in the duodenum, jejunum, ileum, and colon were 2.41, 1.52, 1.82, and 1.09 folds that of the free EVO, respectively, showing significant difference between the two groups only at the duodenum (P<0.05), not at the jejunum, ileum or colon. Conclusion EHD can significantly improve the intestinal absorption of the EVO in rats. |
| Key words: evodiamine inclusion complex high performance liquid chromatography in situ intestinal absorption |
