Intestinal absorption characteristics of evodiamine hydroxypropyl-β-cyclodextrin inclusion complex in rats / 第二军医大学学报

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 (7525), 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.