目的研究牡荆素鼠李糖苷(RHV)的大鼠在体肠吸收动力学特征。方法采用HPLC法测定RHV在肠循环液中的药物浓度;采用UV法测定肠循环液中酚红浓度;以大鼠原位灌注模型考查RHV的肠吸收动力学情况。结果RHV浓度为20、10、5μg·ml^-1的吸收速率常数(Ka)分别为0.0416、0.0478、0.0312h^-1;肠循环液pH4、6、8时RHV的‰分别为0.0253、0.0478、0.0588h^-1;RHV在十二指肠、空肠、回肠和结肠时的Ka分别为0.0479、0.0308、0.0322、0.0305h^-1。结论RHV浓度对RHV的Ka无显著性影响;在pH4—8时,随肠循环液pH的增大,RHV的肠增加;RHV在大鼠十二指肠、空肠、回肠和结肠的吸收无显著性差异(P〉0.05);RHV在大鼠肠道的吸收呈一级动力学过程,吸收机制为被动扩散。
OBJECTIVE To determine the intestinal absorption characters of rhamnosylvitexin (RHV) in rats. METHODS The concentration of RHV in the intestine perfusate was determined by HPLC. The concentration of phenolsulfonphthalein in the intestine perfusate was determined by UV. The absorption kinetics were obtained by the in situ perfusion method in rats. RESULTS The absorption rate constants (Ka) of RHV were 0. 0416,0. 0478,0. 0312 h^-1 at the concentration of 20,10,5 μg·ml^-1 ,respectively; Ka of RHV were 0. 0253,0. 0478,0. 0588 h^-1 at the pH of 4,6,8 ,respectively; Ka of RHV were 0. 0479,0. 0308,0. 0322,0. 0305 h^-1 at duodenum,jejunum,ileum and colon, respectively. CONCLUSION Concentration of RHV has no significant effect on its absorption kinetics. The absorption rate of RHV increases with the increasing of pH value of the perfusate in the range of pH4 - 8. There is no significant difference between the Ka of RHV at duodenum, jejunum, ileum and colon. The intestinal absorption of RHV is a first -order process with the passive diffusion mechanism.