Intestinal absorption investigation of ZYS-01 by single pass intestinal perfusion model in situ / 中国药学杂志

ABSTRACT

OBJECTIVE: To study the in situ small intestinal absorption mechanism of ZYS-01 in rats and discuss its absorption mechanism. METHODS: Single pass intestinal perfusion model was established, intestinal perfusate concentration of ZYS-01 was measured by HPLC, using the gravimetric method corrected the perfusate volume, absorptions of different dose groups of ZYS-01 in different segments and the effect of P-glycoprotein(P-gp) inhibitors on the absorption of ZYS-01 were investigated. RESULTS: ZYS-01 was absorpted in the whole small intestinal segments, its absorption rate was related to intestinal segments and perfusate concentrations, Peff was more than 0.2×10-4 cm·s-1. P-gp inhibitors could obviously increase the absorption of ZYS-01 in different intestinal segments. CONCLUSION: ZYS-01 is high permeable drug, it can be absorpted in the whole small intestinal segments, duodenum has the fastest absorption rate. the absorption is effected by different concentrations, low concentration has the fastest absorption rate, with the increasing of concentration, the absorption rate decreased gradually. The absorption mechanism of ZYS-01 is active transport. ZYS-01 may be a substrate for P-gp.