Stereoselective bile excretion of ibuprofen glucuronide and the transport mechanism in the biliary efflux
- VernacularTitle:布洛芬葡萄糖醛酸结合物的立体选择性胆排泄及其机制研究
- Author:
Xijing CHEN
;
Iwaki MASAHIRO
- Publication Type:Journal Article
- Keywords:
ibuprofen;
glucuronide;
EHBR;
Mrp2;
bile excretion;
stereoselectivity
- From:
Chinese Journal of Clinical Pharmacology and Therapeutics
2007;12(10):1163-1167
- CountryChina
- Language:Chinese
-
Abstract:
AIM: To illustrate the effects of drug transporters on the bile efflux of ibuprofen glucuronide(IBG), the difference of bile excretion and plasma concentration of ibuprofen(IB) and its glucuronides was studied in EHBR and normal SD rat(SDR). METHODS: After 20 mg/kg of IB enantiomers administrated intravenously, the bile and blood were collected from the rats and the concentration of IB and their glucuronide were measured by HPLC methods. RESULTS: The bile excretion of IBG was obviously (but no totally) suppressed in EHBR (1.7%±1.0%, 0.6%±0.9% of the dose respectively for S-IBG and R-IBG) compared with that in SDR (18.4%±4.0% and 3.0%±2.4% of the dose respectively for S-IBG and R-IBG), for both kinds of rats, there are more S-IBG excreted than that of R-IBG. As the result of reduction of IBG excreted in bile, the concentration of IBG was higher in blood in EHBRs. CONCLUSION: The results suggest that Mrp2 is the most important transporter for IBG, and other transporter(s) may participate in the process.
