Title: Study on the kinetics of in situ intestinal absorption of febuxostat in rats
Abstract: OBJECTIVE To investigate the absorption characteristics of febuxostat,a new antipodagrics in rat intestine,so as to provide scientific basis for the formulation design of oral preparation of febuxostat.METHODS The absorption kinetics of febuxosatat in various intestinal segments was measured using in situ rat single-pass intestinal perfusion model and the drug concentration was analyzed by ultra performance liquid chromatography(UPLC).The effect of drug concentration on the intestinal absorption was investigated too.RESULTS The Ra,Peff and Pw values of febuxostat in duodenum and colon were significantly higher than those in jejunum and ileum(P0.05).No significant difference in the parameters was found between middle concentration(10 μmol·L-1) group and high concentration(20 μmol·L-1) group(P0.05).However,both of them were obviously higher than those in low concentration(5 μmol·L-1) group(P0.05).CONCLUSION Febuxostat can be well absorbed in the intestine.The absorption rates of febuxostat in duodenum and colon are significantly higher than those in ileum and jejunum.Efflux transport protein may be involved in the intestinal absorption of febuxostat.
Publication Year: 2012
Publication Date: 2012-01-01
Language: en
Type: article
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