Title: Studies on the intestinal absorption kinetics of tacrolimus in rats
Abstract: OBJECTIVE To investigate the absorption kinetics of tacrolimus in rats′ different intestines segments.METHODS The intestine in rats was cannulated for in situ perfusion.The effects of absorption site,drug concentration and pH value on tacrolimus absorption ability were studied.RESULTS The absorption rate constants (Ka) of tacrolimus at duodenum,jejunum,ileum and colon were 0.138 9,0.141 5,0.137 5 and 0.034 7 h-1,respectively.The concentration of 10,20 and 30 μg·mL-1 from the whole intestine,Ka were 0.245 3,0.254 0 and 0.236 1 h-1,respectively.Ka at pH of 5.4,6.8,7.8 from the whole intestine were 0.262 0,0.254 1 and 0.247 3 h-1,respectively.CONCLUSION The absorption of tacrolimus assumed a first-order kinetics with the passive diffusion absorption mechanism.Concentration and pH of the drug solution had no effect on the absorption kinetics.The absorption of tacrolimus was better in duodenum,jejunum and ileum than in colon.
Publication Year: 2010
Publication Date: 2010-01-01
Language: en
Type: article
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