AN IN SITU EXPERIMENTAL MODEL IN RABBITS FOR THE STUDY OF RECTAL ABSORPTION

概要

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An in situ experimental model of rectal absorption was studied in rabbits compared with in vivo determination of drug concentration in the plasma of postcaval vein using indomethacin as drug. Pharmacokinetic parameters were similar between in vivo and in situ. When results from both studies were compared, 60% of the drug administered to the rectum was absorbed from the superior hemorrhoidal vein and the remaining 40% was absorbed from the inferior hemorrhoidal vein. When an aspirin suppository was used in this model, the amount of unaltered aspirin absorbed in the rectal mucosa or space was greater than the absorbed salicylic acid which was metabolized or degradated from aspirin. In the case of insulin, these differences were not seen in the insulin concentration of venous plasma between insulin physiological saline and surfactant suspension. However, using the in situ model, the surfactant effect on rectal absorption of insulin was observed. From the above results, it was concluded that this in situ experimental model of rectal absorption has advantages in that it can be used directly to measure the rectal absorption rate and to determine ratios of easily metabolized and poorly absorbed drugs. Therefore, this model appears to be useful in evaluation of rectal absorption.
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