Studies on Sustained-Release Dosage Forms. II. Pharmacokinetics after Rectal Administration of Indomethacin Suppositories in Rabbits

概要

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The plasma concentration of indomethacin (IM) after administration of sustained-release suppositories containing microencapsulated IM was analyzed by means of the compartment model method and the statistical moment method. The plasma concentration-time course after rectal administration of conventional suppositories followed a two-compartment model with first-order absorption for all doses examined, 6.25,12.5 and 25 mg. The pharmacokinetic constants did not show dose-dependency. It was presumed that the plasma concentration-time course after rectal administration of sustained-release suppositories could be accounted for by a two-compartment model with two consecutive first-order input steps. The release rate constants (k_1) of these dosage forms were very small compared with the absorption rate (k_a). Consequently, the release process from sustainedrelease suppositories was the rate-determining step. This conclusion was confirmed by statistical moment analysis.
社団法人日本薬学会の論文
1983-09-25