Mechanism of Indomethacin Partition between n-Octanol and Water

概要

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To examine the fundamental process of the transfer of indomethacin (LND) to the biological membrane, the partition coefficient between n-octanol and water was measured at various pH values or in the presence of various cations by the shaking-flask method at 25℃. The apparent partition coefficient decreased with increase in pH and the true partition coefficient of unionized IND was determined to be 1.20×10^4,while that of ionized IND was 1.72×10^<-1>. The IND anion was found to be readily transferred to the hydrophobic region by forming ion-pair complexes with cations in the aqueous phase. The ion-pair complex of IND with the ammonium ion was transferred to the organic phase more readily than that with the sodium or potassiumion. In this study, a method for quantitative analysis of the ion-pair partition of an unstable drug at alkaline pH was established under conditions where more than two cationic species were present.
社団法人日本薬学会の論文
1981-08-25