薬物のヒト赤血球膜透過性.安息香酸誘導体の膜透過性と分配係数との構造活性相関性

概要

論文の詳細を見る
The transport properties of benzoic acid and its eighteen derivatives such as o-, m-or p-hydroxybenzoic acid (o-, m-or p-HBA), aminobenzoic acid (o-, m-or p-ABA), toluic acid (o-, m-or p-TA), fluorobenzoic acid (o-, m-or p-FBA), chlorobenzoic acid (o-, m-or p-CBA) and bromobenzoic acid (o-, m-or p-BBA) through human erythrocyte membranes were examined. The drugs having a hydrophilic ortho-substituent and those having a hydrophobic meta-or para-substituent showed higher transport. The ratio of free drugs in erythrocytes, fu_R, did not relate to the partition coefficient (P). However, fu_M (the ratio of free drugs in the plasma) and K_p. (the ratio of partition between erythrocytes and plasma) related to the P : fu_M=-0.3128×log P+0.9727 (R^2=0.8722^<***>), K_p=-0.2558×log P+0.8642 (R^2=0.8413^<***>). In p-nitrophenol-glycosides, the fu_M and the K_p that were predicted from these equations were compatible with the experimental results. It was suggested from these results that the fu_M and the K_p may be predictable from the P.
公益社団法人日本薬学会の論文
1992-10-25