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Correlations entre la structure et des paramêtres pharmacocinétiques dans une série d' amides crésotiniques

1984; Elsevier BV; Volume: 20; Issue: 1-2 Linguagem: Francês

10.1016/0378-5173(84)90224-2

1873-3476

Michel Audran, J. L. Chanal, Gilbert Bergé, R Marignan, Henri Cousse,

Analytical Methods in Pharmaceuticals

L'étude pharmacocinétique de sept amides crésotiniques a été effectuée cnez le rat — les paramêtres pharmacocinétiques suivants: demi-vie du produit inchange, volume de distribution, clairance totale ont été calculés. Des correlations ont pu être envisag'ees entre ces paramêtres pharmacocinétiques et des paramêtres physicochimiques caractéristiques de la structure de ces composés: pKa, lipophilie et encombrement stérique. Pharmacokinetics of seven cresotinamids was studied in rat: half-life, distribution volume, total clearance were calculated. Correlations between these pharmac akinetic parameters and the characteristic physicochemical parameters (pKa, lipophilia, steric volume) of these compounds' structure were discussed. Good correlations were found between half-life and steric volume (log T12 = 0.101 MR −0.912 and between half-life and iipophiiia (log T12−0.127 (log P)2−1.559), and on the other hand, between total clearance and steric volume (log CI = −0.079 MR + 1.854) and between total clearance and lipophilia (log CI = 2.557 log P −0.502 (log P)2 −1.487). However, no correlations were established between distribution volume and any of the characteristic physicochemical parameters of these compounds' structure.