Elsevier

Biochemical Pharmacology

Volume 44, Issue 9, 3 November 1992, Pages 1891-1893
Biochemical Pharmacology

Short communication
Comparative binding of etretinate and acitretin to plasma proteins and erythrocytes

https://doi.org/10.1016/0006-2952(92)90087-YGet rights and content

Abstract

The interactions of etretinate and its main metabolite acitretin with human plasma proteins have been investigated in vitro by an erythrocyte partitioning technique that allows a quantitative estimation of the plasma and erythrocyte binding. Etretinate was extensively lipoprotein-bound (75% of plasma etretinate), with a binding constant for its main low density lipoprotein carrier of 40 × 106 M−1, accounting for 48% of the total plasma-bound drug. Acitretin was mainly albumin-bound (91% of plasma acitretin), with a binding constant of 0.7 × 106 M−1. The total plasma binding of both drugs was > 99% and, in blood, the fractions associated with erythrocytes were 14.5 and 8.1% of the total amount for etretinate and acitretin, respectively.

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