In vitro studies on the distribution of probucol among human plasma lipoproteins

Journal Article · Sat Sep 01 04:00:00 EDT 1984 · Mol. Pharmacol.; (United States)

OSTI ID:6133117

Urien, S; Riant, P; Albengres, E; Brioude, R; Tillement, J P

The role of human plasma lipoproteins as carriers in the blood transport of the cholesterol-lowering and water-insoluble drug, probucol, was investigated in in vitro studies. (/sup 14/C)Probucol was incubated in whole human blood, a serum pool, individual diluted sera, and isolated protein and lipoprotein fractions. In whole blood, about 90% partitioned in plasma. Following ultracentrifugal fractionation of the serum, it was found that less than 5% distributed in the d greater than 1.20 protein fraction (albumin-rich fraction) and more than 95% in the lipoprotein fractions. The distribution of probucol in the lipoprotein fractions correlated with the lipoprotein total lipid volume under saturation conditions (incubation of isolated lipoprotein fractions) as well as nonsaturation conditions (fractionation of serum exposed to (/sup 14/C)probucol). Incubation of the albumin-rich fraction and of apolipoproteins originating from the isolated lipoprotein fractions showed that they account for a negligible part in the interaction of probucol with blood components. The probucol uptake of individual sera was shown to be correlated to the lipid content of the serum. When probucol was incubated in erythrocyte suspensions containing variable amounts of lipoproteins, probucol partitioned less in erythrocytes as the lipoprotein concentration increased in the suspension.

• Research Organization: Faculte de Medecine, Creteil, France
• OSTI ID: 6133117
• Journal Information: Mol. Pharmacol.; (United States), Journal Name: Mol. Pharmacol.; (United States) Vol. 26:2; ISSN MOPMA
• Country of Publication: United States
• Language: English

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560306* -- Chemicals Metabolism & Toxicology-- Man-- (-1987)
59 BASIC BIOLOGICAL SCIENCES
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
AROMATICS
BIOLOGICAL MATERIALS
BLOOD
BLOOD PLASMA
BODY FLUIDS
CARBON 14 COMPOUNDS
DISTRIBUTION
DRUGS
HYDROXY COMPOUNDS
IN VITRO
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
LIPIDS
LIPOPROTEINS
MATERIALS
ORGANIC COMPOUNDS
PHENOLS
PROTEINS
TISSUE DISTRIBUTION
TRACER TECHNIQUES
UPTAKE