Analytical studies and murine pharmacokinetics of cosalane (Meeting abstract).

Important note: Information in this article was accurate in 1995. The state of the art may have changed since the publication date.

Analytical studies and murine pharmacokinetics of cosalane (Meeting abstract).

Proc Annu Meet Am Assoc Cancer Res; 35:A2546 1994. Unique Identifier : AIDSLINE ICDB/95604231
Bigelow J; Mathews L; Chrin L; Horton P; McCormack J; Vermont Cancer Center and Dept. of Pharmacology, Univ. of; Vermont, Burlington, Vermont 05405

Abstract: Cosalane (NSC 640067; COS) is a steroid derivative that contains two aryl carboxylate functions, and exhibits anti-HIV activity apparently by inhibition of viral attachment to target cells. We have developed an assay that is suitable for detection and determination of COS in biological fluids. Samples are prepared for analysis by treatment with a methanol/acetonitrile mixture and HPLC analysis is accomplished using a polymeric reversed-phase column and gradient elution (acetonitrile/water). COS is detected routinely at 230 nm, but detection at 320 nm is feasible for some samples. COS was administered iv to mice, at doses from 1-10 mg/kg, in a cyclodextrin-based vehicle. Plasma concentrations of COS in the 50-100 micromolar range are evident for several hours after iv dosing at 10 mg/kg and concentrations in the 10 micromolar range are observed 24 hr after dosing. Comparable plasma concentrations are observed after ip and sc administration of cos at higher doses (25-50 mg/kg). COS is slowly eliminated from plasma after iv administration (half-life of 500-600 minutes); estimated values for Vd and CL are 3 ml and 0.005 ml/min.

Keywords: Animal Antiviral Agents/*ANALYSIS/BLOOD/*PHARMACOKINETICS Aurintricarboxylic Acid/*ANALOGS & DERIVATIVES/ANALYSIS/BLOOD/ PHARMACOKINETICS Chromatography, High Pressure Liquid HIV/DRUG EFFECTS Mice Spectrophotometry, Ultraviolet ABSTRACT
950228
M9521045

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