DISTRIBUTION OF HALOFENATE IN PLASMA - COMPARATIVE ANALYSIS USING SCATCHARD VS STEPWISE-ASSOCIATION-CONSTANTS

  • 1 January 1976
    • journal article
    • research article
    • Vol. 14  (1) , 75-81
Abstract
The distribution of Halofenate between the free and [human] albumin bound forms was calculated by the use of 2 computer programs using both Scatchard association constants [Kassoc] for a 3,3,7 model and 6 stepwise equilibrium constants over a range of drug concentrations reported in man. The calculations, using either set of constants, showed that only 0.3-0.5% of the drug would be free. Using Scatchard Kassoc, it was estimated that 92 to 95% of the drug would be bound by the high affinity set of sites and lesser amounts by sites of lesser affinity. A more complex pattern of distribution was obtained with the stepwise equilibrium constants. At low concentrations of Halofenate the complex with 1 mol of drug/mol protein was most abundant, and at the highest concentration studied the complex with 2 mol of drug/mol protein was most abundant.

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