Abstract
A liquid chromatographic method for the determination of the degree of protein-binding of drugs has been established, using a stationary phase to which bovine serum albumin has been bonded chemically. In a structurally heterogeneous group of compounds, results of the method correlate well with protein-binding data obtained by equilibrium dialysis (r = 0.89, n = 23, p less than 0.001). Within a series of analogous piperazines a good correlation is found (r = 0.981, n = 11, p less than 0.001). The chromatographic method allows automation of the measurement of protein-binding of large series of compounds with protein-binding ranging between 10 and 99%. The method is not expensive and is less time consuming than equilibrium dialysis. Only 1 mg of technical-grade material is required to determine the protein-binding, and radioactive labelling of the material is not necessary.
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