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Title: Setup and validation of shake-flask procedures for the determinationof partition coefficients (log D) from low drug amounts
Author: Andrés Sanz, Axel
Rosés Pascual, Martí
Ràfols Llach, Clara
Bosch, Elisabeth
Espinosa Ferrer, Sonia
Segarra, Victor
Huerta Castaño, José María
Keywords: Lipofília
Química farmacèutica
Pharmaceutical chemistry
Issue Date: 9-May-2015
Publisher: Elsevier B.V.
Abstract: Several procedures based on the shake-flask method and designed to require a minimum amount of drug for octanol-water partition coefficient determination have been established and developed. The procedures have been validated by a 28 substance set with a lipophilicity range from -2.0 to 4.5 (logD7.4). The experimental partition is carried out using aqueous phases buffered with phosphate (pH 7.4) and n-octanol saturated with buffered water and the analysis is performed by liquid chromatography. In order to have accurate results, four procedures and eight different ratios between phase volumes are proposed. Each procedure has been designed and optimized (for partition ratios) for a specific range of drug lipophilicity (low, regular and high lipophilicity) and solubility (high and low aqueous solubility). The procedures have been developed to minimize the measurement in the octanolic phase. Experimental logD7.4 values obtained from different procedures and partition ratios show a standard deviation lower than 0.3 and there is a nice agreement when these values are compared with the reference literature ones
Note: Versió postprint del document publicat a:
It is part of: European Journal of Pharmaceutical Sciences, 2015, vol. 76, p. 181-191
Related resource:
ISSN: 0928-0987
Appears in Collections:Articles publicats en revistes (Enginyeria Química i Química Analítica)

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