Please use this identifier to cite or link to this item:
https://hdl.handle.net/2445/143737
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 Lipophilicity 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: https://doi.org/10.1016/j.ejps.2015.05.008 |
It is part of: | European Journal of Pharmaceutical Sciences, 2015, vol. 76, p. 181-191 |
URI: | https://hdl.handle.net/2445/143737 |
Related resource: | https://doi.org/10.1016/j.ejps.2015.05.008 |
ISSN: | 0928-0987 |
Appears in Collections: | Articles publicats en revistes (Enginyeria Química i Química Analítica) |
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