کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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5809808 | 1556174 | 2015 | 11 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Setup and validation of shake-flask procedures for the determination of partition coefficients (log D) from low drug amounts Setup and validation of shake-flask procedures for the determination of partition coefficients (log D) from low drug amounts](/preview/png/5809808.png)
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 â2.0 to 4.5 (log D7.4).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 log D7.4 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.
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Journal: European Journal of Pharmaceutical Sciences - Volume 76, 30 August 2015, Pages 181-191