Detailed Study of Precipitation of a Poorly Water Soluble Test Compound Using Methodologies as in Activity And Solubility Screening - Mixing and Automation Effects.

Detailed Study of Precipitation of a Poorly Water Soluble Test Compound Using Methodologies as in Activity And Solubility Screening - Mixing and Automation Effects.
Comb Chem High Throughput Screen. 2013 May 22;
Authors: Gillespie C, Kennedy AR, Edwards D, Dowden L, Daublain P, Halling P
Abstract
Storage of pharmaceutical discovery compounds dissolved in dimethylsulfoxide (DMSO) is commonplace within industry. Often, the DMSO stock solution is added to an aqueous system (e.g. in bioassay or kinetic solubility testing)- since most test compounds are hydrophobic, precipitation could occur. Little is known about the factors affecting this precipitation process at the low (μM) concentrations used in screening analyses. Here, a poorly water soluble test compound (tolnaftate) was used to compare manual and automated pipetting, and explore the effect of mixing variables on precipitation. The amount of drug present in the supernatant after precipitation and centrifugation of the samples was quantified. An unusual result was obtained in three different laboratories: results of experiments performed initially were statistically significantly higher than those performed after a few days in the same lab. No significant differences were found between automated and manual pipetting, including in variability. Vortex mixing was found to give significantly lower supernatant amounts compared to milder mixing types. The mixing employed affects the particle grow...

Source: Combinatorial Chemistry and High Throughput Screening - May 22, 2013 Category: Chemistry Authors: Gillespie C, Kennedy AR, Edwards D, Dowden L, Daublain P, Halling P Tags: Comb Chem High Throughput Screen Source Type: research