Integration of a rapid automated solubility classification into early validation of hits obtained by high throughput screening

A Consistent Dataset of Kinetic Solubilities for Early‐Phase Drug Discovery

“…The lower value of those determined from the visual inspection and nephelometry was used as the final solubility value, which was in some cases corrected for weighing inaccuracies in the preparation of the stock solution. For further details see Reference [19]. Compound solubilities measured using the shake flask method were in good agreement with those measured using nephelometry.…”

“…The final DMSO concentration in the wells was 1.6-5 %. Precipitate in the wells was detected via nephelometric measurements; [19] precipitation leads to an increase in orthogonally scattered light. The last concentration before the nephelometric signal increased was used as the solubility.…”

“…NMR, turbidimetry, potentiometry, UV-Vis and IR spectroscopy methods, and nephelometry are only some examples of techniques used for determining kinetic and thermodynamic solubilities. [18,19] Many of these methods have specific advantages in throughput, accuracy or cost. The solubility endpoint can either be extrapolated from concentration series, or be determined exactly by addition of an incremental amount of compound or incremental variation of solvent properties.…”

Attempts and outcomes of liquisolid technology: An updated chronological compilation of innovative ideas and adjuvants in the field

“…DSC and XRD simultaneously suggested the loss of drug crystallinity of upon liquisolid formulation which was further confirmed and validated by SEM that ensured the superiority of the technique. Bioavailability study indicated that the prepared optimal liquisolid formula did not differ significantly from the marketed famotidine tablets concerning C max , t max , and AUC (0)(1)(2)(3)(4)(5)(6)(7)(8) Figure 2). The role of nonvolatile solvents in enhancement of dissolution behavior can be easily observed by analyzing the obtained dissolution data, but the burden of further increment in these pharmaceutical parameters, falls on nature and type of carrier material used.…”

Interpreting physicochemical experimental data sets

“…Aqueous solubilities can be measured by numerous methods including shake-flask with separation and quantification of the supernatant by ultraviolet-visible (UV) spectroscopy [2][3][4][5][6], liquid chromatography (LC) UV [6][7][8], or LC tandem mass spectroscopy (MSMS) [7], turbidimetric methods [9][10][11] or potentiometric approaches [12,13].…”