PION pSOL

We thank Professor Per Artursson of Uppsala University for allowing us to use the intrinsic solubilities reported in reference [28] prior to their publication, and Suzanne Tilton and Alexis Foreman of pION INC. for some of the pSOL solubility measurements. 

To achieve high quality data with low sample amount, a commercial pSOL instrument (pION, Woburn, MA) can be used. It delivers with an pH metric approach a solubility pH profile with 100 tig of solid compound. The throughput is 4-6 compounds a day. 

Lunn G, Schmuff NR (1997) HPLC Methods for Pharmaceutical Analysis. Wiley-Intersciences, New York Pan L, Ho Q, Tsutsui K et al. (2001) Comparison of chromatographic and spectroscopic methods used to rank compounds for aqueous solubility. I Pharm Sci 90(4) 521-529 PSOL (PION) http //www.pion-inc.com/pSOL.htm Silveston R, Kronberg B (1994) Accurate measurements of solubility and thermodynamic transfer quantities using reversed-phase liquid-liquid chromatography. I Chrom 659(l) 43-56... 

As compound supply is Ukely to be limited, only a few solvent systems can be investigated during initial solubility studies. Typically, the solubility of the com-potmds in water, 0.9% w/v saline, 0.1 M HCl and 0.1 M NaOH will be determined. If there is sufficient compotmd, then the solubility in other systems may be considered (e.g., co-solvents, such as PEG400 and propylene glycol). In addition, the solubility in oils and surfactants systems (e.g.. Tween 80) may be considered. Automated instruments allow ready measure of solubility, such as by using the pION s pSOL (5) whereas as little as 0.1 mg of the compound is sufficient to establish a complete solubility profile. 

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