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Perspectives in solubility measurement and interpretation
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.ORCID iD: 0000-0002-8917-2612
In ADME Res, 1732 First Ave,102, New York, NY 10128 USA.
2019 (English)In: ADMET AND DMPK, ISSN 1848-7718, Vol. 7, no 2, p. 88-105Article, review/survey (Refereed) Published
Abstract [en]

Several key topics in solubility measurement and interpretation are briefly summarized and illustrated with case studies drawing on published solubility determinations as a function of pH. Featured are examples of ionizable molecules that exhibit solubility-pH curve distortion from that predicted by the traditionally used Henderson-Hasselbalch equation and possible interpretations for these distortions are provided. The scope is not exhaustive; rather it is focused on detailed descriptions of a few cases. Topics discussed are limitations of kinetic solubility, 'brick-dust and grease-balls,' applications of simulated and human intestinal fluids, supersaturation and the relevance of pre-nucleation clusters and sub-micellar aggregates in the formation of solids, drug-buffer/excipient complexation, hydrotropic solubilization, acid-base 'supersolubilization,' cocrystal route to supersaturation, as well as data quality assessment and solubility prediction. The goal is to highlight principles of solution equilibria - graphically more than mathematically - that could invite better assay design, to result in improved quality of measurements, and to impart a deeper understanding of the underlying solution chemistry in suspensions of drug solids. The value of solid state characterizations is stressed but not covered explicitly in this mini-review.

Place, publisher, year, edition, pages
IAPC PUBLISHING , 2019. Vol. 7, no 2, p. 88-105
Keywords [en]
Solubility-pH, shake-flask solubility, intrinsic solubility, thermodynamic solubility, Henderson-Hasselbalch equation, supersaturation, pre-nucleation clusters, drug aggregates, drug salts, pharmaceutical cocrystals
National Category
Other Health Sciences
Identifiers
URN: urn:nbn:se:uu:diva-384094DOI: 10.5599/admet.686ISI: 000467047800001OAI: oai:DiVA.org:uu-384094DiVA, id: diva2:1323098
Available from: 2019-06-11 Created: 2019-06-11 Last updated: 2019-06-11Bibliographically approved

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