Literature DB >> 30103861

Brief overview of solubility methods: Recent trends in equilibrium solubility measurement and predictive models.

Árpád Könczöl1, Gergő Dargó2.   

Abstract

Solubility is a crucial physicochemical parameter affecting the whole process of drug discovery and development. Thus, understanding of the methods and concepts to measure and predict this propensity are of utmost importance for the pharmaceutical scientist. Despite their inherent limitations, kinetic solubility screening methods became routine assays by mimicking bioassay conditions and guiding the lead optimization process. In contrast, thermodynamic solubility methods show a clear evolution: miniaturized high throughput assays coupled to analytical techniques such as solid-state characterization, ultra performance liquid chromatography, or polychromatic turbidimetry, have been developed, thereby enabling a more complex physicochemical profiling at the early discovery stage. Solubility prediction still poses a significant challenge at the industrial level. Classification and critical evaluation of recent in silico models are provided. Discussion of experimental and computational methods: was based on relevant industrial references.
Copyright © 2018 Elsevier Ltd. All rights reserved.

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Year:  2018        PMID: 30103861     DOI: 10.1016/j.ddtec.2018.06.001

Source DB:  PubMed          Journal:  Drug Discov Today Technol        ISSN: 1740-6749


  3 in total

1.  Harmonizing solubility measurement to lower inter-laboratory variance - progress of consortium of biopharmaceutical tools (CoBiTo) in Japan.

Authors:  Asami Ono; Naoya Matsumura; Takahiro Kimoto; Yoshiyuki Akiyama; Satoko Funaki; Naomi Tamura; Shun Hayashi; Yukiko Kojima; Masahiro Fushimi; Hiroshi Sudaki; Risa Aihara; Yuka Haruna; Maiko Jiko; Masaru Iwasaki; Takuya Fujita; Kiyohiko Sugano
Journal:  ADMET DMPK       Date:  2019-08-05

Review 2.  Perspectives in solubility measurement and interpretation.

Authors:  Christel A S Bergström; Alex Avdeef
Journal:  ADMET DMPK       Date:  2019-04-05

3.  Drug Solubility Correlation Using the Jouyban-Acree Model: Effects of Concentration Units and Error Criteria.

Authors:  Elaheh Rahimpour; Sima Alvani-Alamdari; William E Acree; Abolghasem Jouyban
Journal:  Molecules       Date:  2022-03-20       Impact factor: 4.411

  3 in total

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