A potentiometric titration method for the crystallization of drug-like organic molecules

Du-Cuny, Lei and Huwyler, Jörg and Fischer, Holger and Kansy, Manfred. (2007) A potentiometric titration method for the crystallization of drug-like organic molecules. International Journal of Pharmaceutics, 342 (1-2). pp. 161-167.

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Official URL: http://edoc.unibas.ch/54623/

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It is generally accepted, that crystalline solids representing a low energy polymorph should be selected for development of oral dosage forms. As a consequence, efficient and robust procedures are needed at an early stage during drug discovery to prepare crystals from drug-like organic molecules. In contrast to the use of supersaturated solutions, we present a potentiometric crystallization procedure where saturated solutions are prepared in a controlled manner by pH-titration. Crystallization is carried out under defined conditions using the sample concentration and experimental pK(a) values as input parameters. Crystals of high quality were obtained for 11 drugs selected to demonstrate the efficiency and applicability of the new method. Technical improvements are suggested to overcome practical limitations and to enhance the possibility of obtaining crystals from molecules in their uncharged form.
Faculties and Departments:05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Pharmaceutical Technology (Huwyler)
UniBasel Contributors:Huwyler, Jörg
Item Type:Article, refereed
Article Subtype:Research Article
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:24 Oct 2017 08:06
Deposited On:24 Oct 2017 08:06

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