Using droplet-based microfluidic technology to study the precipitation of a poorly water-soluble weakly basic drug upon a pH-shift

Edwards, Francine and Tsakmaka, Christina and Mohr, Stephan and Fielden, Peter R. and Goddard, Nick J. and Booth, Jonathan and Tam, Kin Y. (2013) Using droplet-based microfluidic technology to study the precipitation of a poorly water-soluble weakly basic drug upon a pH-shift. Analyst, 138 (1). pp. 339-345. ISSN 0003-2654

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Abstract

The purpose of this study is to develop a droplet-based microfluidic device capable of monitoring drug precipitation upon a shift from gastric pH (pH 1.5) to intestinal pH (pH 6.5-7.0). The extent of precipitation occurring in droplets over time was measured using a novel on-chip laser scattering technique specifically developed for this study. The precipitation of ketoconazole, a poorly water-soluble basic drug, was investigated under different concentrations and pH values. It has been shown that the drug precipitates rapidly under supersaturation. Two water-soluble aqueous polymers, namely, polyvinylpyrrolidone (PVP) and hydroxypropylmethylcellulose (HPMC) have been evaluated as precipitation inhibitors. HPMC was shown to be the most potent precipitation inhibitor. It is envisaged that the microfluidic pH-shift method developed in this study would form a proof-of-concept study, towards the development of a high throughput method for screening pharmaceutical excipients/precipitation inhibitors.

Item Type:
Journal Article
Journal or Publication Title:
Analyst
Uncontrolled Keywords:
/dk/atira/pure/subjectarea/asjc/1300/1303
Subjects:
?? nucleationhumansdissolutionsystemformulationssolubilitysolid dispersionsabsorptionbiochemistryspectroscopyenvironmental chemistryanalytical chemistryelectrochemistry ??
ID Code:
62861
Deposited By:
Deposited On:
13 Mar 2013 13:48
Refereed?:
Yes
Published?:
Published
Last Modified:
15 Jul 2024 13:40