The quest for exceptional drug solubilization in diluted surfactant solutions and consideration of residual solid state
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Publication date
2017
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01A - Journal article
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Parent work
European Journal of Pharmaceutical Sciences
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Volume
111
Issue / Number
Pages / Duration
96-103
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Elsevier
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Abstract
Solubility screening in different surfactant solutions is an important part of pharmaceutical profiling. A particular interest is in low surfactant concentrations that mimic the dilution of an oral dosage form. Despite of intensive previous research on solubilization in micelles, there is only limited data available at low surfactant concentrations and generally missing is a physical state analysis of the residual solid. The present work therefore studied 13 model drugs in 6 different oral surfactant solutions (0.5%, w/w) by concomitant X-ray diffraction (XRPD) analysis to consider effects on solvent-mediated phase transformations. A particular aspect was potential occurrence of exceptionally high drug solubilization. As a result, general solubilization correlations were observed especially between surfactants that share chemical similarity. Exceptional solubility enhancement of several hundred-fold was evidenced in case of sodium dodecyl sulfate solutions with dipyridamole and progesterone. Furthermore, carbamazepine and testosterone showed surfactant-type dependent hydrate formation. The present results are of practical relevance for an optimization of surfactant screenings in preformulation and early development and provide a basis for mechanistic modeling of surfactant effects on solubilization and solid state modifications.
Keywords
Poorly soluble drug, Surfactant, Solubilization, Micelles, Residual solid, Solvent-mediated phase transformation
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0928-0987
1879-0720
1879-0720
Language
English
Created during FHNW affiliation
Yes
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Publication status
Published
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Peer review of the complete publication
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Citation
Saal, W., Alsenz, J., Wyttenbach, N., & Kuentz, M. (2017). The quest for exceptional drug solubilization in diluted surfactant solutions and consideration of residual solid state. European Journal of Pharmaceutical Sciences, 111, 96–103. https://doi.org/10.1016/j.ejps.2017.09.032