Abstract
The solubility of lovastatin and simvastatin (inevitable drugs in the management of cardiovascular diseases) was studied by phase-solubility measurements in multicomponent colloidal and non-colloidal media. Complexation in aqueous solutions of the highly lipophilic statins with β-cyclodextrin (β-CD) in the absence and the presence of dissolved polyvinyl pyrrolidone, its monomeric compound, tartaric acid and urea, respectively, were investigated. For the characterization of the CD-statin inclusion complexes, stability constants for the associates have been calculated.
It was shown that complexation might lead to considerable improvement of the aqueous solubilities of both statins. In binary systems dominantly statin-β-CD associates of 1:1 molar ratios form, which exhibit considerable surface activity.
In statin-CD-additive ternary systems the solubility of the statins could be further improved. The enhanced drug solubilities in the solutions of small molecular mass solutes are likely related due to the peculiar feature of the additives to destroy the H-bonding system of β-CD. In polymer-containing systems statin-CD-polymer associates of supramolecular structure may presumably form in a way that portions of surface-active statin-β-CD complexes are anchored at the macromolecular chains.
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Süle, A., Csempesz, F. (2008). Complexation of Statins with β-Cyclodextrin in Solutions of Small Molecular Additives and Macromolecular Colloids. In: Hórvölgyi, Z.D., Kiss, É. (eds) Colloids for Nano- and Biotechnology. Progress in Colloid and Polymer Science, vol 135. Springer, Berlin, Heidelberg. https://doi.org/10.1007/2882_2008_120
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DOI: https://doi.org/10.1007/2882_2008_120
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