Effect of vinylpyrrolidone polymers on the solubility and supersaturation of drugs; a study using the Cheqsol method

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
Elisenda FornellsClara Ràfols

Abstract

The development of methods to increase the bioavailability of drugs is of great interest, especially for those which are poorly soluble or permeable. One of the strategies to enhance the solubility (which in turn has the potential of increase bioavailability) of drugs is the use of additives in the formulation process, so that the drug can stay supersaturated in biological fluids for a period of time long enough to allow absorption. The use of polymers as pharmaceutical excipients in order to stabilize the supersaturation of drugs is common practice. In this work, the ability of different polymers of vinylpyrrolidone (K-12, K-17, K-25, K-29/32, K-90) and a copolymer of vinylpyrrolidone and vinylacetate (S-630) have been tested for their impact on the supersaturation of drugs. Sixteen drugs of different chemical nature have been selected, and analyzed using the Cheqsol method. The results of the drug alone, and of physical mixtures with the different polymers at several polymer:drug ratios have been compared in terms of supersaturation extent and duration. It has been observed that acidic compounds displayed enhanced solubility in different ways: sometimes the supersaturated state of the drug is maintained for a long time, due t...Continue Reading

Citations

Sep 13, 2019·Drug Development and Industrial Pharmacy·Ardita VeseliAlbin Kristl
Aug 29, 2021·Polymers·Marcin LemanowiczAndrzej Gierczycki
Aug 17, 2020·Journal of Chemical Information and Modeling·Antonio LlinasAlex Avdeef

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