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

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...

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Autores: Fornells, Elisenda, Fuguet i Jordà, Elisabet, Mañé, Meritxell, Ruiz, Rebeca, Box, Karl, Bosch, Elisabeth, Ràfols Llach, Clara
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2018
País:España
Institución:Universidad de Barcelona
Repositorio:Dipòsit Digital de la UB
OAI Identifier:oai:diposit.ub.edu:2445/143522
Acceso en línea:https://hdl.handle.net/2445/143522
Access Level:acceso abierto
Palabra clave:Solubilitat
Desenvolupament de medicaments
Solubility
Drug development
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spelling Effect of vinylpyrrolidone polymers on the solubility and supersaturation of drugs; a study using the Cheqsol methodFornells, ElisendaFuguet i Jordà, ElisabetMañé, MeritxellRuiz, RebecaBox, KarlBosch, ElisabethRàfols Llach, ClaraSolubilitatDesenvolupament de medicamentsSolubilityDrug developmentThe 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 to the precipitation of an amorphous solid, as determined by X-ray diffraction studies; on other occasions supersaturation increases but only for a short time, compared to the drug alone, and then the drug precipitates to a crystalline form. Only a few basic drugs displayed enhanced solubility in the presence of PVP polymers, in contrast to acidic compounds.Elsevier B.V.2018info:eu-repo/semantics/articleinfo:eu-repo/semantics/acceptedVersionapplication/pdfhttps://hdl.handle.net/2445/143522Articles publicats en revistes (Enginyeria Química i Química Analítica)reponame:Dipòsit Digital de la UBinstname:Universidad de BarcelonaInglésVersió postprint del document publicat a: https://doi.org/10.1016/j.ejps.2018.02.025European Journal of Pharmaceutical Sciences, 2018, vol. 117, p. 227-235https://doi.org/10.1016/j.ejps.2018.02.025cc-by-nc-nd (c) Elsevier B.V., 2018http://creativecommons.org/licenses/by-nc-nd/3.0/esinfo:eu-repo/semantics/openAccessoai:diposit.ub.edu:2445/1435222026-05-27T06:46:51Z
dc.title.none.fl_str_mv Effect of vinylpyrrolidone polymers on the solubility and supersaturation of drugs; a study using the Cheqsol method
title Effect of vinylpyrrolidone polymers on the solubility and supersaturation of drugs; a study using the Cheqsol method
spellingShingle Effect of vinylpyrrolidone polymers on the solubility and supersaturation of drugs; a study using the Cheqsol method
Fornells, Elisenda
Solubilitat
Desenvolupament de medicaments
Solubility
Drug development
title_short Effect of vinylpyrrolidone polymers on the solubility and supersaturation of drugs; a study using the Cheqsol method
title_full Effect of vinylpyrrolidone polymers on the solubility and supersaturation of drugs; a study using the Cheqsol method
title_fullStr Effect of vinylpyrrolidone polymers on the solubility and supersaturation of drugs; a study using the Cheqsol method
title_full_unstemmed Effect of vinylpyrrolidone polymers on the solubility and supersaturation of drugs; a study using the Cheqsol method
title_sort Effect of vinylpyrrolidone polymers on the solubility and supersaturation of drugs; a study using the Cheqsol method
dc.creator.none.fl_str_mv Fornells, Elisenda
Fuguet i Jordà, Elisabet
Mañé, Meritxell
Ruiz, Rebeca
Box, Karl
Bosch, Elisabeth
Ràfols Llach, Clara
author Fornells, Elisenda
author_facet Fornells, Elisenda
Fuguet i Jordà, Elisabet
Mañé, Meritxell
Ruiz, Rebeca
Box, Karl
Bosch, Elisabeth
Ràfols Llach, Clara
author_role author
author2 Fuguet i Jordà, Elisabet
Mañé, Meritxell
Ruiz, Rebeca
Box, Karl
Bosch, Elisabeth
Ràfols Llach, Clara
author2_role author
author
author
author
author
author
dc.subject.none.fl_str_mv Solubilitat
Desenvolupament de medicaments
Solubility
Drug development
topic Solubilitat
Desenvolupament de medicaments
Solubility
Drug development
description 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 to the precipitation of an amorphous solid, as determined by X-ray diffraction studies; on other occasions supersaturation increases but only for a short time, compared to the drug alone, and then the drug precipitates to a crystalline form. Only a few basic drugs displayed enhanced solubility in the presence of PVP polymers, in contrast to acidic compounds.
publishDate 2018
dc.date.none.fl_str_mv 2018
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/acceptedVersion
format article
status_str acceptedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/2445/143522
url https://hdl.handle.net/2445/143522
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Versió postprint del document publicat a: https://doi.org/10.1016/j.ejps.2018.02.025
European Journal of Pharmaceutical Sciences, 2018, vol. 117, p. 227-235
https://doi.org/10.1016/j.ejps.2018.02.025
dc.rights.none.fl_str_mv cc-by-nc-nd (c) Elsevier B.V., 2018
http://creativecommons.org/licenses/by-nc-nd/3.0/es
info:eu-repo/semantics/openAccess
rights_invalid_str_mv cc-by-nc-nd (c) Elsevier B.V., 2018
http://creativecommons.org/licenses/by-nc-nd/3.0/es
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Elsevier B.V.
publisher.none.fl_str_mv Elsevier B.V.
dc.source.none.fl_str_mv Articles publicats en revistes (Enginyeria Química i Química Analítica)
reponame:Dipòsit Digital de la UB
instname:Universidad de Barcelona
instname_str Universidad de Barcelona
reponame_str Dipòsit Digital de la UB
collection Dipòsit Digital de la UB
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,300719

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