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Article: Impact of cocrystal solution-state stability on cocrystal dissociation and polymorphic drug recrystallization during dissolution

TitleImpact of cocrystal solution-state stability on cocrystal dissociation and polymorphic drug recrystallization during dissolution
Authors
KeywordsCocrystal solution-state stability
Polymorphism
Curcumin
Supersaturation
Cocrystal dissociation
Issue Date2021
PublisherElsevier BV. The Journal's web site is located at http://www.elsevier.com/locate/ijpharm
Citation
International Journal of Pharmaceutics, 2021, v. 610, p. article no. 121239 How to Cite?
AbstractThe present study aimed to investigate how cocrystal solution-state stability may affect the polymorphic drug formation and transition during dissolution. In this work, curcumin-resorcinol (CUR-RES), curcumin-hydroquinone (CUR-HYQ) and curcumin-phloroglucinol (CUR-PHL) cocrystals were employed for dissolution studies in three buffer systems to study the effects of solvent and cocrystal thermodynamic stability. The undissolved solids were collected at designed time points and characterized by powder X-ray diffraction, differential scanning calorimetry and scanning electron microscopy. In pH 1.2 buffer, three cocrystals generated > 94% of metastable CUR form III with trace amount of stable CUR form I, while the phase purity of CUR form III recrystallized from buffers containing ethanol (EtOH) were decreased dramatically. For the same cocrystal, the cocrystal form maintained longer in the pH 1.2 buffer when compared with buffers containing EtOH. The phase purity of recrystallized CUR form III in the metastable cocrystal systems followed a linear relationship against CUR solubility, while the thermodynamically stable cocrystal resulted in a non-linear relationship. Due to different intermolecular interactions analyzed by 1H NMR, the stable cocrystal required a higher supersaturation level to precipitate pure CUR form III, in comparison to two metastable cocrystals. Our study offers important insights into mitigating the risk of recrystallization of drug polymorphs during cocrystal dissolution and demonstrates the potential use of cocrystals for drug polymorph preparation, both of which are crucial to the pharmaceutical cocrystal development and reformulation of existing drugs.
Persistent Identifierhttp://hdl.handle.net/10722/307701
ISSN
2021 Impact Factor: 6.510
2020 SCImago Journal Rankings: 1.153
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorXUAN, B-
dc.contributor.authorChen, YCS-
dc.contributor.authorWong, KC-
dc.contributor.authorChen, R-
dc.contributor.authorLo, PS-
dc.contributor.authorLakerveld, R-
dc.contributor.authorTong, HHY-
dc.contributor.authorChow, SF-
dc.date.accessioned2021-11-12T13:36:32Z-
dc.date.available2021-11-12T13:36:32Z-
dc.date.issued2021-
dc.identifier.citationInternational Journal of Pharmaceutics, 2021, v. 610, p. article no. 121239-
dc.identifier.issn0378-5173-
dc.identifier.urihttp://hdl.handle.net/10722/307701-
dc.description.abstractThe present study aimed to investigate how cocrystal solution-state stability may affect the polymorphic drug formation and transition during dissolution. In this work, curcumin-resorcinol (CUR-RES), curcumin-hydroquinone (CUR-HYQ) and curcumin-phloroglucinol (CUR-PHL) cocrystals were employed for dissolution studies in three buffer systems to study the effects of solvent and cocrystal thermodynamic stability. The undissolved solids were collected at designed time points and characterized by powder X-ray diffraction, differential scanning calorimetry and scanning electron microscopy. In pH 1.2 buffer, three cocrystals generated > 94% of metastable CUR form III with trace amount of stable CUR form I, while the phase purity of CUR form III recrystallized from buffers containing ethanol (EtOH) were decreased dramatically. For the same cocrystal, the cocrystal form maintained longer in the pH 1.2 buffer when compared with buffers containing EtOH. The phase purity of recrystallized CUR form III in the metastable cocrystal systems followed a linear relationship against CUR solubility, while the thermodynamically stable cocrystal resulted in a non-linear relationship. Due to different intermolecular interactions analyzed by 1H NMR, the stable cocrystal required a higher supersaturation level to precipitate pure CUR form III, in comparison to two metastable cocrystals. Our study offers important insights into mitigating the risk of recrystallization of drug polymorphs during cocrystal dissolution and demonstrates the potential use of cocrystals for drug polymorph preparation, both of which are crucial to the pharmaceutical cocrystal development and reformulation of existing drugs.-
dc.languageeng-
dc.publisherElsevier BV. The Journal's web site is located at http://www.elsevier.com/locate/ijpharm-
dc.relation.ispartofInternational Journal of Pharmaceutics-
dc.subjectCocrystal solution-state stability-
dc.subjectPolymorphism-
dc.subjectCurcumin-
dc.subjectSupersaturation-
dc.subjectCocrystal dissociation-
dc.titleImpact of cocrystal solution-state stability on cocrystal dissociation and polymorphic drug recrystallization during dissolution-
dc.typeArticle-
dc.identifier.emailWong, KC: kcwong47@hku.hk-
dc.identifier.emailTong, HHY: henry002@hku.hk-
dc.identifier.emailChow, SF: asfchow@hku.hk-
dc.identifier.authorityChow, SF=rp02296-
dc.description.naturelink_to_subscribed_fulltext-
dc.identifier.doi10.1016/j.ijpharm.2021.121239-
dc.identifier.pmid34742828-
dc.identifier.scopuseid_2-s2.0-85118888023-
dc.identifier.hkuros330400-
dc.identifier.volume610-
dc.identifier.spagearticle no. 121239-
dc.identifier.epagearticle no. 121239-
dc.identifier.isiWOS:000718955600005-
dc.publisher.placeNetherlands-

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