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- Publisher Website: 10.1016/j.ijpharm.2021.121239
- Scopus: eid_2-s2.0-85118888023
- PMID: 34742828
- WOS: WOS:000718955600005
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Article: Impact of cocrystal solution-state stability on cocrystal dissociation and polymorphic drug recrystallization during dissolution
Title | Impact of cocrystal solution-state stability on cocrystal dissociation and polymorphic drug recrystallization during dissolution |
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Authors | |
Keywords | Cocrystal solution-state stability Polymorphism Curcumin Supersaturation Cocrystal dissociation |
Issue Date | 2021 |
Publisher | Elsevier 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? |
Abstract | The 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 Identifier | http://hdl.handle.net/10722/307701 |
ISSN | 2023 Impact Factor: 5.3 2023 SCImago Journal Rankings: 0.954 |
ISI Accession Number ID |
DC Field | Value | Language |
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dc.contributor.author | XUAN, B | - |
dc.contributor.author | Chen, YCS | - |
dc.contributor.author | Wong, KC | - |
dc.contributor.author | Chen, R | - |
dc.contributor.author | Lo, PS | - |
dc.contributor.author | Lakerveld, R | - |
dc.contributor.author | Tong, HHY | - |
dc.contributor.author | Chow, SF | - |
dc.date.accessioned | 2021-11-12T13:36:32Z | - |
dc.date.available | 2021-11-12T13:36:32Z | - |
dc.date.issued | 2021 | - |
dc.identifier.citation | International Journal of Pharmaceutics, 2021, v. 610, p. article no. 121239 | - |
dc.identifier.issn | 0378-5173 | - |
dc.identifier.uri | http://hdl.handle.net/10722/307701 | - |
dc.description.abstract | The 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.language | eng | - |
dc.publisher | Elsevier BV. The Journal's web site is located at http://www.elsevier.com/locate/ijpharm | - |
dc.relation.ispartof | International Journal of Pharmaceutics | - |
dc.subject | Cocrystal solution-state stability | - |
dc.subject | Polymorphism | - |
dc.subject | Curcumin | - |
dc.subject | Supersaturation | - |
dc.subject | Cocrystal dissociation | - |
dc.title | Impact of cocrystal solution-state stability on cocrystal dissociation and polymorphic drug recrystallization during dissolution | - |
dc.type | Article | - |
dc.identifier.email | Wong, KC: kcwong47@hku.hk | - |
dc.identifier.email | Tong, HHY: henry002@hku.hk | - |
dc.identifier.email | Chow, SF: asfchow@hku.hk | - |
dc.identifier.authority | Chow, SF=rp02296 | - |
dc.description.nature | link_to_subscribed_fulltext | - |
dc.identifier.doi | 10.1016/j.ijpharm.2021.121239 | - |
dc.identifier.pmid | 34742828 | - |
dc.identifier.scopus | eid_2-s2.0-85118888023 | - |
dc.identifier.hkuros | 330400 | - |
dc.identifier.volume | 610 | - |
dc.identifier.spage | article no. 121239 | - |
dc.identifier.epage | article no. 121239 | - |
dc.identifier.isi | WOS:000718955600005 | - |
dc.publisher.place | Netherlands | - |