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New Lidocaine-Based Pharmaceutical Cocrystals: Preparation, Characterization, and Influence of the Racemic vs. Enantiopure Coformer on the Physico-Chemical Properties

hal.structure.identifierUnité de Technologies Chimiques et Biologiques pour la Santé [UTCBS - UM 4 (UMR 8258 / U1267)]
dc.contributor.authorMA, Panpan
hal.structure.identifierInstitut Galien Paris-Saclay [IGPS]
dc.contributor.authorTOUSSAINT, Balthazar
hal.structure.identifierUnité de Technologies Chimiques et Biologiques pour la Santé [UTCBS - UM 4 (UMR 8258 / U1267)]
dc.contributor.authorROBERTI, Enrica Angela
hal.structure.identifierUnité de Technologies Chimiques et Biologiques pour la Santé [UTCBS - UM 4 (UMR 8258 / U1267)]
dc.contributor.authorSCORNET, Noémie
hal.structure.identifierUnité de Technologies Chimiques et Biologiques pour la Santé [UTCBS - UM 4 (UMR 8258 / U1267)]
dc.contributor.authorSANTOS SILVA, Axel
hal.structure.identifierUnité de Technologies Chimiques et Biologiques pour la Santé [UTCBS - UM 4 (UMR 8258 / U1267)]
dc.contributor.authorCASTILLO HENRÍQUEZ, Luis
hal.structure.identifierUniversité Paris Cité [UPCité]
dc.contributor.authorCADASSE, Monique
hal.structure.identifierLaboratoire Ondes et Matière d'Aquitaine [LOMA]
dc.contributor.authorNÉGRIER, Philippe
hal.structure.identifierInstitut Européen de Chimie et Biologie [IECB]
dc.contributor.authorMASSIP, Stéphane
hal.structure.identifierCibles Thérapeutiques et conception de médicaments [CiTCoM - UMR 8038]
dc.contributor.authorDUFAT, Hanh
hal.structure.identifierCibles Thérapeutiques et conception de médicaments [CiTCoM - UMR 8038]
dc.contributor.authorHAMMAD, Karim
hal.structure.identifierUniversità degli Studi di Modena e Reggio Emilia = University of Modena and Reggio Emilia [UNIMORE]
dc.contributor.authorBARALDI, Cecilia
hal.structure.identifierUniversità degli Studi di Modena e Reggio Emilia = University of Modena and Reggio Emilia [UNIMORE]
dc.contributor.authorGAMBERINI, Maria Cristina
hal.structure.identifierUnité de Technologies Chimiques et Biologiques pour la Santé [UTCBS - UM 4 (UMR 8258 / U1267)]
dc.contributor.authorRICHARD, Cyrille
hal.structure.identifierCentre Interdisciplinaire de Nanoscience de Marseille [CINaM]
dc.contributor.authorVEESLER, Stéphane
hal.structure.identifierUnité de Technologies Chimiques et Biologiques pour la Santé [UTCBS - UM 4 (UMR 8258 / U1267)]
dc.contributor.authorESPEAU, Philippe
hal.structure.identifierNational Central University [Taiwan] [NCU]
dc.contributor.authorLEE, Tu
hal.structure.identifierUnité de Technologies Chimiques et Biologiques pour la Santé [UTCBS - UM 4 (UMR 8258 / U1267)]
dc.contributor.authorCORVIS, Yohann
dc.date.created2023-03-29
dc.date.issued2023
dc.identifier.issn1999-4923
dc.description.abstractEnThis study describes the preparation, characterization, and influence of the enantiopure vs. racemic coformer on the physico-chemical properties of a pharmaceutical cocrystal. For that purpose, two new 1:1 cocrystals, namely lidocaine:dl-menthol and lidocaine:d-menthol, were prepared. The menthol racemate-based cocrystal was evaluated by means of X-ray diffraction, infrared spectroscopy, Raman, thermal analysis, and solubility experiments. The results were exhaustively compared with the first menthol-based pharmaceutical cocrystal, i.e., lidocaine:l-menthol, discovered in our group 12 years ago. Furthermore, the stable lidocaine/dl-menthol phase diagram has been screened, thoroughly evaluated, and compared to the enantiopure phase diagram. Thus, it has been proven that the racemic vs. enantiopure coformer leads to increased solubility and improved dissolution of lidocaine due to the low stable form induced by menthol molecular disorder in the lidocaine:dl-menthol cocrystal. To date, the 1:1 lidocaine:dl-menthol cocrystal is the third menthol-based pharmaceutical cocrystal, after the 1:1 lidocaine:l-menthol and the 1:2 lopinavir:l-menthol cocrystals reported in 2010 and 2022, respectively. Overall, this study shows promising potential for designing new materials with both improved characteristics and functional properties in the fields of pharmaceutical sciences and crystal engineering.
dc.language.isoen
dc.publisherMDPI
dc.subject.enDL-menthol
dc.subject.enphysico-chemical compatibility
dc.subject.enthermodynamic stability
dc.subject.encocrystallization
dc.subject.endissolution kinetics
dc.subject.ensolubility enhancement
dc.subject.ensolid state
dc.subject.encrystal engineering
dc.subject.enlidocaine
dc.title.enNew Lidocaine-Based Pharmaceutical Cocrystals: Preparation, Characterization, and Influence of the Racemic vs. Enantiopure Coformer on the Physico-Chemical Properties
dc.typeArticle de revue
dc.identifier.doi10.3390/pharmaceutics15041102
dc.subject.halChimie/Chimie thérapeutique
dc.subject.halSciences du Vivant [q-bio]/Sciences pharmaceutiques/Médicaments
bordeaux.journalPharmaceutics
bordeaux.page1102
bordeaux.volume15
bordeaux.issue4
bordeaux.peerReviewedoui
hal.identifierhal-04083694
hal.version1
hal.popularnon
hal.audienceInternationale
hal.origin.linkhttps://hal.archives-ouvertes.fr//hal-04083694v1
bordeaux.COinSctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=Pharmaceutics&rft.date=2023&rft.volume=15&rft.issue=4&rft.spage=1102&rft.epage=1102&rft.eissn=1999-4923&rft.issn=1999-4923&rft.au=MA,%20Panpan&TOUSSAINT,%20Balthazar&ROBERTI,%20Enrica%20Angela&SCORNET,%20No%C3%A9mie&SANTOS%20SILVA,%20Axel&rft.genre=article


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