{"title":"利用先进的营养保健品共聚物阐明氟康唑的结晶过程，从而改进配方策略","authors":"Payal Vithlapara, Malaykumar Chotaliya, Dhaval Mori, Kiran Dudhat","doi":"10.1007/s12247-024-09848-4","DOIUrl":null,"url":null,"abstract":"<div><h3>Introduction</h3><p>This current research reports the synthesis and characterization of a cocrystal of Fluconazole (FLU), a widely used antifungal drug, with a nutraceutical coformer (NCF) that has potential health benefits as well as improving its solubility and antifungal activity.</p><h3>Method</h3><p>The co-crystal was obtained by solvent evaporation in a stoichiometric ratio using three natural coformers: Ferulic acid, caffeic acid, and glycerine, and characterized by various analytical techniques, including Powder x-ray diffraction (PXRD), Differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) spectroscopy.</p><h3>Results</h3><p>The cocrystals showed lower heats of fusion (ΔH) compared to pure Fluconazole, indicating the possibility of increased entropy and solubility for all cocrystals. Using the solvent evaporation method with ferulic acid, caffeic acid, and glycine showed significant enhancement of solubility, ranging from 1.06-fold to 4.80-fold, depending on the co-former and different media used.</p><h3>Discussion and Conclusion</h3><p>The zone of inhibition assay showed that cocrystals of Fluconazole with nutraceuticals (FLU+CAF, FLU+GLY, and FLU+FER) exhibited higher zones of inhibition compared to pure Fluconazole and DMSO control. Solubility and dissolution studies revealed that cocrystals of Fluconazole with nutraceutical coformers could be an effective approach to enhancing the solubility and antifungal activity of Fluconazole.</p><h3>Graphical Abstract</h3>\n<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"19 4","pages":""},"PeriodicalIF":2.7000,"publicationDate":"2024-06-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Elucidating of Fluconazole Cocrystallization With a Cutting-Edge Nutraceutical Coformer for Enhanced Formulation Strategies\",\"authors\":\"Payal Vithlapara, Malaykumar Chotaliya, Dhaval Mori, Kiran Dudhat\",\"doi\":\"10.1007/s12247-024-09848-4\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><h3>Introduction</h3><p>This current research reports the synthesis and characterization of a cocrystal of Fluconazole (FLU), a widely used antifungal drug, with a nutraceutical coformer (NCF) that has potential health benefits as well as improving its solubility and antifungal activity.</p><h3>Method</h3><p>The co-crystal was obtained by solvent evaporation in a stoichiometric ratio using three natural coformers: Ferulic acid, caffeic acid, and glycerine, and characterized by various analytical techniques, including Powder x-ray diffraction (PXRD), Differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) spectroscopy.</p><h3>Results</h3><p>The cocrystals showed lower heats of fusion (ΔH) compared to pure Fluconazole, indicating the possibility of increased entropy and solubility for all cocrystals. Using the solvent evaporation method with ferulic acid, caffeic acid, and glycine showed significant enhancement of solubility, ranging from 1.06-fold to 4.80-fold, depending on the co-former and different media used.</p><h3>Discussion and Conclusion</h3><p>The zone of inhibition assay showed that cocrystals of Fluconazole with nutraceuticals (FLU+CAF, FLU+GLY, and FLU+FER) exhibited higher zones of inhibition compared to pure Fluconazole and DMSO control. Solubility and dissolution studies revealed that cocrystals of Fluconazole with nutraceutical coformers could be an effective approach to enhancing the solubility and antifungal activity of Fluconazole.</p><h3>Graphical Abstract</h3>\\n<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>\",\"PeriodicalId\":656,\"journal\":{\"name\":\"Journal of Pharmaceutical Innovation\",\"volume\":\"19 4\",\"pages\":\"\"},\"PeriodicalIF\":2.7000,\"publicationDate\":\"2024-06-25\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Pharmaceutical Innovation\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://link.springer.com/article/10.1007/s12247-024-09848-4\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Pharmaceutical Innovation","FirstCategoryId":"3","ListUrlMain":"https://link.springer.com/article/10.1007/s12247-024-09848-4","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Elucidating of Fluconazole Cocrystallization With a Cutting-Edge Nutraceutical Coformer for Enhanced Formulation Strategies
Introduction
This current research reports the synthesis and characterization of a cocrystal of Fluconazole (FLU), a widely used antifungal drug, with a nutraceutical coformer (NCF) that has potential health benefits as well as improving its solubility and antifungal activity.
Method
The co-crystal was obtained by solvent evaporation in a stoichiometric ratio using three natural coformers: Ferulic acid, caffeic acid, and glycerine, and characterized by various analytical techniques, including Powder x-ray diffraction (PXRD), Differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) spectroscopy.
Results
The cocrystals showed lower heats of fusion (ΔH) compared to pure Fluconazole, indicating the possibility of increased entropy and solubility for all cocrystals. Using the solvent evaporation method with ferulic acid, caffeic acid, and glycine showed significant enhancement of solubility, ranging from 1.06-fold to 4.80-fold, depending on the co-former and different media used.
Discussion and Conclusion
The zone of inhibition assay showed that cocrystals of Fluconazole with nutraceuticals (FLU+CAF, FLU+GLY, and FLU+FER) exhibited higher zones of inhibition compared to pure Fluconazole and DMSO control. Solubility and dissolution studies revealed that cocrystals of Fluconazole with nutraceutical coformers could be an effective approach to enhancing the solubility and antifungal activity of Fluconazole.
期刊介绍：
The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories:
Materials science,
Product design,
Process design, optimization, automation and control,
Facilities; Information management,
Regulatory policy and strategy,
Supply chain developments ,
Education and professional development,
Journal of Pharmaceutical Innovation publishes four issues a year.
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