Preparation, characterization, and evaluation of bedaquiline fumarate: ascorbic acid co-crystals with enhanced pharmaceutical and physicochemical properties
Abstract Background Bedaquiline fumarate (BDQ) is an anti-tubercular Biopharmaceutics Classification System (BCS class-II) drug & it has very less solubility. Therefore, an effort has been made to prepare the bedaquiline fumarate co-crystal to improve its physicochemical and pharmaceutical chara...
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SpringerOpen
2025-06-01
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| Series: | Future Journal of Pharmaceutical Sciences |
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| Online Access: | https://doi.org/10.1186/s43094-025-00790-x |
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| author | Shital D. Godse Ranjit B. Mohare Vishal P. Zambre Vidhya K. Bhusari Minal Ghante |
| author_facet | Shital D. Godse Ranjit B. Mohare Vishal P. Zambre Vidhya K. Bhusari Minal Ghante |
| author_sort | Shital D. Godse |
| collection | DOAJ |
| description | Abstract Background Bedaquiline fumarate (BDQ) is an anti-tubercular Biopharmaceutics Classification System (BCS class-II) drug & it has very less solubility. Therefore, an effort has been made to prepare the bedaquiline fumarate co-crystal to improve its physicochemical and pharmaceutical characteristics. Results Using the solvent evaporation method, the drug bedaquiline fumarate and co-former ascorbic acid (AA) were co-crystallized. A series of analytical techniques, i.e., X-ray diffraction (XRD), Fourier transformation infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and UV spectroscopy, etc., were used for the analysis of co-crystal to predict co-crystal formation by molecular docking. Micromeritic study and tablet formulation were done of bedaquiline fumarate and co-crystal formulation (1:2) batch. A permeability study was conducted on the chicken ileum. Conclusion Active pharmaceutical ingredients can co-crystallize with other small molecules or co-formers to create new solid dosage forms that have better physicochemical characteristics than pure drugs. 22 co-formers were screened with the drug, ascorbic acid was selected as a co-former because it has a binding energy of − 1.2 kcal/mol, two hydrogen bonds are formed, and it becomes readily soluble in water. This study indicated that ascorbic acid as a co-former can increase the dissolution profile of bedaquiline fumarate by the co-crystallization approach. |
| format | Article |
| id | doaj-art-d9d70b0eebfb4f7292a7f69f0c06ee4d |
| institution | OA Journals |
| issn | 2314-7253 |
| language | English |
| publishDate | 2025-06-01 |
| publisher | SpringerOpen |
| record_format | Article |
| series | Future Journal of Pharmaceutical Sciences |
| spelling | doaj-art-d9d70b0eebfb4f7292a7f69f0c06ee4d2025-08-20T02:30:45ZengSpringerOpenFuture Journal of Pharmaceutical Sciences2314-72532025-06-0111111410.1186/s43094-025-00790-xPreparation, characterization, and evaluation of bedaquiline fumarate: ascorbic acid co-crystals with enhanced pharmaceutical and physicochemical propertiesShital D. Godse0Ranjit B. Mohare1Vishal P. Zambre2Vidhya K. Bhusari3Minal Ghante4Department of Pharmaceutical Quality Assurance, Vishwakarma University School of PharmacyDepartment of Pharmaceutical Chemistry, Smt. Kashibai Navale College of PharmacyDepartment of Pharmaceutical Chemistry, Smt. Kashibai Navale College of PharmacyDepartment of Pharmaceutical Chemistry, Smt. Kashibai Navale College of PharmacyDepartment of Pharmaceutical Chemistry, Smt. Kashibai Navale College of PharmacyAbstract Background Bedaquiline fumarate (BDQ) is an anti-tubercular Biopharmaceutics Classification System (BCS class-II) drug & it has very less solubility. Therefore, an effort has been made to prepare the bedaquiline fumarate co-crystal to improve its physicochemical and pharmaceutical characteristics. Results Using the solvent evaporation method, the drug bedaquiline fumarate and co-former ascorbic acid (AA) were co-crystallized. A series of analytical techniques, i.e., X-ray diffraction (XRD), Fourier transformation infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and UV spectroscopy, etc., were used for the analysis of co-crystal to predict co-crystal formation by molecular docking. Micromeritic study and tablet formulation were done of bedaquiline fumarate and co-crystal formulation (1:2) batch. A permeability study was conducted on the chicken ileum. Conclusion Active pharmaceutical ingredients can co-crystallize with other small molecules or co-formers to create new solid dosage forms that have better physicochemical characteristics than pure drugs. 22 co-formers were screened with the drug, ascorbic acid was selected as a co-former because it has a binding energy of − 1.2 kcal/mol, two hydrogen bonds are formed, and it becomes readily soluble in water. This study indicated that ascorbic acid as a co-former can increase the dissolution profile of bedaquiline fumarate by the co-crystallization approach.https://doi.org/10.1186/s43094-025-00790-xBedaquiline fumarateCo-crystallizationSolubilityFourier transform infrared spectroscopyX-ray diffractometry |
| spellingShingle | Shital D. Godse Ranjit B. Mohare Vishal P. Zambre Vidhya K. Bhusari Minal Ghante Preparation, characterization, and evaluation of bedaquiline fumarate: ascorbic acid co-crystals with enhanced pharmaceutical and physicochemical properties Future Journal of Pharmaceutical Sciences Bedaquiline fumarate Co-crystallization Solubility Fourier transform infrared spectroscopy X-ray diffractometry |
| title | Preparation, characterization, and evaluation of bedaquiline fumarate: ascorbic acid co-crystals with enhanced pharmaceutical and physicochemical properties |
| title_full | Preparation, characterization, and evaluation of bedaquiline fumarate: ascorbic acid co-crystals with enhanced pharmaceutical and physicochemical properties |
| title_fullStr | Preparation, characterization, and evaluation of bedaquiline fumarate: ascorbic acid co-crystals with enhanced pharmaceutical and physicochemical properties |
| title_full_unstemmed | Preparation, characterization, and evaluation of bedaquiline fumarate: ascorbic acid co-crystals with enhanced pharmaceutical and physicochemical properties |
| title_short | Preparation, characterization, and evaluation of bedaquiline fumarate: ascorbic acid co-crystals with enhanced pharmaceutical and physicochemical properties |
| title_sort | preparation characterization and evaluation of bedaquiline fumarate ascorbic acid co crystals with enhanced pharmaceutical and physicochemical properties |
| topic | Bedaquiline fumarate Co-crystallization Solubility Fourier transform infrared spectroscopy X-ray diffractometry |
| url | https://doi.org/10.1186/s43094-025-00790-x |
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