Impact of Solvent-Mediated Phase Transitions by Artificial Gastrointestinal Buffers on Efavirenz Polymorphs
The implications of various pH solutions in the gastrointestinal fluid system as solvent-mediated phase transitions on concurrent polymorphism transformation, notably metastable polymorphic forms of Efavirenz (EFV), has never been investigated. The impact will be shifting in the solubility and cryst...
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MDPI AG
2025-01-01
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| author | Yoga Windhu Wardhana Eli Nuraisyah Angga Prawira Kautsar Patihul Husni Arif Budiman Anis Yohana Chaerunisaa |
| author_facet | Yoga Windhu Wardhana Eli Nuraisyah Angga Prawira Kautsar Patihul Husni Arif Budiman Anis Yohana Chaerunisaa |
| author_sort | Yoga Windhu Wardhana |
| collection | DOAJ |
| description | The implications of various pH solutions in the gastrointestinal fluid system as solvent-mediated phase transitions on concurrent polymorphism transformation, notably metastable polymorphic forms of Efavirenz (EFV), has never been investigated. The impact will be shifting in the solubility and crystallinity of EFV polymorphisms, particularly metastable Forms II and III. EFV’s metastable form is generated by recrystallization with n-hexane and methanol, which were all immersed in artificial digestion buffer solutions for 10 and 100 h, respectively. Form II showed a 9–13.2% increase in solubility, whereas Form III increased by 2–7.3% over Form I. Interestingly, Form II revealed decreased crystallinity, but Form III tended to retain or slightly increase. In acidic solutions, all metastable polymorphs had the highest solubility and crystallinity. Form III appears to have a lower impact on phase transitions owing to pH variations than Form II. These findings indicate that variability in the pH of digestive secretions are essential steps in developing successful pharmaceutical formulations. Finally, our findings provide information on the complex interaction between solvents, pH variations, and EFV polymorphs. The findings identified the importance of these factors in the development of successful pharmaceutical formulations. |
| format | Article |
| id | doaj-art-bc6ce97268764f9caa89ab79a0955b04 |
| institution | Kabale University |
| issn | 2073-4352 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Crystals |
| spelling | doaj-art-bc6ce97268764f9caa89ab79a0955b042025-01-24T13:28:07ZengMDPI AGCrystals2073-43522025-01-011514810.3390/cryst15010048Impact of Solvent-Mediated Phase Transitions by Artificial Gastrointestinal Buffers on Efavirenz PolymorphsYoga Windhu Wardhana0Eli Nuraisyah1Angga Prawira Kautsar2Patihul Husni3Arif Budiman4Anis Yohana Chaerunisaa5Department of Pharmaceutics and Pharmaceuticals Technology, Faculty of Pharmacy, Universitas Padjadjaran (UNPAD), Sumedang 45363, IndonesiaDepartment of Pharmaceutics and Pharmaceuticals Technology, Faculty of Pharmacy, Universitas Padjadjaran (UNPAD), Sumedang 45363, IndonesiaDepartment of Pharmaceutics and Pharmaceuticals Technology, Faculty of Pharmacy, Universitas Padjadjaran (UNPAD), Sumedang 45363, IndonesiaDepartment of Pharmaceutics and Pharmaceuticals Technology, Faculty of Pharmacy, Universitas Padjadjaran (UNPAD), Sumedang 45363, IndonesiaDepartment of Pharmaceutics and Pharmaceuticals Technology, Faculty of Pharmacy, Universitas Padjadjaran (UNPAD), Sumedang 45363, IndonesiaDepartment of Pharmaceutics and Pharmaceuticals Technology, Faculty of Pharmacy, Universitas Padjadjaran (UNPAD), Sumedang 45363, IndonesiaThe implications of various pH solutions in the gastrointestinal fluid system as solvent-mediated phase transitions on concurrent polymorphism transformation, notably metastable polymorphic forms of Efavirenz (EFV), has never been investigated. The impact will be shifting in the solubility and crystallinity of EFV polymorphisms, particularly metastable Forms II and III. EFV’s metastable form is generated by recrystallization with n-hexane and methanol, which were all immersed in artificial digestion buffer solutions for 10 and 100 h, respectively. Form II showed a 9–13.2% increase in solubility, whereas Form III increased by 2–7.3% over Form I. Interestingly, Form II revealed decreased crystallinity, but Form III tended to retain or slightly increase. In acidic solutions, all metastable polymorphs had the highest solubility and crystallinity. Form III appears to have a lower impact on phase transitions owing to pH variations than Form II. These findings indicate that variability in the pH of digestive secretions are essential steps in developing successful pharmaceutical formulations. Finally, our findings provide information on the complex interaction between solvents, pH variations, and EFV polymorphs. The findings identified the importance of these factors in the development of successful pharmaceutical formulations.https://www.mdpi.com/2073-4352/15/1/48efavirenzmetastable polymorphssolvent-mediated transitionssolubilitycrystallinity indexartificial gastrointestinal buffers |
| spellingShingle | Yoga Windhu Wardhana Eli Nuraisyah Angga Prawira Kautsar Patihul Husni Arif Budiman Anis Yohana Chaerunisaa Impact of Solvent-Mediated Phase Transitions by Artificial Gastrointestinal Buffers on Efavirenz Polymorphs Crystals efavirenz metastable polymorphs solvent-mediated transitions solubility crystallinity index artificial gastrointestinal buffers |
| title | Impact of Solvent-Mediated Phase Transitions by Artificial Gastrointestinal Buffers on Efavirenz Polymorphs |
| title_full | Impact of Solvent-Mediated Phase Transitions by Artificial Gastrointestinal Buffers on Efavirenz Polymorphs |
| title_fullStr | Impact of Solvent-Mediated Phase Transitions by Artificial Gastrointestinal Buffers on Efavirenz Polymorphs |
| title_full_unstemmed | Impact of Solvent-Mediated Phase Transitions by Artificial Gastrointestinal Buffers on Efavirenz Polymorphs |
| title_short | Impact of Solvent-Mediated Phase Transitions by Artificial Gastrointestinal Buffers on Efavirenz Polymorphs |
| title_sort | impact of solvent mediated phase transitions by artificial gastrointestinal buffers on efavirenz polymorphs |
| topic | efavirenz metastable polymorphs solvent-mediated transitions solubility crystallinity index artificial gastrointestinal buffers |
| url | https://www.mdpi.com/2073-4352/15/1/48 |
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