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Background <p>Bedaquiline fumarate (BDQ) is an anti-tubercular Biopharmaceutics Classification System (BCS class-II) drug &amp; 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.</p> Results <p>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.</p> Conclusion <p>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&#xa0;binding energy of − 1.2&#xa0;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.</p>

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Preparation, characterization, and evaluation of bedaquiline fumarate: ascorbic acid co-crystals with enhanced pharmaceutical and physicochemical properties

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年6月6日

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  • Shital D. Godse,
  • Ranjit B. Mohare,
  • Vishal P. Zambre,
  • Vidhya K. Bhusari,
  • Minal Ghante

摘要

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.