Combining Two Antitubercular Drugs, Clofazimine and 4-Aminosalicylic Acid, in Order to Improve Clofazimine Aqueous Solubility and 4-Aminosalicylic Acid Thermal Stability

BODART, Laurie;DERLET, Amélie;Buol, Xavier;Leyssens, Tom;Wouters, Johan;et.al.
(2020) Journal of Pharmaceutical Sciences — Vol. 109, n° 12, p. 3645-3652 (2020)

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Authors
  • BODART, LaurieUNamur
    Author
  • DERLET, AmélieUNamur
    Author
  • Buol, XavierUCLouvain
    Author
  • Leyssens, TomUCLouvain
    Author
  • Wouters, JohanUNamur
    Author
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Abstract
Four forms of a salt combining two antitubercular drugs, clofazimine and 4-aminosalicylic acid, are reported and the crystal structure of two of these forms are described. TG/DSC analysis of all four forms demonstrate an increase in the temperature at which degradation (upon decarboxylation) occurs in comparison to pure 4-aminosalicylic acid. Water solubility evaluation indicates a significant increase of the amount of clofazimine detected in water (10.26 ± 0.52 mg/mL for form I, 12.27 ± 0.32 mg/mL for form II, 7.15 ± 0.43 mg/mL for form III and 8.50 ± 1.24 mg/mL for form IV) in comparison to pure clofazimine (0.20 ± 0.03 mg/mL)
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BODART, L., DERLET, A., Buol, X., Leyssens, T., TUMANOV, N., & Wouters, J. (2020). Combining Two Antitubercular Drugs, Clofazimine and 4-Aminosalicylic Acid, in Order to Improve Clofazimine Aqueous Solubility and 4-Aminosalicylic Acid Thermal Stability. Journal of Pharmaceutical Sciences, 109(12), 3645-3652. https://doi.org/10.1016/j.xphs.2020.09.024 (Original work published 2020)