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Inclusion Complexes of Cyproterone Acetate with Cyclodextrins in Aqueous Solution

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Abstract

Cyproterone acetate (CPA) is a steroidal antiandrogen with a progestogenic activity. Given that this molecule has a very poor water solubility (2.1 μg/mL), different cyclodextrins (CDs) were tested to form inclusion complexes and to increase solubility. Two different techniques were compared to study the affinity between CPA and CDs: phase-solubility studies and NMR spectroscopy. The stoichiometry and the stability constant could be determined for most complexes with the aid of phase-solubility studies. The greatest increase in solubility was achieved with the methylated β-CDs, but hydroxypropylated β- and γ-CDs also gave enhanced solubilities. 1H-NMR studies showed a solubility increase similar to that found with phase-solubility studies. The proof of inclusion in the2,6-dimethyl-β-CD (DIMEB) was shown by 1H-NMR and t-ROESY spectra.

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Authors and Affiliations

  1. Service de Chimie Moléculaire, CEA Saclay, F-91191, Gif-sur-Yvette Cedex, France

    Bruno Perly

Authors
  1. Sandrine Henry De Hassonville
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  2. Bruno Perly
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  3. Géraldine Piel
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  4. Thierry Van Hees
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  5. Valéry Barillaro
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  6. Pascal Bertholet
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  7. Luc Delattre
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  8. Brigitte Evrard
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De Hassonville, S.H., Perly, B., Piel, G. et al. Inclusion Complexes of Cyproterone Acetate with Cyclodextrins in Aqueous Solution. Journal of Inclusion Phenomena 44, 289–292 (2002). https://doi.org/10.1023/A:1023099611604

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  • DOI: https://doi.org/10.1023/A:1023099611604

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