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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REFERENCES
F. Djedaï ni and B. Perly: J. Pharm. Sci. 80, 1157–1161 (1991).
R. Vianna, M.V. Bentley et al.: Int. J. Pharm. 167, 205–213 (1998).
K. Higuchi and K.A. Connors: Adv. Anal. Chem. Instr. 4, 117–212 (1965).
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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