Abstract :
[en] 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 the 2,6-dimethyl-β-CD (DIMEB) was shown by 1H-NMR and t-ROESY spectra.
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