| Autor: | Sandrine Henry De Hassonville, Bruno Perly, Géraldine Piel, Thierry Van Hees, Valéry Barillaro, Pascal Bertholet, Luc Delattre, Brigitte Evrard |
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| Rok vydání: | 2002 |
| Předmět: | |
| Zdroj: | Journal of Inclusion Phenomena and Macrocyclic Chemistry. 44:289-292 |
| ISSN: | 0923-0750 |
| DOI: | 10.1023/a:1023099611604 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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