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Inclusion Complexes of Cyproterone Acetate with Cyclodextrins in Aqueous Solution
Henry de Hassonville, Sandrine; Perly, Bruno; Piel, Géraldine et al.
2002In Journal of Inclusion Phenomena and Macrocyclic Chemistry, 44, p. 289-292
Peer reviewed
 

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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.
Disciplines :
Pharmacy, pharmacology & toxicology
Author, co-author :
Henry de Hassonville, Sandrine
Perly, Bruno
Piel, Géraldine ;  Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique et magistrale
Van Hees, Thierry ;  Université de Liège - ULiège > Département de pharmacie > Pharmacie clinique et pharmacie hospitalière
Delattre, Luc ;  Université de Liège - ULiège > Département de pharmacie > Département de pharmacie
Evrard, Brigitte  ;  Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique
Language :
English
Title :
Inclusion Complexes of Cyproterone Acetate with Cyclodextrins in Aqueous Solution
Publication date :
2002
Event name :
11th International Cyclodextrin Symposium
Event place :
Reyjavik, Iceland
Audience :
International
Journal title :
Journal of Inclusion Phenomena and Macrocyclic Chemistry
ISSN :
1388-3127
eISSN :
1573-1111
Publisher :
Kluwer Academic Publishers, Netherlands
Volume :
44
Pages :
289-292
Peer reviewed :
Peer reviewed
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