Improvement in the physicochemical properties of ketoconazole through complexation with cyclodextrin derivatives
Küçük Resim Yok
Tarih
2002
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
Highly-soluble cyclodextrin derivatives, such as hydroxypropyl-ß -cyclodextrin (HP-ß-CD) and methyl-ß-cyclodextrin (MEB), were tested as solubilizing agents for ketoconazole, with the aim of improving the physicochemical and biopharmaceutical properties of this lipophilic imidazole antifungal agent. Products were prepared in four molecular ratios by physical mixing, kneading and spray-drying methods. The kneaded products in a ratio of 1:2 and the spray-dried products exhibited the highest dissolution rates. The phase solubility diagrams of ketoconazole with these cyclodextrins at 25°C in water and in simulated intestinal medium were constructed. A solubility diagram of AL type was obtained with HP-ß-CD, and one of A P type with MEB. The complexes were characterized by thermal methods (DSC, TG, DTG and DTA). Multicomponent systems were prepared with tartaric acid. The effects of water-soluble polymers, e.g., polyvinylpyrrolidone, on the aqueous solubility of ketoconazole were investigated. Particle size distribution, surface area, partition coefficient, heat of dissolution and wettability studies were also carried out. The formation of inclusion complexes was observed by means of thermoanalytical studies.
Açıklama
Anahtar Kelimeler
DSC, Hydroxypropyl-ß-cyclodextrin, Inclusion complexation, Ketoconazole, Methyl-ß-cyclodextrin, Partition coefficient, Phase diagrams, Rate of dissolution
Kaynak
Journal of Inclusion Phenomena
WoS Q Değeri
Scopus Q Değeri
N/A
Cilt
44
Sayı
01.Apr
