Improvement in the physicochemical properties of ketoconazole through complexation with cyclodextrin derivatives

Filiz Taneri, Tamer Güneri, Z. Aigner, Michael Kata

Research output: Contribution to journalArticle

27 Citations (Scopus)

Abstract

Highly-soluble cyclodextrin derivatives, such as hydroxypropyl-β -cyclodextrin (HP-β-CD) and methyl-β-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-β-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.

Original languageEnglish
Pages (from-to)257-260
Number of pages4
JournalJournal of Inclusion Phenomena
Volume44
Issue number1-4
DOIs
Publication statusPublished - 2002

Fingerprint

ketoconazole
Ketoconazole
cyclodextrins
Cyclodextrins
Complexation
physicochemical properties
solubility
chemical derivatives
sprayers
Solubility
dissolving
products
diagrams
wettability
particle size distribution
imidazoles
Dissolution
water
Hot Temperature
drying

Keywords

  • DSC
  • Hydroxypropyl-β-cyclodextrin
  • Inclusion complexation
  • Ketoconazole
  • Methyl-β-cyclodextrin
  • Partition coefficient
  • Phase diagrams
  • Rate of dissolution

ASJC Scopus subject areas

  • Chemistry(all)
  • Condensed Matter Physics

Cite this

Improvement in the physicochemical properties of ketoconazole through complexation with cyclodextrin derivatives. / Taneri, Filiz; Güneri, Tamer; Aigner, Z.; Kata, Michael.

In: Journal of Inclusion Phenomena, Vol. 44, No. 1-4, 2002, p. 257-260.

Research output: Contribution to journalArticle

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