Influence of cyclodextrin complexation on the physicochemical and biopharmaceutical properties of ketoconazole

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

Research output: Contribution to journalArticle

15 Citations (Scopus)

Abstract

The effects of hydroxypropyl-β-cyclodextrin and methyl-β- cyclodextrin on the solubility of ketoconazole were studied. Products were prepared by physical mixing, kneading and spray-drying methods in four molecular ratios. Kneaded products in a ratio of drug: cyclodextrin (1:2) and spray-dried products showed the highest dissolution rate. Phase solubility diagrams of ketoconazole with these cyclodextrins at 25°C in water and simulated intestinal medium were constructed. A solubility diagram of AL type was obtained with hydroxypropyl-β-cyclodextrin, and Ap type with methyl-β- cyclodextrin. 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. The particle size of ketoconazole (70 ∼ μm) is reduced to 12 μm by the preparation of spray-dried products. As the solubilty in water increased, the partition coefficient, surface tension and wetting angle values decreased. Ketoconazole needed more energy for dissolution compared to the products. In order to examine complex formation thermal methods were used.

Original languageEnglish
Pages (from-to)15-23
Number of pages9
JournalJournal of Inclusion Phenomena
Volume47
Issue number1-2
DOIs
Publication statusPublished - Oct 2003

Fingerprint

biopharmaceuticals
ketoconazole
Ketoconazole
cyclodextrins
Cyclodextrins
Complexation
Solubility
solubility
sprayers
products
dissolving
diagrams
Water
water
Dissolution
Hot Temperature
kneading
heat
Povidone
Spray 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

Influence of cyclodextrin complexation on the physicochemical and biopharmaceutical properties of ketoconazole. / Taneri, Filiz; Güneri, Tamer; Aigner, Z.; Kata, Michael.

In: Journal of Inclusion Phenomena, Vol. 47, No. 1-2, 10.2003, p. 15-23.

Research output: Contribution to journalArticle

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