Solubilty and dissolution studies of antifungal drug:hydroxybutenyl-β-cyclodextrin complexes

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• 作者：Charles M. Buchanan ; Norma L. Buchanan ; Kevin J. Edgar and Michael G. Ramsey
• 关键词：Antifungal ; Clotrimazole ; Complex ; Dissolution ; Drug ; Hydroxybutenyl ; β ; cyclodextrin ; HBenBCD ; Hetoconazole ; Solubility ; Voriconazole
• 刊名：Cellulose
• 出版年：2007
• 出版时间：February, 2007
• 年：2007
• 卷：14
• 期：1
• 页码：35-47
• 全文大小：281 KB
• 刊物类别：Chemistry and Materials Science
• 刊物主题：Chemistry
  Bioorganic Chemistry
  Physical Chemistry
  Organic Chemistry
  Polymer Sciences
  
• 出版者：Springer Netherlands
• ISSN：1572-882X

文摘

The solubilities of voriconazole, ketoconazole, and clotrimazole with and without hydroxybutenyl-β-cyclodextrin (HBenBCD) in aqueous media were examined. The solubility of these antifungal drugs was significantly improved by complexation with HBenBCD. Both the pH and the type of buffer used to adjust the medium pH had a very significant effect on drug solubilities and the apparent binding constants of the drug:cyclodextrin complexes. Additionally, the stereochemistry of tartrate buffers was found to influence both the electrostatic interaction between drug and tartrate as well as complexation of the drug-tartrate aggregate by HBenBCD. We also compared the solubilization of these antifungal drugs by HBenBCD to other cyclodextrin derivatives with different substituents under identical experimental conditions and found that the amount of drug solubilized was in some cases influenced strongly by the nature of the cyclodextrin. Solid antifungal drug:HBenBCD complexes were prepared and their dissolution profiles were obtained which showed that HBenBCD improved both the rate of dissolution and the amount of drug dissolved.