title: Improving glyburide solubility and dissolution by complexation with hydroxybutenyl-beta-cyclodextrin.
abstract: OBJECTIVE
  Glyburide, an important drug for type 2 diabetes, has extremely poor aqueous solubility and resulting low bioavailability. This study describes the ability of hydroxybutenyl-beta-cyclodextrin (HBenBCD) to form complexes with glyburide, with enhanced solubility and dissolution rate in vitro.
  
  
  METHODS
  Glyburide and glyburide-HBenBCD were evaluated in various test media known to simulate human gastrointestinal conditions in the fasted and fed states, respectively.
  
  
  RESULTS
  At approximately 14 wt% drug load, in the presence of HBenBCD, an almost 400-fold increase in glyburide aqueous solubility was observed. In the presence of HBenBCD, glyburide solubility was also significantly improved in all physiologically relevant test media. Subsequent dissolution experiments confirmed the solubility study results; the dissolution rate and total amount of drug released were significantly increased.
  
  
  CONCLUSIONS
  Complexation with HBenBCD may be an effective way to increase the bioavailability of glyburide.
authors.affiliation: Goethe University, Institute of Pharmaceutical Technology, Frankfurt/Main, Germany. sandra.klein@em.uni-frankfurt.de
authors.forename: Sandra
authors.initials: S
authors.lastname: Klein
authors.forename: Michael F
authors.initials: MF
authors.lastname: Wempe
authors.forename: Thomas
authors.initials: T
authors.lastname: Zoeller
authors.forename: Norma L
authors.initials: NL
authors.lastname: Buchanan
authors.forename: Juanelle L
authors.initials: JL
authors.lastname: Lambert
authors.forename: Michael G
authors.initials: MG
authors.lastname: Ramsey
authors.forename: Kevin J
authors.initials: KJ
authors.lastname: Edgar
authors.forename: Charles M
authors.initials: CM
authors.lastname: Buchanan
mesh_terms: D002214:Capsules / Q000737:chemistry; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D004055:Differential Thermal Analysis / Q000379:methods; D005750:Gastric Juice / Q000737:chemistry; D005780:Gelatin / Q000737:chemistry; D005905:Glyburide / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D004364:Pharmaceutical Preparations / Q000138:chemical synthesis / Q000737:chemistry; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods; D013696:Temperature; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D002214:Capsules; D004364:Pharmaceutical Preparations; D047392:beta-Cyclodextrins; D005780:Gelatin; D005905:Glyburide