title: Slow-release of famotidine from tablets consisting of chitosan/sulfobutyl ether β-cyclodextrin composites.
abstract: An intermolecular complex formed from a 1:1 weight ratio of chitosan (CS, molecular weight 30 kDa) and sulfobutyl ether β-cyclodextrin (SBE-β-CyD, degree of substitution 7) was less soluble than either of the original components. The release of famotidine from tablets composed of a simple mixture of CS and SBE-β-CyD is slower in media at pH 1.2 than at 6.8. Macroscopic observation of tablets and a kinetic analysis of release profiles suggested that, at pH 1.2, the drug was slowly released from the less-soluble CS/SBE-β-CyD complex formed on the surface of the tablet immediately after exposure to water, accompanied by the dissolution of the interpolymer complex and, ultimately, the erosion and disintegration of the tablet. In the case of the medium at pH 6.8, the formation of a gel by CS was the cause of the slow release, especially for CS/SBE-β-CyD tablets which were significantly gelated and both the diameter and thickness of the tablet had expanded. The in vitro slow releasing characteristic of the CS/SBE-β-CyD tablet was reflected in the in vivo absorption of the drug after oral administration to rats. These results suggest that a simple mixing of CS and SBE-β-CyD is potentially useful for the controlled release of a drug.
authors.affiliation: Faculty of Pharmaceutical Sciences, Sojo University, 4-22-1 Ikeda, Nishi-Ku, Kumamoto 860-0082, Japan.
authors.forename: Makoto
authors.initials: M
authors.lastname: Anraku
authors.affiliation: Faculty of Pharmaceutical Sciences, Sojo University, 4-22-1 Ikeda, Nishi-Ku, Kumamoto 860-0082, Japan.
authors.forename: Ayumu
authors.initials: A
authors.lastname: Hiraga
authors.affiliation: Faculty of Pharmaceutical Sciences, Sojo University, 4-22-1 Ikeda, Nishi-Ku, Kumamoto 860-0082, Japan.
authors.forename: Daisuke
authors.initials: D
authors.lastname: Iohara
authors.affiliation: New Product Development Ligand Pharmaceuticals Inc., 2029 Becker Drive, Suite 217 Lawrence, KS 66047, USA.
authors.forename: James D
authors.initials: JD
authors.lastname: Pipkin
authors.affiliation: DDS Research Institute, Sojo University, 4-22-1 Ikeda, Nishi-Ku, Kumamoto 860-0082, Japan.
authors.forename: Kaneto
authors.initials: K
authors.lastname: Uekama
authors.affiliation: Faculty of Pharmaceutical Sciences, Sojo University, 4-22-1 Ikeda, Nishi-Ku, Kumamoto 860-0082, Japan. Electronic address: fhira@ph.sojo-u.ac.jp.
authors.forename: Fumitoshi
authors.initials: F
authors.lastname: Hirayama
mesh_terms: D000818:Animals; D000897:Anti-Ulcer Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D048271:Chitosan; D003692:Delayed-Action Preparations; D015738:Famotidine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D005782:Gels; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013607:Tablets; D047392:beta-Cyclodextrins
chemical_list: D000897:Anti-Ulcer Agents; D003692:Delayed-Action Preparations; D005782:Gels; D013607:Tablets; D047392:beta-Cyclodextrins; C093196:SBE4-beta-cyclodextrin; D015738:Famotidine; D048271:Chitosan
keywords: Chitosan; Extending release; Famotidine; Interpolymer complex; Release control; Sulfobutyl ether β-cyclodextrin