title: Enhanced solubility and bioavailability of flurbiprofen by cycloamylose.
abstract: The effect of cycloamylose on the aqueous solubility of flurbiprofen was investigated. To improve the solubility and bioavailability of flurbiprofen (poor water solubility), a solid dispersion was spray dried with a solution of flurbiprofen and cycloamylose at a weight ratio of 1:1. The physicochemical properties of solid dispersions were investigated using SEM, DSC, and X-ray diffraction. The dissolution and bioavailability in rats were evaluated compared with a commercial product. Cycloamylose increased solubility of flurbiprofen approximately 12-fold and dissolution of it by 2-fold. Flurbiprofen was present in an unchanged crystalline state, and cycloamylose was a solubilizing agent for flurbiprofen in this solid dispersion. Furthermore, the dispersion gave higher AUC and C(max) values compared with the commercial product, indicating that it improved the oral bioavailability of flurbiprofen in rats. Thus, the solid dispersion may be useful to deliver flurbiprofen with enhanced bioavailability without changes in crystalline structure.
authors.affiliation: Department of Food Engineering, Dankook University, Cheonan, Korea.
authors.forename: Hyung Hee
authors.initials: HH
authors.lastname: Baek
authors.forename: So Young
authors.initials: SY
authors.lastname: Kwon
authors.forename: Shin-Joung
authors.initials: SJ
authors.lastname: Rho
authors.forename: Won Seok
authors.initials: WS
authors.lastname: Lee
authors.forename: Ho-Joon
authors.initials: HJ
authors.lastname: Yang
authors.forename: Jung-Mi
authors.initials: JM
authors.lastname: Hah
authors.forename: Han-Gon
authors.initials: HG
authors.lastname: Choi
authors.forename: Yong-Ro
authors.initials: YR
authors.lastname: Kim
authors.forename: Chul Soon
authors.initials: CS
authors.lastname: Yong
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D003505:Cyclodextrins / Q000737:chemistry*; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry*; D005480:Flurbiprofen / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics*; D008297:Male; D008855:Microscopy, Electron, Scanning; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013499:Surface Properties; D014961:X-Ray Diffraction
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D003505:Cyclodextrins; D005079:Excipients; D005480:Flurbiprofen