title: Physicochemical characterization and in vivo evaluation of flurbiprofen-loaded solid dispersion without crystalline change.
abstract: To develop a novel flurbiprofen-loaded solid dispersion without crystalline change, various flurbiprofen-loaded solid dispersions were prepared with water, sodium carboxylmethyl cellulose (Na-CMC), and Tween 80. The effect of Na-CMC and Tween 80 on aqueous solubility of flurbiprofen was investigated. The physicochemical properties of solid dispersions were investigated using SEM, DSC, and X-ray diffraction. The dissolution and bioavailability in rats were evaluated compared to commercial product. Unlike conventional solid dispersion systems, the flurbiprofen-loaded solid dispersion gave a relatively rough surface and changed no crystalline form of drug. These solid dispersions were formed by attaching hydrophilic carriers to the surface of drug without crystal change, resulting in changing the hydrophobic drug to hydrophilic form. Furthermore, the flurbiprofen-loaded solid dispersion at the weight ratio of flurbiprofen/Na-CMC/Tween 80 of 6/2.5/0.5 improved ~60-fold drug solubility. It gave higher AUC, T(max), and C(max) compared to commercial product. The solid dispersion improved almost 1.5-fold bioavailability of drug compared to commercial product in rats. Thus, the flurbiprofen-loaded solid dispersion would be useful to deliver poorly water-soluble flurbiprofen with enhanced bioavailability without crystalline change.
authors: College of Pharmacy, Yeungnam University, 214-1 Dae-Dong, Gyongsan 712-749, South Korea.
authors: Dong Hoon
authors: DH
authors: Oh
authors: Young-Joon
authors: YJ
authors: Park
authors: Jun Heok
authors: JH
authors: Kang
authors: Chul Soon
authors: CS
authors: Yong
authors: Han-Gon
authors: HG
authors: Choi
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry* / Q000493:pharmacokinetics; D019540:Area Under Curve; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D002266:Carboxymethylcellulose Sodium / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004304:Dosage Forms; D004337:Drug Carriers / Q000737:chemistry* / Q000493:pharmacokinetics; D005480:Flurbiprofen / Q000737:chemistry* / Q000493:pharmacokinetics; D057927:Hydrophobic and Hydrophilic Interactions; D050866:Liquid Crystals / Q000737:chemistry; D008297:Male; D008855:Microscopy, Electron, Scanning; D011136:Polysorbates / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013607:Tablets / Q000138:chemical synthesis / Q000737:chemistry; D014867:Water / Q000737:chemistry; D014961:X-Ray Diffraction
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004304:Dosage Forms; D004337:Drug Carriers; D011136:Polysorbates; D013607:Tablets; D014867:Water; D005480:Flurbiprofen; D002266:Carboxymethylcellulose Sodium