title: Improved dissolution and anti-inflammatory effect of ibuprofen by solid dispersion.
abstract: The purpose of this study was to improve the dissolution rate and anti-inflammatory effect of ibuprofen by a solid dispersion (SD) method. Initial screening was developed based on drug solubility in carriers in the liquid state to select a suitable water-soluble carrier system for the preparation of SDs. The dissolution of ibuprofen in urea was higher than in PEG4000 or mannitol. Thus, urea was selected as the carrier for the preparation of SDs. SDs were characterized in terms of dissolution, differential scanning calorimetry (DSC), X-ray diffraction (XRD), scanning electron microscopy (SEM), and Fourier transform infrared (FTIR) spectroscopy. Solid dispersion-based (SDBT) and conventional (CT) tablets were prepared by the wet granulation method. The anti-inflammatory effect of SDBT was evaluated using the mouse ear edema test with xylene. In vitro release results indicated that the ibuprofen dissolution rate was improved by the SD. SD characterization results suggested that ibuprofen partly precipitates in crystalline and amorphous forms after SD preparation and that ibuprofen and urea do not interact. SDBT displayed more significant anti-inflammatory effects than CT. The dissolution rate and anti-inflammatory effect of ibuprofen were significantly enhanced by the ibuprofen-urea SD.
authors.affiliation: College of Marine Life Sciences, Ocean University of China, Qingdao, 266003, China.
authors.forename: Liyuan
authors.initials: L
authors.lastname: Chen
authors.forename: Qifeng
authors.initials: Q
authors.lastname: Dang
authors.forename: Chengsheng
authors.initials: C
authors.lastname: Liu
authors.forename: Jun
authors.initials: J
authors.lastname: Chen
authors.forename: Lei
authors.initials: L
authors.lastname: Song
authors.forename: Xiguang
authors.initials: X
authors.lastname: Chen
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D004195:Disease Models, Animal; D004337:Drug Carriers; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy*; D007052:Ibuprofen / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D008297:Male; D051379:Mice; D008855:Microscopy, Electron, Scanning; D011897:Random Allocation; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014508:Urea; D014961:X-Ray Diffraction; D014992:Xylenes
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D014992:Xylenes; D014508:Urea; D007052:Ibuprofen