title: Spherical crystals of celecoxib to improve solubility, dissolution rate and micromeritic properties.
abstract: Celecoxib spherical agglomerates were prepared with polyvinylpyrrolidone (PVP) using acetone, water and chloroform as solvent, non-solvent and bridging liquid, respectively. The agglomerates were characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), IR spectroscopic studies and scanning electron microscopy (SEM). The IR spectroscopy and DSC results indicated the absence of any interactions between drug and additives. XRD studies showed a decrease in crystallinity in agglomerates. The crystals exhibited significantly improved micromeritic properties compared to pure drug. The loading efficiency (% or mg drug per 100 mg crystals) was in the range of 93.9 +/- 2.3 and 97.3 +/- 1.3% (n = 3) with all formulations. The aqueous solubility and dissolution rate of the drug from crystals was significantly (p < 0.05) increased (nearly two times). The solubility and in vitro drug release rates increased with an increase in PVP concentration (from 2.5 to 10%). The SEM studies showed that the crystal posseses a good spherical shape with smooth and regular surface.
authors.affiliation: Department of Pharmaceutics, N.E.T. Pharmacy College, Navodaya Nagar, Mantralayam Road, Raichur-584103, India. vrmgupta_05@yahoo.co.in
authors.forename: Venkadari Rammohan
authors.initials: VR
authors.lastname: Gupta
authors.forename: Srinivas
authors.initials: S
authors.lastname: Mutalik
authors.forename: Madhobhai M
authors.initials: MM
authors.lastname: Patel
authors.forename: Girish K
authors.initials: GK
authors.lastname: Jani
mesh_terms: D002152:Calorimetry, Differential Scanning; D000068579:Celecoxib; D002626:Chemistry, Pharmaceutical; D003460:Crystallization / Q000379:methods; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics; D007700:Kinetics; D008747:Methylcellulose / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D010592:Pharmaceutic Aids / Q000737:chemistry; D011208:Powders / Q000737:chemistry; D011720:Pyrazoles / Q000737:chemistry* / Q000493:pharmacokinetics*; D012995:Solubility; D013055:Spectrophotometry, Infrared; D013449:Sulfonamides / Q000737:chemistry* / Q000493:pharmacokinetics*; D013678:Technology, Pharmaceutical / Q000379:methods*; D014867:Water; D014961:X-Ray Diffraction
chemical_list: D016861:Cyclooxygenase Inhibitors; D010592:Pharmaceutic Aids; D011208:Powders; D011720:Pyrazoles; D013449:Sulfonamides; D014867:Water; D008747:Methylcellulose; D000068579:Celecoxib