title: Improvement on solubility of fluticasone propionate with cyclodextrins by mechanochemical activation.
abstract: To enhance the solubility and in vitro dissolution of fluticasone propionate (FP), a novel approach was developed with mechanochemical treatment. The order of solubilizing effect of β-CD derivatives was observed as HP-β-CD-SBE-β-CD-β-CD-HE-β-CD, consequently, HP-β-CD showed the highest stability constant. To further improve FP solubility, FP and HP-β-CD were grinded using a roll mill, the optimal conditions, determined through single factor experiments, were as follows: rotation frequency of 60 Hz; milling time of 6h. mass ratio of 1: 7. In comparison with pure FP, a 280-fold increase in solubility and a 2.15-fold higher dissolution rate of ground mixture was obtained. The characterization of FP and HP-β-CD complexes had been analyzed by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD) and fourier transform infrared spectroscopy (FT-IR). The results suggested that the interaction between FP and HP-β-CD was strengthened and an amorphous ground mixture was gained. After stored for 60 days, the ground mixtures were stable both chemically and physically.
authors: Key Laboratory for Green Pharmaceutical Technologies and Related Equipment of Ministry of Education, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou, China.
authors: Jiajia
authors: J
authors: Dai
authors: Key Laboratory for Green Pharmaceutical Technologies and Related Equipment of Ministry of Education, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou, China.
authors: Xianrui
authors: X
authors: Liang
authors: Key Laboratory for Green Pharmaceutical Technologies and Related Equipment of Ministry of Education, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou, China.
authors: Weike
authors: W
authors: Su
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000730:Androstadienes / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D018360:Crystallography, X-Ray; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry*; D000068298:Fluticasone; D005938:Glucocorticoids / Q000737:chemistry*; D007700:Kinetics; D008855:Microscopy, Electron, Scanning; D033362:Powder Diffraction; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D000730:Androstadienes; D005079:Excipients; D005938:Glucocorticoids; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; C093196:SBE4-beta-cyclodextrin; D000068298:Fluticasone