Dissolution enhancement of poorly water-soluble APIs processed by hot-melt extrusion using hydrophilic polymers
作者： M. Maniruzzaman , M. M. Rana , J. S. Boateng , J. C. Mitchell , D. Douroumis
DOI: 10.3109/03639045.2012.670642
关键词:
摘要: The aim of this study was to investigate the efficiency hydrophilic polymers enhance dissolution rate poorly water-soluble active pharmaceutical ingredients (APIs) processed by hot-melt extrusion (HME). Indomethacin (INM) and famotidine (FMT) were selected as model substances while polyvinyl caprolactam graft copolymer, soluplus (SOL) vinylpyrrolidone-vinyl acetate copolymer grades, Kollidon VA64 (VA64) Plasdone S630 (S630) used polymeric carriers. For purpose study, drug–polymer binary blends at various ratios a Randcastle single screw extruder. physicochemical properties morphology extrudates evaluated through X-ray diffraction (XRD), differential scanning calorimetry (DSC) electron microscopy (SEM). Increased drug loadings up 40% achieved in extruded formulations for both drugs. INM FMT exhibited strong plasticization effects with increasing concentrations found be molecularly dispersed within polymer blends. vitro studies showed increased INM/FMT release rates all compared that pure APIs alone.
sussex.ac.uk
gre.ac.uk
informahealthcare.com参考文章(29)
Jessica Albers, Hot-melt extrusion with poorly soluble drugs Deutsche Nationalbibliothek. ,(2008)
Gordon L. Amidon, Hans Lennernäs, Vinod P. Shah, John R. Crison, A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo Bioavailability Pharmaceutical Research. ,vol. 12, pp. 413- 420 ,(1995) , 10.1023/A:1016212804288
Sheng Qi, Andreas Gryczke, Peter Belton, Duncan Q.M. Craig, Characterisation of solid dispersions of paracetamol and EUDRAGIT E prepared by hot-melt extrusion using thermal, microthermal and spectroscopic analysis. International Journal of Pharmaceutics. ,vol. 354, pp. 158- 167 ,(2008) , 10.1016/J.IJPHARM.2007.11.048
P.B. Deasy, M.F.L. Law, Use of extrusion-spheronization to develop an improved oral dosage form of indomethacin International Journal of Pharmaceutics. ,vol. 148, pp. 201- 209 ,(1997) , 10.1016/S0378-5173(96)04846-6
Karel Six, Tinne Daems, Jan de Hoon, Anne Van Hecken, Marleen Depre, Marie-Paule Bouche, Paul Prinsen, Geert Verreck, Jef Peeters, Marcus E. Brewster, Guy Van den Mooter, Clinical study of solid dispersions of itraconazole prepared by hot-stage extrusion European Journal of Pharmaceutical Sciences. ,vol. 24, pp. 179- 186 ,(2005) , 10.1016/J.EJPS.2004.10.005
Charles M. Hansen, The Universality of the Solubility Parameter Industrial & Engineering Chemistry Product Research and Development. ,vol. 8, pp. 2- 11 ,(1969) , 10.1021/I360029A002
Angus Forster, John Hempenstall, Thomas Rades, Characterization of glass solutions of poorly water-soluble drugs produced by melt extrusion with hydrophilic amorphous polymers. Journal of Pharmacy and Pharmacology. ,vol. 53, pp. 303- 315 ,(2010) , 10.1211/0022357011775532
Soon Wook Hong, Bong Sang Lee, Su Jun Park, Hong Ryeol Jeon, Ki Young Moon, Mean Hyung Kang, Sang Han Park, Sung-Up Choi, Woo Heon Song, Jaehwi Lee, Young Wook Choi, Solid dispersion formulations of megestrol acetate with copovidone for enhanced dissolution and oral bioavailability. Archives of Pharmacal Research. ,vol. 34, pp. 127- 135 ,(2011) , 10.1007/S12272-011-0115-2
Larissa A Wenning, M Gail Murphy, Laura P James, Jeffrey L Blumer, James D Marshall, John Baier, Ann O Scheimann, Deborah L Panebianco, Ling Zhong, Roy Eisenhandler, Kuang C Yeh, Gregory L Kearns, Pharmacokinetics of famotidine in infants. Clinical Pharmacokinectics. ,vol. 44, pp. 395- 406 ,(2005) , 10.2165/00003088-200544040-00004
David J. Greenhalgh, Adrian C. Williams, Peter Timmins, Peter York, Solubility parameters as predictors of miscibility in solid dispersions Journal of Pharmaceutical Sciences. ,vol. 88, pp. 1182- 1190 ,(1999) , 10.1021/JS9900856