The effect of supercritical CO2 as a reversible plasticizer and foaming agent on the hot stage extrusion of itraconazole with EC 20 cps

被引:37
作者
Verreck, Geert
Decorte, Annelies
Heymans, Koen
Adriaensen, Jef
Liu, Dehua
Tomasko, David L.
Arien, Albertina
Peeters, Jef
Rombaut, Patrick
Van den Mooter, Guy
Brewster, Marcus E.
机构
[1] Johnson & Johnson Pharmaceut Res & Dev, B-2340 Beerse, Belgium
[2] Ohio State Univ, Dept Chem Engn, Columbus, OH 43210 USA
[3] Katholieke Univ Leuven, Lab Farmacotechnol & Biofarm, B-3000 Louvain, Belgium
关键词
hot stage extrusions; itraconazole; ethylcellulose; solid dispersion; pressurized gas; supercritical fluid;
D O I
10.1016/j.supflu.2006.05.005
中图分类号
O64 [物理化学(理论化学)、化学物理学];
学科分类号
070304 ; 081704 ;
摘要
The aim of the Current research project vias to explore the possibilities of combining pressurized carbon dioxide with hot stage extrusion during manufacturing of solid dispersions of itraconazole and ethylcellulose 20 cps (EC 20 cps), to evaluate the ability of the pressurized gas to act as a reversible plasticizer and to produce a foamed extrudate. The physicochemical characteristics of the extrudates with and without injection of carbon dioxide were evaluated with reference to the morphology of the solid dispersion, release characteristics of the drug, and particle properties. Carbon dioxide acted as a plasticizer for itraconazole/EC 20 cps, reducing the processing temperature during the hot stage extrusion process. The macroscopic morphology changed to a foam-like structure due to expansion of the carbon dioxide at the extrusion die. This resulted in increased specific surface area and porosity and as a consequence milling efficiency was improved. (C) 2006 Elsevier B.V. All rights reserved.
引用
收藏
页码:153 / 162
页数:10
相关论文
共 35 条
[1]   Plasticization of polymers with supercritical carbon dioxide: Experimental determination of glass-transition temperatures [J].
Alessi, P ;
Cortesi, A ;
Kikic, I ;
Vecchione, F .
JOURNAL OF APPLIED POLYMER SCIENCE, 2003, 88 (09) :2189-2193
[2]  
[Anonymous], AM SOC MECH ENG
[3]   Melt extrusion: from process to drug delivery technology [J].
Breitenbach, J .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2002, 54 (02) :107-117
[4]   PLASTICIZATION OF GLASSY-POLYMERS BY CO2 [J].
CHIOU, JS ;
BARLOW, JW ;
PAUL, DR .
JOURNAL OF APPLIED POLYMER SCIENCE, 1985, 30 (06) :2633-2642
[5]   Characterization of ibuprofen as a nontraditional plasticizer of ethyl cellulose [J].
De Brabander, C ;
Van den Mooter, G ;
Vervaet, C ;
Remon, JP .
JOURNAL OF PHARMACEUTICAL SCIENCES, 2002, 91 (07) :1678-1685
[6]   Supercritical carbon dioxide assisted blending of polystyrene and poly(methyl methyacrylate) [J].
Elkovitch, MD ;
Tomasko, DL ;
Lee, LJ .
POLYMER ENGINEERING AND SCIENCE, 1999, 39 (10) :2075-2084
[7]   Effect of supercritical carbon dioxide on morphology development during polymer blending [J].
Elkovitch, MD ;
Lee, LJ ;
Tomasko, DL .
POLYMER ENGINEERING AND SCIENCE, 2000, 40 (08) :1850-1861
[8]   EVALUATION OF HOT-MELT EXTRUSION AS A NEW TECHNIQUE FOR THE PRODUCTION OF POLYMER-BASED PELLETS FOR SUSTAINED-RELEASE CAPSULES CONTAINING HIGH LOADINGS OF FREELY SOLUBLE DRUGS [J].
FOLLONIER, N ;
DOELKER, E ;
COLE, ET .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1994, 20 (08) :1323-1339
[9]   VARIOUS WAYS OF MODULATING THE RELEASE OF DILTIAZEM HYDROCHLORIDE FROM HOT-MELT EXTRUDED SUSTAINED-RELEASE PELLETS PREPARED USING POLYMERIC MATERIALS [J].
FOLLONIER, N ;
DOELKER, E ;
COLE, ET .
JOURNAL OF CONTROLLED RELEASE, 1995, 36 (03) :243-250
[10]   Continuous microcellular polystyrene foam extrusion with supercritical CO2 [J].
Han, XM ;
Koelling, KW ;
Tomasko, DL ;
Lee, LJ .
POLYMER ENGINEERING AND SCIENCE, 2002, 42 (11) :2094-2106