Evaluation of polar lipid-hydrophilic polymer microparticles

被引:46
作者
Savolainen, M
Herder, J
Khoo, C
Lövqvist, K
Dahlqvist, C
Glad, H
Juppo, AM
机构
[1] Univ Helsinki, Pharmaceut Technol Div, Dept Pharm, FIN-00014 Helsinki, Finland
[2] AstraZeneca R&D Molndal, SE-43183 Molndal, Sweden
[3] Chalmers Univ Technol, Dept Mat & Surface Chem, SE-41296 Gothenburg, Sweden
关键词
controlled release; felodipine; hydrophilic polymer; polar lipid; solid dispersion; spray chilling;
D O I
10.1016/S0378-5173(03)00336-3
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The aim of the present study was to prepare controlled-release tablets of poorly-soluble drug, felodipine. Spray chilling was used to formulate the drug, the polar lipids and the hydrophilic polymers into solid dispersion microparticles, which were then compressed. The microparticles were characterised by Fourier transform infrared and Raman spectroscopies, X-ray powder diffraction, hot-stage microscopy, scanning electron microscopy, and image analysis. The crystallinity of felodipine had decreased in all the samples, and the amount of crystalline felodipine varied depending on the composition of the solid dispersion. The particles were spherical with the median particle diameter ranging from 20 to 35 mum. The addition of hydrophilic polymer into the matrix widened the particle size distribution and increased the amount of agglomerates. Most promising dissolution patterns were obtained from tablets containing glycerides e.g. from Precirol((R)) ATO 5/Pluronic((R)) F 127 tablets the release was of zero order. (C) 2003 Elsevier B.V. All rights reserved.
引用
收藏
页码:47 / 62
页数:16
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