溶剂变化法制备萘普康球形团聚

P. K. Kulkarni, M. Dixit, Achint Jain
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引用次数: 19

摘要

萘普生是一种消炎药,具有较差的水溶性和流动性。采用溶剂变化法制备球形团聚体。通过构造三元图确定了球团聚用溶剂的组成。萘普生球形凝聚结晶介质为四氢呋喃(良好溶剂);水(不良溶剂);醋酸异丙酯(桥接液)的比例分别为29:61:10。用差示扫描量热法、红外光谱法、x射线衍射法和扫描电镜对球状团块进行了表征。进行了微粒化和溶出行为研究。对桥接液用量、搅拌时间、搅拌时间等工艺参数进行了优化。并与纯样品和再结晶样品进行了溶出形貌比较。球形团聚体结晶度降低,微晶性质改善。由于萘普生的溶出度与粒径或表面积有关,因此与纯样品相比,球形团聚体的溶出度没有提高。关键词:球形团聚体;甲氧萘丙酸;结晶度;解散。DOI: http://dx.doi.org/10.3329/sjps.v4i1.8860 SJPS 2011;4 (1): 1 - 8
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Spherical Agglomeration of Naproxan by Solvent Change Method
Naproxen, an anti-inflammatory drug, exhibits poor water solubility and flow properties. Spherical agglomerates were prepared by solvent change method. Solvent composition for spherical agglomeration was determined by constructing ternary diagram. Crystallization medium used for spherical agglomerates of naproxen consisted of tetra-hydro-furan (good solvent); water (poor solvent); isopropyl acetate (bridging liquid) in the ratio of 29:61:10, respectively. Spherical agglomerates were characterized by differential scanning calorimetry, infrared spectroscopy, X-ray diffractometry and scanning electron microscopy. Micromeritic and dissolution behavior studies were carried out. Process variables such as amount of bridging liquid, stirring time and duration of stirring were optimized. Dissolution profile of the spherical agglomerates was compared with pure sample and recrystallized sample. Spherical agglomerates exhibited decreased crystallinity and improved micromeritic properties. The dissolution of the spherical agglomerates was not improved compared with pure sample because the dissolution of naproxen dependent on particle size or surface area. Key words : Spherical agglomerates; Naproxen; Crystallinity; Dissolution. DOI: http://dx.doi.org/10.3329/sjps.v4i1.8860 SJPS 2011; 4(1): 1-8
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