Rasenack N, Müller B W
Department of Pharmaceutics and Biopharmaceutics, Christian Albrecht University Kiel, Gutenbergstr. 76, 24118 Kiel, Germany.
Drug Dev Ind Pharm. 2002 Oct;28(9):1077-89. doi: 10.1081/ddc-120014575.
Different crystal forms of the analgesic drug ibuprofen were prepared and characterized in this study. Various conditions were used for the crystallization: crystallization was carried out using the solvent change method, the temperature change method, and the solvent evaporation method. Crystals were grown from different solvents. Different crystal forms with different properties were observed: cubic, needle-shaped, and plate-shaped crystals were obtained. Spherical agglomeration occurs when crystallization is carried out in acetonitrile or methanol. Flowability of these spherical crystals is increased. All crystals were determined as isomorphic by differential scanning calorimetry and x-ray analysis--which queries doubtful results of recent publications. Properties like dissolution behavior and properties influencing the manufacturing of dosage forms--like flowability--differ. Thus the choice of the optimal preparation method influencing the crystal habit is important in manufacturing the drug ibuprofen.
本研究制备并表征了镇痛药物布洛芬的不同晶型。采用了各种条件进行结晶:使用溶剂变化法、温度变化法和溶剂蒸发法进行结晶。晶体从不同溶剂中生长。观察到具有不同性质的不同晶型:获得了立方晶、针状晶和板状晶。在乙腈或甲醇中进行结晶时会出现球形团聚。这些球形晶体的流动性增加。通过差示扫描量热法和X射线分析确定所有晶体为同构——这对近期出版物的可疑结果提出了质疑。溶解行为等性质以及影响剂型制造的性质——如流动性——存在差异。因此,在布洛芬药物制造中,选择影响晶体习性的最佳制备方法很重要。