Docoslis Aristides, Huszarik Krista L, Papageorgiou George Z, Bikiaris Dimitrios, Stergiou Dimitrios, Georgarakis E
Department of Chemical Engineering, Queen's University at Kingston, Ontario, Canada.
AAPS J. 2007 Dec 7;9(3):E361-70. doi: 10.1208/aapsj0903043.
In the present study, a series of solid dispersions of the drug nimodipine using polyethylene glycol as carrier were prepared following the hot-melt method. Micro-Raman spectroscopy in conjunction with X-ray powder diffractometry was used for the characterization of the solid structure, including spatial distribution, physical state, and presence of polymorphs, as well as storage stability of nimodipine in its solid formulations. The effect of storage time on drug stability was investigated by examination of the samples 6 months and 18 months after preparation. Confocal micro-Raman mapping performed on the samples showed that the drug was not uniformly distributed on a microscopic level. The presence of crystals of nimodipine with sizes varying between one and several micrometers was detected, and the crystal size seemed to increase with overall drug content. In samples examined 6 months after preparation it was found that the crystals existed mainly as the racemic compound, whereas after 18 months of storage mainly crystal conglomerates were observed.
在本研究中，采用热熔法制备了一系列以聚乙二醇为载体的尼莫地平固体分散体。利用显微拉曼光谱结合X射线粉末衍射法对固体结构进行表征，包括空间分布、物理状态、多晶型物的存在情况，以及尼莫地平在其固体剂型中的储存稳定性。通过对制备后6个月和18个月的样品进行检测，研究了储存时间对药物稳定性的影响。对样品进行的共聚焦显微拉曼映射显示，药物在微观层面上分布不均匀。检测到存在尺寸在1至几微米之间变化的尼莫地平晶体，并且晶体尺寸似乎随着药物总含量的增加而增大。在制备后6个月检测的样品中发现，晶体主要以消旋化合物形式存在，而在储存18个月后主要观察到晶体聚集体。
