Savolainen Marja, Herder Jenny, Khoo Cynthia, Lövqvist Karin, Dahlqvist Carina, Glad Håkan, Juppo Anne Mari
Department of Pharmacy, Pharmaceutical Technology Division, University of Helsinki, P.O. Box 56, FIN-00014, Finland.
Int J Pharm. 2003 Aug 27;262(1-2):47-62. doi: 10.1016/s0378-5173(03)00336-3.
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 microm. 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 ATO 5/Pluronic F127 tablets the release was of zero order.
本研究的目的是制备难溶性药物非洛地平的控释片。采用喷雾冷却法将药物、极性脂质和亲水性聚合物制成固体分散体微粒,然后进行压片。通过傅里叶变换红外光谱和拉曼光谱、X射线粉末衍射、热台显微镜、扫描电子显微镜和图像分析对微粒进行表征。所有样品中非洛地平的结晶度均有所降低,结晶态非洛地平的量因固体分散体的组成而异。微粒呈球形,中位粒径范围为20至35微米。向基质中添加亲水性聚合物拓宽了粒径分布并增加了团聚体的量。含甘油酯的片剂获得了最有前景的溶出模式;例如,Precirol ATO 5/普朗尼克F127片剂的释放为零级。