Department of Analytical Chemistry, University of Barcelona (UB), Martí i Franquès 1-11, 08028 Barcelona, Spain.
J Pharm Biomed Anal. 2009 Dec 5;50(5):847-52. doi: 10.1016/j.jpba.2009.07.006. Epub 2009 Aug 5.
A controlled azacytidine release system based on drug encapsulation with a polymer material has been prepared and characterized. The drug systems were prepared by precipitation from solutions, using supercritical CO2 antisolvent technique operating in a semi-continuous mode. Azacytidine was dissolved in dimethylsulfoxide and poly-lactic acid in methylene chloride. The two solutions were mixed before being sprayed into the supercritical reactor. Experimental conditions were 40 degrees C for temperature, 11 MPa for pressure, and a CO2 flow rate of 30 ml min(-1). The precipitated drug-polymer particles were further characterized to determine the percentage of encapsulated drug and establish the delivery kinetics under various release conditions. A sustained delivery of the drug over a period of various hours was obtained. Besides, an improved stability of the coated drug with respect to the pure azacytidine was found, thus proving the suitability of this approach for dealing with unstable compounds.
已制备并表征了基于药物包封的聚合物材料的受控阿扎胞苷释放系统。通过超临界 CO2 抗溶剂技术在半连续模式下从溶液中沉淀制备药物系统。阿扎胞苷溶解在二甲基亚砜中，聚乳酸溶解在二氯甲烷中。两种溶液在被喷射到超临界反应器之前混合。实验条件为温度 40 摄氏度，压力 11 MPa，CO2 流速 30 ml min(-1)。沉淀的药物-聚合物颗粒进一步进行了表征，以确定包封药物的百分比，并在各种释放条件下建立释放动力学。在不同的小时数内获得了药物的持续释放。此外，发现与纯阿扎胞苷相比，包衣药物的稳定性得到了提高，从而证明了这种方法处理不稳定化合物的适用性。
