Verraedt Els, Van den Mooter Guy, Martens Johan A
Centre for Surface Chemistry and Catalysis, K.U. Leuven, Kasteelpark Arenberg, Leuven, Belgium.
J Pharm Sci. 2011 Oct;100(10):4295-301. doi: 10.1002/jps.22617. Epub 2011 May 12.
A new synthesis route for large spherical particles of amorphous microporous silica (AMS) was developed. These novel spherical porous particles with diameter of around 100 µm and pore diameter smaller than 2 nm were prepared using an oil drop method. Molten ibuprofen was successfully loaded into the AMS pores. In vitro release experiments revealed that ibuprofen was released from the spheres via a slow pore diffusion process lasting up to 14 days. Experimentally determined diffusion coefficients of ibuprofen in the porous spheres were of the order of 10(-15) -10(-16) m(2) s(-1) . The present findings reveal the potential of AMS spheres for controlled release of small drug molecules over long time periods. The spherical shape of the AMS particles is advantageous in formulation processes as it provides adequate powder flow properties and reliable release profiles.
开发了一种用于制备大尺寸球形无定形微孔二氧化硅（AMS）颗粒的新合成路线。采用油滴法制备了这些新型球形多孔颗粒，其直径约为100 µm，孔径小于2 nm。布洛芬熔体成功地负载到AMS孔中。体外释放实验表明，布洛芬通过持续长达14天的缓慢孔扩散过程从球体中释放出来。实验测定的布洛芬在多孔球体中的扩散系数约为10^(-15) - 10^(-16) m² s^(-1) 。目前的研究结果揭示了AMS球体在长时间控制释放小药物分子方面的潜力。AMS颗粒的球形形状在制剂过程中具有优势，因为它提供了足够的粉末流动性和可靠的释放曲线。
