超临界流体快速膨胀法制备超细阿昔洛韦粒子

Preparation of Ultra-fine Particles of Acyclovir Using Rapid Expansion of Supercritical Solution

以二氧化碳作为超临界溶剂,采用超临界溶液快速膨胀技术制备得到超细阿昔洛韦药物粒子,在一定的温度和压力情况下,测定了阿昔洛韦在超临界二氧化碳中的溶解度,考察了各种操作参数对药物粒子粒径的影响,研究了药物粒子粒径随各种操作参数的变化规律。结果表明：阿昔洛韦在超临界二氧化碳中的溶解度较小,在10-5~10-6之间（摩尔分率）,溶解度随着温度和压力的升高而增大,不存在文献中所报道的反向区。同时实验结果表明：药物粒子粒径变化对预膨胀温度最敏感,粒径随预膨胀温度的升高而减小;一定范围内随收集距离的增大而增大;在萃取温度较低的情况下,粒子粒径基本随着萃取温度的升高而减小;随着萃取温度的升高,在相对较高预膨胀温度下,粒径随着萃取温度升高而增大。

This work was on the preparation of ultra-fine particles of acyclovir （ACV） in rapid expansion of supereritieal solution （RESS）. The solubility of ACV in supercritical CO2 was measured and effects of operation conditions on the size of ACV particles were investigated. It was found that ACV had poor solubility in SCF-CO2 and the value increased with the increasing of pressure and temperature. No retrograde area was found as reported in some literatures. In the RESS experiment, particles prepared were generally smaller, more uniform and better morphology than the starting material. The size of particles decreased with the increasing of preexpansion temperature, and increased with the increasing of collection distance. At lower extraction temperature, the size of particles decreased with the increasing of temperature. At a relatively high pre-expansion temperature, the particle size increased with the increasing of extraction temperature.