Development of basic technologies for the practical production and particulate design of pharmaceutical organic nanoparticles by the rapid expansion of supercritical solutions (RESS) technique

测定了4种药物有机化合物在超临界二氧化碳中的溶解度和11种二氧化碳+药物有机化合物体系的固-液-气三相平衡，这对理解和设计超临界溶液快速膨胀(RESS)技术具有重要意义。采用RESS法制备了RS-(±)-布洛芬、乙酰水杨酸和茶碱的粒径分布较窄的纳米球形微粒(DAV&AP；200 nm)。研究发现，RESS法制备的纳米颗粒的性质受过饱和度控制，过饱和度定义为制备溶质饱和超临界溶液时溶质的化学势与所产生颗粒收集段溶质的化学势之差。

The solubility of four pharmaceutical organic compounds in supercritical carbon dioxide and the solid-liquid-gas three-phase equilibria for eleven carbon dioxide + pharmaceutical organic compound systems, which are very important to understand and design the rapid expansion of supercritical solutions (RESS) technique, were measured. The nano-sized spherical particles (dav ≈ 200 nm) with the narrow particle size distribution of RS-(±)-ibuprofen, acetylsalicylic acid and theophylline were produced by the RESS technique. The properties of the nanoparticles produced by the RESS technique were found to be controlled by the supersaturation defined as the difference between the chemical potential of the solute at the section of preparing the supercritical solution saturated with the solute and that at the section of the collection of the produced particles.