超临界快速膨胀法制备植物甾醇超细微粒  

Micronization of Phytosterol by the RESS Technique with Supercritical CO_2

作　　者：蒋思媛[1] 赵亚平[1] 于文利[1] 黎英[1] 

机构地区：[1]上海交通大学化学化工学院,上海200240

出　　处：《精细化工》2004年第2期129-132,共4页Fine Chemicals

基　　金：上海市科委纳米专项基金资助(项目编号:0243nm097)

摘　　要：通过药物颗粒的微细化,降低其粒度,增大比表面积,进而提高药物颗粒的溶解度,可以有效地改善难溶药物的生物利用度。该文采用超临界流体快速膨胀法(RESS)微细化植物甾醇颗粒。利用SEM分析了沉淀颗粒的形貌及粒径大小。分析了过程参数与所制备颗粒粒度的关系。研究发现,当喷嘴内径Dn从60μm减小到40μm,植物甾醇颗粒粒径由10～20μm减小为5μm;预膨胀压力p0从15MPa增加到25MPa时,颗粒粒径由10～15μm降至5μm;预膨胀温度T0由318K升高到333K时,颗粒粒径由5～10μm减小为1μm,粒径分布也趋于均匀。喷嘴温度Tn对粒径无显著影响。该法制备得到1～20μm无定形植物甾醇微细颗粒,且具有更高的溶解速率,比原料植物甾醇早3h达到饱和溶解度。By reducing the particle size,the pharmaceutical particles have greater specific surfaces which lead to better solubility.Consequently the bioavailability of pharmaceutical substances can be improved by micronizing the particles.In this paper, the micronization of phytosterol particles is researched by the RESS (rapid expansion of supercritical solutions) process.The morphology and size of particles were studied through SEM.The relationship between processing parameters and the final size of the particles was studied.It was found that the size of phytosterol particles decreased from 10～20 μm to 5 μm when the inner diameter of nozzle,D_n,was decreased from 60 μm to 40 μm;there was a decrease of particle size from 10～15 μm to 5 μm when the preexpansion pressure,p_0,was increased from 15 MPa to 25 MPa;increase of the preexpansion temperature from 318 K to 333 K caused a significant decrease of particle size from 5～10 μm to 1 μm and a narrowing of particle size distribution.No regular relation between nozzle temperature and the particle size was found.Amorphous particles ranging from 1 μm to 20 μm were obtained by the RESS process.The RESS-processed phytosterol, of which the dissolution rate was much higher,realized the dissolution equilibrium 3 hours earlier than that unprocessed.

关 键 词：超临界快速膨胀 植物甾醇 微细化 CO2 

分 类 号：O629.21[理学—有机化学]