应用超临界反溶剂技术制备吸入式给药微粒  

Preparing Microparticles for Inhalation Drug Delivery by Supercritical Antisolvent Process

作　　者：陈畅[1,2] 詹世平[2] 张苗苗[2] 李志义[1] 

机构地区：[1]大连理工大学流体与粉体工程研究设计所,辽宁大连116012 [2]大连大学环境与化学工程学院,辽宁大连116622

出　　处：《高校化学工程学报》2011年第3期470-474,共5页Journal of Chemical Engineering of Chinese Universities

基　　金：国家自然科学基金(20876017)

摘　　要：吸入式给药作为一种新型非入侵式给药系统,具有延长用药时间、增强治疗效果、提高病人顺应性等优点,是人们一直探索的理想的给药途径。吸入式给药中载药基体的制备是目前研究的热点。在自制的超临界反溶剂过程实验装置上,以聚乳酸作为研究对象,二氯甲烷-丙酮（1：1,V：V）为混合溶剂,制备了粒径较小、粒径分布较窄的载药基体微粒,分别研究了压力、温度、溶液流速和溶液浓度对微粒形态、粒径和粒径分布的影响。结果表明：选用二氯甲烷-丙酮为溶剂,制备的微粒粒径小,粒径分布窄,并且大部分微粒形态呈完整的球形;各影响因素对微粒粒径及粒径分布均有不同的影响,通过调节操作参数可制得粒径在0.8~4μm的微粒,符合吸入式给药微粒粒径的要求。Inhalation drug delivery is a new non-invasive delivery system which possesses several advantages,such as extending drug duration,enhancing therapeutic effect and elevating patient compliance.The preparation of the drug-loading matrix for the inhalation drug delivery is a study focus.In order to prepare more uniform and smaller drug-loading microparticles,an experimental apparatus for supercritical antisolvent（SAS） process was set up.The drug-loading microparticles of poly-l-lactide（PLLA） were prepared by SAS process with dichloromethane-acetone（1：1,V：V） as mixed solvent.The effects of process parameters including the pressure,the temperature,the solution concentration and the solution flow rate,on the particle size and particle size distributions were investigated experimentally.The results show that the PLLA microparticles prepared with acetone and dichloromethane as mixed solvent are much smaller and more uniform.The morphology of the most microparticles prepared is globular.Using SAS process,the PLLA microparticles with diameters of 0.8~4 μm can be obtained by adjusting process parameters,and the prepared micropaticles are suitable for inhalation delivery system.

关 键 词：吸入式给药 微粒 聚乳酸 超临界反溶剂过程 

分 类 号：TQ460.6[化学工程—制药化工] R944.9[医药卫生—药剂学]