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通过气溶胶溶剂萃取系统制备泼尼松龙多组分纳米颗粒。

Prednisolone multicomponent nanoparticle preparation by aerosol solvent extraction system.

作者信息

Moribe Kunikazu, Fukino Mika, Tozuka Yuichi, Higashi Kenjirou, Yamamoto Keiji

机构信息

Graduate School of Pharmaceutical Sciences, Chiba University, Inage-ku, Chiba, Japan.

出版信息

Int J Pharm. 2009 Oct 1;380(1-2):201-5. doi: 10.1016/j.ijpharm.2009.06.030. Epub 2009 Jul 2.

Abstract

Prednisolone nanoparticles were prepared in the presence of a hydrophilic polymer and a surfactant by the aerosol solvent extraction system (ASES). A ternary mixture of prednisolone, polyethylene glycol (PEG), and sodium dodecyl sulfate (SDS) dissolved in methanol was sprayed through a nozzle into the reaction vessel filled with supercritical carbon dioxide. After the ASES process was repeated, precipitates of the ternary components were obtained by depressurizing the reaction vessel. When a methanolic solution of prednisolone/PEG 4000/SDS at a weight ratio of 1:6:2 was sprayed under the optimized ASES conditions, the mean particle size of prednisolone obtained after dispersing the precipitates in water was observed to be ca. 230 nm. Prednisolone nanoparticles were not obtained by the binary ASES process for prednisolone, in the presence of either PEG or SDS. Furthermore, ternary cryogenic cogrinding, as well as solvent evaporation, was not effective for the preparation of prednisolone nanoparticles. As the ASES process can be conducted under moderate temperature conditions, the ASES process that was applied to the ternary system appeared to be one of the most promising methods for the preparation of drug nanoparticles using the multicomponent system.

摘要

通过气溶胶溶剂萃取系统(ASES),在亲水性聚合物和表面活性剂存在的情况下制备泼尼松龙纳米颗粒。将溶解在甲醇中的泼尼松龙、聚乙二醇(PEG)和十二烷基硫酸钠(SDS)的三元混合物通过喷嘴喷入充满超临界二氧化碳的反应容器中。重复ASES过程后,通过对反应容器减压获得三元组分的沉淀物。当在优化的ASES条件下以1:6:2的重量比喷雾泼尼松龙/PEG 4000/SDS的甲醇溶液时,将沉淀物分散在水中后得到的泼尼松龙的平均粒径约为230 nm。在仅存在PEG或SDS的情况下,通过泼尼松龙的二元ASES过程无法获得泼尼松龙纳米颗粒。此外,三元低温共研磨以及溶剂蒸发对于制备泼尼松龙纳米颗粒均无效。由于ASES过程可以在温和的温度条件下进行,因此应用于三元体系的ASES过程似乎是使用多组分体系制备药物纳米颗粒最有前景的方法之一。

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