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使用无毒溶剂在 CO(2)介质中制备聚合物颗粒:配方及与相分离法的比较。

Preparation of polymeric particles in CO(2) medium using non-toxic solvents: formulation and comparisons with a phase separation method.

机构信息

LUNAM Université, Angers, France.

出版信息

Eur J Pharm Biopharm. 2012 Nov;82(3):498-507. doi: 10.1016/j.ejpb.2012.08.005. Epub 2012 Aug 29.

DOI:10.1016/j.ejpb.2012.08.005
PMID:22959993
Abstract

The aim of this work was to elaborate formulation strategies to encapsulate a protein into biodegradable polymeric particles for sustained release purpose. In this paper, two encapsulation methods will be presented, one dealing with a phase separation phenomenon while the other involving an emulsification/extraction process in CO(2) medium. In those methods, only non-volatile injectable solvents such as glycofurol or isosorbide dimethyl ether were used to dissolve the polymer. Moreover, experimental designs were built up to help us to go further in the understanding of the processes and to better predict output responses in design space. Spherical particles were successfully generated with a satisfactory encapsulation yield. Further characterization steps such as in vitro, in vivo releases will be carried out to validate the interest of our encapsulation methods in the development of drug delivery systems.

摘要

这项工作的目的是阐述将蛋白质包封在可生物降解的聚合物颗粒中的配方策略,以实现缓释目的。本文将介绍两种封装方法,一种涉及相分离现象,另一种涉及在 CO(2)介质中的乳化/提取过程。在这些方法中,仅使用非挥发性可注射溶剂,如甘油呋喃或异山梨醇二甲醚来溶解聚合物。此外,还建立了实验设计来帮助我们进一步了解这些过程,并更好地在设计空间中预测输出响应。成功地生成了具有令人满意的包封产率的球形颗粒。将进行进一步的体外、体内释放等表征步骤,以验证我们的封装方法在药物传递系统开发中的应用价值。

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