热熔挤出技术制备固体分散体的辅料研究进展.PDFVIP

现代药物与临床 Drugs Clinic 第 29 卷 第 5 期 2014 年 5 月 ·557 · • 综述 • 热熔挤出技术制备固体分散体的辅料研究进展 张赫然，宋丽明，王彦竹，王杏林* 天津药物研究院 释药技与药代动力学国家重点实验室，天津 300193 摘 要：热熔挤出技术（HME ）是一种制备固体分散体的新技术。固体分散体的制备和性质主要依赖于辅料的选择。HME 的辅料应具有较强的热塑性、较高的热稳定性、适宜的熔融黏度和原辅料的相容性。依据辅料的用途，HME 的辅料主要分 为载体、塑化剂和功能性辅料。依据载体溶解能力的不同，载体又分为水溶性、难溶性和肠溶性 3 类，对应制备出速释、缓 控释功能的固体分散体。通过塑化剂和功能性辅料的修饰和辅助，进一步优化固体分散体的稳定性和释放特性。主要从载体、 塑化剂和功能性辅料等方面对 HME 的辅料进行综述，旨在为固体分散体载体的选择、固体分散体的制备提供参考和依据。 关键词：热熔挤出技术；固体分散体；辅料；载体；塑化剂 中图分类号：R94 文献标志码：A 文章编号：1674 - 5515(2014)05 - 0557 - 07 DOI: 10.7501/j.issn.1674-5515.2014.05.025 Research progress on excipients of solid dispersion prepared by hot-melt extrusion technique ZHANG He-ran, SONG Li-ming, WANG Yan-zhu, WANG Xing-lin State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China Abstract: Hot melt extrusion (HME) technique has emerged as a novel process technology for preparing solid dispersion. The preparation and properties of solid dispersion mainly depend on the choice of excipients. HME excipients should have strong thermoplasticity, high thermal stability, suitable melt viscosity, and compatibility of raw materials. In terms of the use of excipients, HME excipients were mainly divided into carrier, plasticizer, and functional materials. Based on the solubility of carrier, it could be divided into three categories such as water soluble, insoluble, and enteric carriers, corresponding to a fast, time controlled, or modified release of solid dispersion. Through the assistance of plasticizer and functional materials, the stability and release characteristics of solid dispersion are much better