热熔融挤出技术在制备口服固体分散体中的应用

Application of Hot-melt Extrusion to Preparation of Oral Solid Dispersion

热熔融挤出是指药物、聚合物载体等在熔融状态下混合,以一定的压力、速度和形状挤出形成无定形产品的一种技术,具有连续化操作、减少粉尘、操作简单、不使用有机溶剂等特点。应用该技术制备口服固体分散体,对提高难溶性药物溶出度、调节药物释放速率、增强药物稳定性等有突出的优势。本文综述了热熔融挤出技术的原理、设备及应用该技术上市的口服制剂,探讨其制备固体分散体需关注的问题,旨在推动其在我国创新药物制剂研发中的应用。

Hot melt extrusion is one of the most widely applied processing technology in the plastics, rubber and food industry. Today, this technology has found its place in the array of pharmaceutical field for the manufacture of a variety of dosage forms such as granules, pellets, tablets, suppositories, implants, stents, transdermal systems and ophthalmic inserts. Hot-melt extrusion, which has the advantages of continuous operation, dust reduction, simple process, absent of organic solvents and so on, is the process of pumping raw materials with a rotating screw under the elevated temperature and pressure through a die to form a product with the uniform shape. The solid dispersion prepared by hot-melt extrusion has its distinct predominance in increasing drug solubility, adjusting drug release and improving drug stability. However, as with other breakthrough innovations, numerous obstacles had to be overcome before commercialization of the technology and resulting dosage forms. This paper aims to promote the research and development of pharmaceutical preparations in innovative drug by reviewing the theory, equipment and commercial oral products of hot-melt extrusion and analyzing the critical problems in the process of preparing solid dispersion with hotmelt extrusion.