注射纳米混悬剂制备及表征的研究进展

Research Progress of Preparation and Characterization of Nanosuspensions for Injection

将难溶性药物制成纳米混悬剂可提高其溶解度和溶出度。纳米混悬剂能以不同途径给药。其中,由于纳米混悬剂载药量高、给药体积小,因此可减轻不良反应和注射部位疼痛。本文归纳了注射纳米混悬剂的制备方法及表征指标。制备方法主要包括介质研磨、高压均质等由大颗粒裂解成小颗粒的类型,沉淀法、乳化法等由小颗粒聚集成大颗粒的类型,以及两种类型方法的联合应用。此外,简述了处方中稳定剂种类和浓度的影响。

Nanosuspension technology can be used to enhance the solubility and dissolution of poorly soluble drugs. And nanosuspensions can be administered via various routes. Adverse reactions and injection site pain of the nanosuspensions for injection can be reduced due to its high drug loading and small dose volume. This paper describes the preparation methods and characterization of the nanosuspensions for injection. The ＂top-down＂ technology（such as milling method and high pressure homogenization） and ＂bottom-up＂ technology（such as precipitation, emulsifi cation, etc.） as well as the combination of these two technologies are reviewed. Moreover, the effects of type and concentration of stabilizers in nanosuspensions are briefl y introduced.