Zhang Xin, Guan Jian, Ni Rui, Li Luk Chiu, Mao Shirui
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
Abbott Laboratories, Abbott Park, Illinois 60064.
J Pharm Sci. 2014 Jul;103(7):2166-2176. doi: 10.1002/jps.24015. Epub 2014 May 19.
To test the feasibility of preparing redispersible powders from nanosuspensions without further addition of drying protectants, Lovastatin was processed into nanosuspensions and subsequently converted into a powder form using a spray-drying process. The effects of spray-drying process parameters and stabilizers on the properties of the spray-dried powders were evaluated. The inlet air temperature was found to have the most pronounced impact; a low-inlet air temperature consistently yielded dried powders with improved redispersibility. This was attributed to the low Peclet number associated with a low-inlet air temperature, making nanoparticles less prone to aggregation and coalescence during spray drying, as evidenced by the well-defined boundary shown between nanoparticles in the SEM photomicrographs of the spray-dried microparticles. The influence of atomization pressure is significant particularly at a low-inlet air temperature. The redispersibility index value of the powder is dependent on the type of stabilizers used in the nanosuspension formulation. Spray-dried powders with acceptable redispersibility were prepared with drug concentration as high as 3%. In conclusion, with optimized process parameters and selected stabilizers, spray drying is a feasible process in the solidification of nanosuspensions with high drug loading and acceptable redispersibility.
为了测试在不额外添加干燥保护剂的情况下由纳米混悬液制备可再分散粉末的可行性，将洛伐他汀加工成纳米混悬液，随后使用喷雾干燥工艺将其转化为粉末形式。评估了喷雾干燥工艺参数和稳定剂对喷雾干燥粉末性质的影响。发现进气温度的影响最为显著；低进气温度始终能得到具有改善的再分散性的干燥粉末。这归因于与低进气温度相关的低佩克莱数，使得纳米颗粒在喷雾干燥过程中不易聚集和聚结，喷雾干燥微粒的扫描电子显微镜照片中纳米颗粒之间清晰的边界证明了这一点。雾化压力的影响尤为显著，特别是在低进气温度下。粉末的再分散性指数值取决于纳米混悬液配方中使用的稳定剂类型。制备出了药物浓度高达3%且具有可接受再分散性的喷雾干燥粉末。总之，通过优化工艺参数和选择稳定剂，喷雾干燥是一种可行的工艺，可用于固化具有高药物载量和可接受再分散性的纳米混悬液。
