Kostelanská Klára, Prudilová Barbora Blahová, Holešová Sylva, Vlček Jakub, Vetchý David, Gajdziok Jan
Department of Pharmaceutical Technology, Faculty of Pharmacy, Masaryk University, Palackého Třída 1946/1, 612 00 Brno, Czech Republic.
Department of Physical Chemistry, Faculty of Science, Palacký University Olomouc, Tř. 17. Listopadu 1192/12, 771 46 Olomouc, Czech Republic.
Pharmaceutics. 2022 Apr 8;14(4):818. doi: 10.3390/pharmaceutics14040818.
High specific surface area (SSA), porous structure, and suitable technological characteristics (flow, compressibility) predetermine powder carriers to be used in pharmaceutical technology, especially in the formulation of liquisolid systems (LSS) and solid self-emulsifying delivery systems (s-SEDDS). Besides widely used microcrystalline cellulose, other promising materials include magnesium aluminometasilicates, mesoporous silicates, and silica aerogels. Clay minerals with laminar or fibrous internal structures also provide suitable properties for liquid drug incorporation. This work aimed at a comparison of 14 carriers' main properties. Cellulose derivatives, silica, silicates, and clay minerals were evaluated for flow properties, shear cell experiments, SSA, hygroscopicity, pH, particle size, and SEM. The most promising materials were magnesium aluminometasilicates, specifically Neusilin US2, due to its proper flow, large SSA, etc. Innovative materials such as FujiSil or Syloid XDP 3050 were for their properties evaluated as suitable. The obtained data can help choose a suitable carrier for formulations where the liquid phase is incorporated into the solid dosage form. All measurements were conducted by the same methodology and under the same conditions, allowing a seamless comparison of property evaluation between carriers, for which available company or scientific sources do not qualify due to different measurements, conditions, instrumentation, etc.
高比表面积(SSA)、多孔结构以及合适的工艺特性(流动性、可压缩性)使粉末载体注定要用于制药技术,尤其是在液固系统(LSS)和固体自乳化给药系统(s-SEDDS)的制剂中。除了广泛使用的微晶纤维素外,其他有前景的材料还包括铝硅酸镁、介孔硅酸盐和二氧化硅气凝胶。具有层状或纤维状内部结构的粘土矿物也为液体药物的掺入提供了合适的特性。这项工作旨在比较14种载体的主要特性。对纤维素衍生物、二氧化硅、硅酸盐和粘土矿物进行了流动性、剪切细胞实验、SSA、吸湿性、pH值、粒度和扫描电子显微镜(SEM)评估。最有前景的材料是铝硅酸镁,特别是Neusilin US2,因为它具有适当的流动性、较大的SSA等。像FujiSil或Syloid XDP 3050这样的创新材料因其性能被评估为合适。所获得的数据有助于为将液相掺入固体剂型的制剂选择合适的载体。所有测量均采用相同的方法并在相同的条件下进行,从而能够对载体之间的性能评估进行无缝比较,而由于测量、条件、仪器等不同,现有的公司或科学来源无法做到这一点。