Davis Mark T, Potter Catherine B, Mohammadpour Maryam, Albadarin Ahmad B, Walker Gavin M
Synthesis and Solid State Pharmaceutical Centre (SSPC), The BernalInstitute, University of Limerick, Ireland.
Synthesis and Solid State Pharmaceutical Centre (SSPC), The BernalInstitute, University of Limerick, Ireland.
Int J Pharm. 2017 Mar 15;519(1-2):365-372. doi: 10.1016/j.ijpharm.2017.01.043. Epub 2017 Jan 25.
A range of 17 ternary formulations of itraconazole (ITZ), HPMCP and Soluplus have been manufactured using spray drying. These amorphous solid dispersions (ASDs) were very stable against crystallisation and ITZ was found to be amorphous in all formulations after one year at 40°C/75% RH. A number of solid state analytical techniques including PXRD, DSC, small angle X-ray scattering, FTIR and solid state NMR were used to characterise the physicochemical properties of the ASDs following processing and storage and to assess any interactions between components. Microtrac laser scattering analysis revealed a relationship between polymer levels and particle size distribution (PSD). Dissolution studies indicated that higher Soluplus content in the formulation resulted in higher concentrations of ITZ in acidic media.
已通过喷雾干燥制备了一系列包含伊曲康唑（ITZ）、羟丙甲纤维素邻苯二甲酸酯（HPMCP）和聚乙烯己内酰胺（Soluplus）的17种三元制剂。这些无定形固体分散体（ASD）对结晶非常稳定，并且在40°C/75%相对湿度下放置一年后，发现所有制剂中的ITZ均为无定形。使用了多种固态分析技术，包括粉末X射线衍射（PXRD）、差示扫描量热法（DSC）、小角X射线散射、傅里叶变换红外光谱（FTIR）和固态核磁共振，来表征加工和储存后ASD的物理化学性质，并评估各组分之间的任何相互作用。Microtrac激光散射分析揭示了聚合物含量与粒度分布（PSD）之间的关系。溶出度研究表明，制剂中较高的Soluplus含量会导致在酸性介质中ITZ的浓度更高。
