Division of Pharmaceutical Technology, Faculty of Pharmacy, FI-00014, University of Helsinki, Finland.
Int J Pharm. 2012 Jan 17;422(1-2):125-31. doi: 10.1016/j.ijpharm.2011.10.040. Epub 2011 Oct 28.
In this study, indomethacin-loaded thermally oxidized mesoporous silicon microparticles (TOPSi-IMC) were formulated into tablets with excipients in order to improve the dissolution and permeability properties of the poorly soluble drug. Formulations of TOPSi-IMC particles and excipients were prepared at different TOPSi-IMC particle ratios (25, 30 and 35%). The formulations were compressed by direct compression technique with a single punch tablet machine. For comparison, a formulation containing the bulk IMC (indomethacin) and the same excipients without thermally oxidized mesoporous silicon microparticles particles (TOPSi) was prepared and compressed into tablets. The TOPSi-IMC tablets were characterised according to weight, thickness, crushing strength, disintegration time and dissolution rate. The results of this study show that TOPSi-IMC particles can be compressed to a conventional tablet. The release rate of the drug and its permeation across intestinal cells model (Caco-2) from TOPSi-IMC tablets was improved compared to the bulk IMC tablets. The dissolution rate and permeability of IMC from the tablets decreased with increasing ratio of the TOPSi-IMC particles in the formulation. The phenomenon is, presumably, a result of the loss of unique pore structure of the particles due to deformation of the particles under the compression load.
在这项研究中，将吲哚美辛负载的热氧化介孔硅微球（TOPSi-IMC）与赋形剂制成片剂，以改善难溶性药物的溶解和渗透性。以不同的 TOPSi-IMC 颗粒比例（25、30 和 35%）制备 TOPSi-IMC 颗粒和赋形剂的制剂。采用单冲压片机的直接压缩技术将制剂压缩成片剂。为了进行比较，制备了含有块状 IMC（吲哚美辛）和相同赋形剂但不含热氧化介孔硅微球颗粒（TOPSi）的制剂，并将其压缩成片剂。根据重量、厚度、抗压强度、崩解时间和溶出速率对 TOPSi-IMC 片剂进行了表征。研究结果表明，TOPSi-IMC 颗粒可被压缩成常规片剂。与块状 IMC 片剂相比，TOPSi-IMC 片剂中药物的释放速率及其穿过肠细胞模型（Caco-2）的渗透性能得到了提高。片剂中 TOPSi-IMC 颗粒的比例增加，药物的溶出率和渗透性降低。这种现象可能是由于颗粒在压缩载荷下的变形导致颗粒独特的孔结构丧失所致。
