Division of Pharmaceutical Technology, Department of Chemistry, University of Hamburg, Bundesstrasse, Hamburg, Germany.
Pharm Dev Technol. 2012 Nov-Dec;17(6):649-53. doi: 10.3109/10837450.2011.572897. Epub 2011 Jul 8.
Novel tableting excipients are continuously developed and advertised with superior flow and compaction characteristics.
The objective of this study was to compare two traditionally used and two novel tableting excipients with regard to their physical and tableting properties as well as their magnesium stearate sensitivity. Avicel(®) PH102 (microcrystalline cellulose) was compared to the novel co-processed excipient Prosolv(®) SMCC90 (silicified microcrystalline cellulose), whereas Anhydrous Emcompress(®) (anhydrous dicalcium phosphate) was compared to the novel spherically granulated excipient Fujicalin(®) (anhydrous dicalcium phosphate).
True density, particle size, specific surface area (SSA), flowability, tabletability, and magnesium stearate sensitivity of the excipients was determined.
Due to the silification process (Prosolv(®)) and the unique manufacturing process (Fujicalin(®)), the novel excipients showed a comparably larger SSA. Hardest tablets by far could be obtained with Prosolv(®), followed by Avicel(®) and Fujicalin(®). Avicel(®) and Prosolv(®) were sensitive to magnesium stearate, whereas Fujicalin(®) and Emcompress(®) did not show lubricant sensitivity. This confirms the plastic deformation behavior of microcrystalline cellulose and the brittle fracture of anhydrous dicalcium phosphate.
Compared to the traditional excipients the investigated novel tableting excipients were advantageous with regard to their SSA and their tableting properties.
新型压片辅料不断被开发和宣传，具有优越的流动性和可压缩性。
本研究旨在比较两种传统和两种新型压片辅料在物理和压片性能以及硬脂酸镁敏感性方面的差异。将 Avicel（®） PH102（微晶纤维素）与新型共处理辅料 Prosolv（®） SMCC90（硅化微晶纤维素）进行比较，同时将 Anhydrous Emcompress（®）（无水磷酸氢钙）与新型球形颗粒化辅料 Fujicalin（®）（无水磷酸氢钙）进行比较。
测定辅料的真密度、粒径、比表面积（SSA）、流动性、可压性和硬脂酸镁敏感性。
由于硅化过程（Prosolv（®））和独特的制造工艺（Fujicalin（®）），新型辅料的 SSA 相对较大。迄今为止，最硬的片剂可以用 Prosolv（®）获得，其次是 Avicel（®）和 Fujicalin（®）。Avicel（®）和 Prosolv（®）对硬脂酸镁敏感，而 Fujicalin（®）和 Emcompress（®）则没有表现出润滑剂敏感性。这证实了微晶纤维素的塑性变形行为和无水磷酸氢钙的脆性断裂。
与传统辅料相比，研究中考察的新型压片辅料在 SSA 和压片性能方面具有优势。
