Rasenack Norbert, Müller Bernd W
Department of Pharmaceutics and Biopharmaceutics, Christian Albrecht University Kiel, Gutenbergstrasse 76, D-24118 Kiel, Germany.
Int J Pharm. 2002 Sep 5;244(1-2):45-57. doi: 10.1016/s0378-5173(02)00296-x.
The tableting behavior of drugs can be affected by changes in the crystal habit. Different crystal habits of the common analgesic drugs ibuprofen and acetaminophen were prepared. Their tableting behavior was characterized. In the case of ibuprofen, a plate-shaped crystal was compared with the common needle-shaped form. In the case of acetaminophen, plate-shaped and prismatic crystals of two different particle sizes were prepared. The aim was to find a crystal form that is suitable for direct compression with only a low amount of excipients. This requires a substance that forms stable compacts at low punch forces, having a good flowability and only a low tendency to stick to the punches. In order to compare the tableting behavior of different substances, a comparative factor (T-factor) was calculated, based on typical parts of the punch force/displacement-profile and properties of the resulting compact. This method works with low amounts of substance and allows a rapid reproducible determination of the tableting behavior. The method was evaluated by characterizing different typical excipients normally used for the production of tablets.
药物的压片行为会受到晶体习性变化的影响。制备了常见镇痛药布洛芬和对乙酰氨基酚的不同晶体习性。对它们的压片行为进行了表征。就布洛芬而言,将板状晶体与常见的针状晶体进行了比较。就对乙酰氨基酚而言,制备了两种不同粒径的板状和棱柱形晶体。目的是找到一种仅需少量辅料就能适用于直接压片的晶型。这需要一种在低冲压力下能形成稳定片剂、具有良好流动性且粘附冲头倾向低的物质。为了比较不同物质的压片行为,基于冲压力/位移曲线的典型部分和所得片剂的性质计算了一个比较因子(T因子)。该方法适用于少量物质,并能快速重现性地测定压片行为。通过表征通常用于生产片剂的不同典型辅料对该方法进行了评估。