Quodbach Julian, Kleinebudde Peter
Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-University , Duesseldorf , Germany.
Pharm Dev Technol. 2015;20(6):762-8. doi: 10.3109/10837450.2014.920357. Epub 2014 May 22.
Tablet disintegration can be influenced by several parameters, such as storage conditions, type and amount of disintegrant, and relative tablet density. Even though these parameters have been mentioned in the literature, the understanding of the disintegration process is limited. In this study, water uptake and force development of disintegrating tablets are analyzed, as they reveal underlying processes and interactions. Measurements were performed on dibasic calcium phosphate tablets containing seven different disintegrants stored at different relative humidities (5-97%), and on tablets containing disintegrants with different mechanisms of action (swelling and shape recovery), compressed to different relative densities. Disintegration times of tablets containing sodium starch glycolate are affected most by storage conditions, which is displayed in decreased water uptake and force development kinetics. Disintegration times of tablets with a swelling disintegrant are only marginally affected by relative tablet density, whereas the shape recovery disintegrant requires high relative densities for quick disintegration. The influence of relative tablet density on the kinetics of water uptake and force development greatly depends on the mechanism of action. Acquired data allows a detailed analysis of the influence of storage conditions and mechanisms of action on disintegration behavior.
片剂崩解会受到几个参数的影响，如储存条件、崩解剂的类型和用量以及片剂的相对密度。尽管这些参数在文献中已有提及，但对崩解过程的理解仍然有限。在本研究中，对崩解片剂的吸水和力的发展进行了分析，因为它们揭示了潜在的过程和相互作用。对含有七种不同崩解剂的磷酸氢钙片剂在不同相对湿度（5 - 97%）下储存的情况进行了测量，以及对含有不同作用机制（膨胀和形状恢复）崩解剂且压制成不同相对密度的片剂进行了测量。含有羟丙甲纤维素的片剂的崩解时间受储存条件影响最大，表现为吸水和力发展动力学的降低。具有膨胀崩解剂的片剂的崩解时间仅略微受片剂相对密度的影响，而形状恢复崩解剂则需要高相对密度才能快速崩解。片剂相对密度对吸水和力发展动力学的影响很大程度上取决于作用机制。所获得的数据有助于详细分析储存条件和作用机制对崩解行为的影响。
