Quodbach Julian, Kleinebudde Peter
a Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-University , Duesseldorf , Germany.
Pharm Dev Technol. 2016 Sep;21(6):763-74. doi: 10.3109/10837450.2015.1045618. Epub 2015 May 15.
Tablet disintegration is an important factor for drug release and can be modified with excipients called tablet disintegrants. Tablet disintegrants act via different mechanisms and the efficacy of these excipients is influenced by various factors.
In this review, the existing literature on tablet disintegration is critically reviewed. Potential disintegration mechanisms, as well as impact factors on the disintegration process will be discussed based on experimental evidence.
Search terms for Scopus and Web of Science included "tablet disintegration", "mechanism tablet disintegration", "superdisintegrants", "disintegrants", "swelling force", "disintegration force", "disintegration mechanisms", as well as brand names of commonly applied superdisintegrants. References of identified papers were screened as well.
Experimental data supports swelling and shape recovery as main mechanisms of action of disintegrants. Other tablet excipients and different manufacturing techniques greatly influence the disintegration process.
The use of different excipients, experimental setups and manufacturing techniques, as well as the demand for original research led to a distinct patchwork of knowledge. Broader, more systematic approaches are necessary not only to structure the past but also future findings.
片剂崩解是药物释放的一个重要因素,可通过称为片剂崩解剂的辅料进行调节。片剂崩解剂通过不同机制起作用,这些辅料的功效受多种因素影响。
在本综述中,对现有的关于片剂崩解的文献进行了批判性综述。将根据实验证据讨论潜在的崩解机制以及崩解过程的影响因素。
Scopus和Web of Science的检索词包括“片剂崩解”、“片剂崩解机制”、“超级崩解剂”、“崩解剂”、“膨胀力”、“崩解力”、“崩解机制”以及常用超级崩解剂的品牌名称。对已识别论文的参考文献也进行了筛选。
实验数据支持膨胀和形状恢复是崩解剂的主要作用机制。其他片剂辅料和不同的制造技术对崩解过程有很大影响。
不同辅料、实验设置和制造技术的使用,以及对原创研究的需求导致了知识的明显拼凑。不仅需要更广泛、更系统的方法来梳理过去的研究成果,也需要用其来指导未来的研究发现。