El-Barghouthi Musa, Eftaiha Ala'a, Rashid Iyad, Al-Remawi Mayyas, Badwan Adnan
Chemistry Department, Hashemite University, Zarqa, Jordan.
Drug Dev Ind Pharm. 2008 Apr;34(4):373-83. doi: 10.1080/03639040701657792.
Disintegrants and fillers represent important excipients for immediate-release solid dosage forms in many pharmaceutical applications. A new excipient based on the coprecipitation of chitosan and silica has been achieved. The "intimate" physical association between chitosan and silica creates an insoluble, hydrophilic, highly absorbent material, consequently, resulting in superiority in water uptake, water saturation for gelling formation, and compactability among other superdisintegrants. The new excipient has an outstanding functionality that does not primarily depend on water wicking and swelling properties. In fact, it translates it into superior disintegration characteristics with improved powder flow and compaction properties. Thus, the new excipient could act as a superdisintegrant and pharmaceutical filler at the same time. Studies have shown that chitosan-silica delivers superior performance in wet granulation formulations and is the only disintegrant that is effective at all concentrations in tablet formulation.
崩解剂和填充剂是许多药物应用中速释固体剂型的重要辅料。一种基于壳聚糖和二氧化硅共沉淀的新型辅料已经研制成功。壳聚糖和二氧化硅之间的“紧密”物理结合形成了一种不溶性、亲水性、高吸水性材料，因此，在吸水性、形成凝胶所需的水饱和度以及与其他超级崩解剂相比的可压性方面具有优势。这种新型辅料具有出色的功能，其主要功能并不依赖于水的毛细作用和膨胀特性。事实上，它转化为具有优异崩解特性以及改善的粉末流动性和压缩性能。因此，这种新型辅料可以同时作为超级崩解剂和药物填充剂。研究表明，壳聚糖 - 二氧化硅在湿法制粒制剂中表现出卓越的性能，并且是片剂制剂中在所有浓度下均有效的唯一崩解剂。
