Sugimoto M, Matsubara K, Koida Y, Kobayashi M
Product Technology Development Laboratory, Department of Pharmaceutics, Tanabe Seiyaku Co., Ltd., 16-89 Kashima 3-chome, Yodogawa-ku, Osaka 532-8505, Japan.
Pharm Dev Technol. 2001 Nov;6(4):487-93. doi: 10.1081/pdt-120000287.
Elderly people, children and patients sometimes have difficulties swallowing tablets. To solve this problem, a novel method of preparing tablets that disintegrate rapidly in the mouth was developed. A tablet with high porosity is required for rapid disintegration, but such a tablet is generally fragile. To make a tablet having both high porosity and practical strength, amorphous sucrose, which has good compactability, was used. Mannitol powder with freeze-dried amorphous sucrose was tableted at low compression and stored under certain conditions. The tablet disintegrated rapidly in the mouth, because of its high porosity. The tensile strength of the tablet increased remarkably during storage, while the porosity of the tablet seemed almost unchanged. The results of thermal analysis and powder x-ray diffraction measurement showed that the amorphous sucrose in tablet crystallized during storage. The increase in the tensile strength of the tablet was due to crystallization of the amorphous sucrose and formation of new internal contact points in the tablet. It was concluded that this crystalline transition method is a very useful method to prepare a rapidly disintegrating tablet.
老年人、儿童和患者有时在吞咽片剂时会遇到困难。为了解决这个问题，开发了一种制备在口腔中快速崩解的片剂的新方法。快速崩解需要具有高孔隙率的片剂，但这种片剂通常很脆。为了制备兼具高孔隙率和实用强度的片剂，使用了具有良好可压性的无定形蔗糖。将含有冻干无定形蔗糖的甘露醇粉末在低压力下压片并在特定条件下储存。该片剂由于其高孔隙率而在口腔中迅速崩解。片剂的拉伸强度在储存期间显著增加，而片剂的孔隙率似乎几乎不变。热分析和粉末X射线衍射测量结果表明，片剂中的无定形蔗糖在储存期间结晶。片剂拉伸强度的增加是由于无定形蔗糖的结晶和片剂中新的内部接触点的形成。得出的结论是，这种结晶转变方法是制备快速崩解片剂的非常有用的方法。
