Mizumoto Takao, Masuda Yoshinori, Yamamoto Takeshi, Yonemochi Estuo, Terada Katsuhide
Pharmaceutical Research and Development Labs., Astellas Pharma Inc., 180 Ozumi, Yaizu, Shizuoka 425-0072, Japan.
Int J Pharm. 2005 Dec 8;306(1-2):83-90. doi: 10.1016/j.ijpharm.2005.09.009. Epub 2005 Oct 27.
As our society is becoming increasingly aged, the development of an appropriate dosage form for the elderly patients is mostly desirable. A novel fast-disintegrating tablet was investigated in this study as a user-friendly dosage form for the aged. Advantages of this formulation have sufficient hardness and can be manufactured by commonly used equipment. Saccharides can be divided into high- and low-compressibility categories, and an appropriate material for fast-disintegrating tablets was created by taking advantage of this fact. To improve the compressibility of low-compressibility saccharides, particle modification was conducted by coating and granulating a low-compressibility saccharide with a high one to enable the production of a fast-disintegrating tablet. Another discovery was that the high-compressibility saccharide used as a binder solution was present in an amorphous state after the granulation process. The crystal change from amorphous to crystal state intentionally by a conditioning process after compression enabled to increase tablet hardness by strengthening adhesion between particles. The conditioning process made it possible to achieve sufficient hardness while maintaining the fast disintegration time. As a result, this fast-disintegrating tablet that can be manufactured by commonly used equipment, can be used for the dosing of a wide range drugs.
随着我们的社会老龄化程度日益加深，开发适合老年患者的剂型变得极为必要。在本研究中，一种新型速崩片作为一种方便老年人使用的剂型进行了研究。该制剂的优点是具有足够的硬度，并且可以通过常用设备制造。糖类可分为高压缩性和低压缩性类别，利用这一事实创造了一种适合速崩片的材料。为了提高低压缩性糖类的压缩性，通过用高压缩性糖类对低压缩性糖类进行包衣和制粒来进行颗粒改性，从而能够生产速崩片。另一个发现是，用作粘合剂溶液的高压缩性糖类在制粒过程后呈无定形状态。压缩后通过老化处理有意使晶体从无定形转变为结晶状态，能够通过加强颗粒间的粘附力来提高片剂硬度。老化处理使得在保持快速崩解时间的同时能够达到足够的硬度。结果，这种可以通过常用设备制造的速崩片可用于多种药物的给药。
