Formulation design of a novel fast-disintegrating tablet.
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.
Mizumoto
Takao
T
Pharmaceutical Research and Development Labs., Astellas Pharma Inc., 180 Ozumi, Yaizu, Shizuoka 425-0072, Japan. takao.mizumoto@jp.astellas.com
Masuda
Yoshinori
Y
Yamamoto
Takeshi
T
Yonemochi
Estuo
E
Terada
Katsuhide
K
D000082:Acetaminophen / Q000737:chemistry; D003460:Crystallization; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D015195:Drug Design; D006245:Hardness Tests; D010316:Particle Size; D011208:Powders; D012995:Solubility; D013402:Sugar Alcohols / Q000737:chemistry*; D013607:Tablets; D014961:X-Ray Diffraction
D004337:Drug Carriers; D011208:Powders; D013402:Sugar Alcohols; D013607:Tablets; D000082:Acetaminophen