Factors affecting the characteristics of rapidly disintegrating tablets in the mouth prepared by the crystalline transition of amorphous sucrose.
The aim of this study is to investigate the factors affecting the characteristics of rapidly disintegrating tablets containing an amorphous ingredient prepared by crystalline transition method (CTM) under various storage conditions. Effect of storage conditions and formulating ratio of amorphous sucrose on the characteristic changes (tensile strength, porosity, and disintegration time) of the rapidly disintegrating tablets was studied. The storage conditions of different temperature and humidity affected the rate of crystalline transition and the increase in the tablet tensile strength. The faster crystalline transition resulted in a faster rate of increase in the tablet tensile strength. Regarding the effect of the formulating ratio of amorphous sucrose, in the case of 20-100%, the tensile strength after storage as a function of the porosity could be plotted on the same curve. For tablets containing 100% amorphous sucrose, the tablets with different porosity changed to almost the same structure due to the crystalline transition. Hence, the higher formulating ratio of amorphous sucrose provided the longer disintegration time in the mouth. Therefore, we concluded that the formulating ratio of 10-20% of the amorphous sucrose in the tablet is suitable for the rapidly disintegrating tablet in the mouth when prepared by CTM.
Sugimoto
Masaaki
M
Development Laboratories, Tanabe Seiyaku Co., Ltd., 16-89 Kashima 3-chome, Yodogawa-ku, Osaka 532-8505, Japan. sugimoto@tanabe.co.jp
Maejima
Toru
T
Narisawa
Shinji
S
Matsubara
Koji
K
Yoshino
Hiroyuki
H
D003460:Crystallization; D006801:Humans; D009055:Mouth / Q000187:drug effects / Q000378:metabolism*; D016062:Porosity; D012995:Solubility; D013395:Sucrose / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism*; D013607:Tablets; D013718:Tensile Strength; D013997:Time Factors
D013607:Tablets; D013395:Sucrose