title: The preparation of rapidly disintegrating tablets in the mouth.
abstract: 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.
authors.affiliation: Product Technology Development Laboratory, Department of Pharmaceutics, Tanabe Seiyaku Co., Ltd., 16-89 Kashima 3-chome, Yodogawa-ku, Osaka 532-8505, Japan. sugimoto@tanabe.co.jp
authors.forename: M
authors.initials: M
authors.lastname: Sugimoto
authors.forename: K
authors.initials: K
authors.lastname: Matsubara
authors.forename: Y
authors.initials: Y
authors.lastname: Koida
authors.forename: M
authors.initials: M
authors.lastname: Kobayashi
mesh_terms: D000284:Administration, Oral; D002626:Chemistry, Pharmaceutical; D003460:Crystallization; D005612:Freeze Drying; D006801:Humans; D008353:Mannitol / Q000138:chemical synthesis / Q000493:pharmacokinetics; D009055:Mouth / Q000378:metabolism*; D010880:Piperidines / Q000008:administration & dosage / Q000493:pharmacokinetics; D016062:Porosity; D012995:Solubility; D013395:Sucrose / Q000138:chemical synthesis / Q000493:pharmacokinetics; D013607:Tablets / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D013678:Technology, Pharmaceutical / Q000379:methods*; D013718:Tensile Strength
chemical_list: D010880:Piperidines; D013607:Tablets; C028458:tipepidine; D008353:Mannitol; D013395:Sucrose