title: Effect of preparation method on properties of orally disintegrating tablets made by phase transition.
abstract: In order to evaluate the effect of preparation method on the properties of orally disintegrating (OD) tablets, OD tablets were prepared by compressing a mixture of high melting point sugar alcohol (HMP-SA) and low melting point sugar alcohol (LMP-SA) and subsequent heating. In the direct compression method (DCM) where the LMP-SA was added as a powder, both hardness and disintegration time were increased by decreasing the particle size of the LMP-SA. In the wet granule compression method (WGCM), where the LMP-SA was added as an aqueous binder solution, the tablets became harder with less heating compared to tablets prepared by DCM. Using 1% xylitol as the LMP-SA provided tablets with sufficient hardness when prepared by WGCM, as opposed to DCM where 5% xylitol was necessary to prepare tablets with similar hardness. These results suggest that uniformly distributed LMP-SA on the surface of HMP-SA particles in WGCM might diffuse more easily during the heating process compared to mechanically mixed LMP-SA in DCM, resulting in an increase in tablet hardness even with a short heating time and low content of LMP-SA. In addition, disintegration and hardness stability of the tablets were affected by the LMP-SA content when prepared by WGCM, suggesting that the LMP-SA content should be regulated to assure the stability of OD tablet characteristics.
authors.affiliation: Formulation Technology Research Laboratories, DAIICHI SANKYO CO. LTD., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan. kuno.yoshio.h2@daiichisankyo.co.jp
authors.forename: Yoshio
authors.initials: Y
authors.lastname: Kuno
authors.forename: Masazumi
authors.initials: M
authors.lastname: Kojima
authors.forename: Shuichi
authors.initials: S
authors.lastname: Ando
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Nakagami
mesh_terms: D055598:Chemical Phenomena; D002627:Chemistry, Physical; D003460:Crystallization; D004339:Drug Compounding; D004896:Erythritol / Q000008:administration & dosage / Q000737:chemistry; D006244:Hardness; D010316:Particle Size; D016062:Porosity; D011208:Powders; D012995:Solubility; D013607:Tablets / Q000737:chemistry*; D014199:Trehalose / Q000008:administration & dosage / Q000737:chemistry; D014961:X-Ray Diffraction; D014993:Xylitol / Q000737:chemistry
chemical_list: D011208:Powders; D013607:Tablets; D014199:Trehalose; D004896:Erythritol; D014993:Xylitol