title: Hygroscopicity of a sugarless coating layer formed by the interaction between mannitol and poly(vinyl alcohol) (PVA).
abstract: A sugarless layer that provides protection against moisture is formed on tablets when a coating solution comprising mannitol and poly(vinyl alcohol) (PVA) is applied. The objective of this study is to investigate the relationship between the formation of such a sugarless layer and the resulting hygroscopic properties in order to derive an appropriate sugarless coating. The hygroscopicity of the sugarless layer is shown to be strongly affected by the addition of PVA, and has the lowest at concentration ratios between 15:2.5 and 15:4 (w/w) of mannitol and PVA. The polymorphic form of mannitol is different in formulations with different mannitol:PVA concentration ratios. Mannitol occurs in the α-form at mannitol:PVA concentration ratios between 15:1 and 15:4 (w/w). Moreover, PVA affects the molecular motions in the region associated with the OH stretch, OH deformation, and CH2 wag of mannitol. In particular, the molecular motions change considerably at mannitol:PVA concentration ratio of 15:2.5 and 15:4 (w/w). In addition, the surface state of the sugarless layer depends on the amount of PVA added, and exhibits the smoothest surface at a mannitol:PVA concentration ratio between 15:2.5 and 15:4 (w/w). Thus, the hygroscopicity is related to the surface states of the sugarless layer, which, in turn, is affected by the change in the molecular motions of mannitol due to the interactions between mannitol and PVA.
authors.affiliation: Healthcare Research Institute, Wakunaga Pharmaceutical Co., Ltd. , 1624 Shimokotachi, Koda-cho, Akitakata-shi, Hiroshima 739-1195, Japan.
authors.forename: Masaharu
authors.initials: M
authors.lastname: Higuchi
authors.affiliation: Healthcare Research Institute, Wakunaga Pharmaceutical Co., Ltd. , 1624 Shimokotachi, Koda-cho, Akitakata-shi, Hiroshima 739-1195, Japan.
authors.forename: Shouko
authors.initials: S
authors.lastname: Tanaka
authors.affiliation: Healthcare Research Institute, Wakunaga Pharmaceutical Co., Ltd. , 1624 Shimokotachi, Koda-cho, Akitakata-shi, Hiroshima 739-1195, Japan.
authors.forename: Koichi
authors.initials: K
authors.lastname: Tamura
authors.affiliation: Department of Production & Technology, Wakunaga Pharmaceutical Co., Ltd. , 1624 Shimokotachi, Koda-cho, Akitakata-shi, Hiroshima 739-1195, Japan. Electronic address: takasa1137@hotmail.co.jp.
authors.forename: Yukoh
authors.initials: Y
authors.lastname: Sakata
mesh_terms: D005079:Excipients / Q000737:chemistry; D008353:Mannitol / Q000737:chemistry*; D018625:Microscopy, Atomic Force; D015394:Molecular Structure; D011142:Polyvinyl Alcohol / Q000737:chemistry*; D017550:Spectroscopy, Fourier Transform Infrared; D017155:Wettability
chemical_list: D005079:Excipients; D008353:Mannitol; D011142:Polyvinyl Alcohol
keywords: Crystallinity; Hygroscopicity; Mannitol; PVA; Polymorphic form; Sugarless layer; Surface states