Effect of Moisture on Impact Toughness of Sugar-Coated Tablets Manufactured by the Dusting Method

Abstract

Moisture is one of the most important factors for clarifying the characteristics of solid dosage forms in the pharmaceutical field. There have been a number of reports regarding the effects of moisture on physicochemical properties such as stability of drugs, 1) compactibility of drugs and excipients, 2,3) friability of tablets, 4) and amorphous-to-crystalline transformation 5,6) in solid dosage forms. Moisture in solid dosage forms has attracted much interest over the last decade. Much research is currently in progress.Moisture in solid dosage forms is generally classified into mobile and immobile water.1,7-9) The measurement of mobile water is expressed by water activity or equilibrium relative humidity (ERH). The water activity of a substance is defined as the ratio of the vapor pressure of water due to the substance to the vapor pressure of pure water at the same temperature. ERH is water activity expressed as a percentage.9) Since the amount of mobile water is critical to physicochemical properties on tablets and ERH is easy to measure, we used ERH as a parameter of moisture content in tablets in this study.In our previous work, 10) we proposed a new dusting method for improvement of impact toughness of sugarcoated tablets. The new dusting method uses a dusting powder containing microcrystalline cellulose (MCC). There have been a number of reports regarding the effect of moisture on MCC properties and the moisture sorption and desorption of MCC. [11][12][13][14] Fielden et al. reported that MCC was capable of physically retaining a high percentage of water within itself, while also allowing easy removal by evaporation.11) Suzuki et al. reported that the physical structure of MCC changed during the wet granulation process, and the interaction between MCC and water was gradually strengthened.12) Moisture thus affects the physical properties of MCC.Although there have been several reports regarding the relationship between moisture and color change on sugarcoated tablets, 15-17) the effect of moisture on impact toughness of sugar-coated tablets has not been sufficiently clarified. Above all, the effect of moisture on impact toughness of sugar-coated tablets with MCC has not been sufficiently clarified. Therefore, the purpose of this study was to clarify the effect of moisture on the impact toughness of sugar-coated tablets manufactured by the dusting method. Furthermore, we conducted a free fall test for evaluation of impact toughness of sugar-coated tablets with low moisture content manufactured by the dusting method using dusting powder with or without MCC. We also investigated the relationship between the friability test and the free fall test. ExperimentalMaterials Core tablets containing fursultiamine hydrochloride, vitamin B 6 , vitamin B 12 . vitamin E were used. The weight, diameter, radius of curvature and thickness of core tablets were 180 mg, 8 mm, 6.5 mm, 4.25 mm, respectively. Sucrose (Ensuiko Sugar Refining Co.), talc (Matsumura Sangyo Co.), precipitated calcium carbonate (Nitto Funka Kougyo Co.)...

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“…Ohmori et al . () found that incorporating 20% MCC in the subcoating layer of sugar‐coated tablets by dusting method improved the wettability of the subcoating layer and increased the surface roughness of the subcoating and resistance against impact to the tablets.…”