Optimization and Advantages of Molded Tablets Using Trehalose as a Binder

Chem Pharm Bull (Tokyo). 2023;71(6):416-423. doi: 10.1248/cpb.c23-00090.

Abstract

Molded tablets are manufactured by molding wet powder at low pressure and drying. Typically, water-soluble polymers are used as a binder; however, the ratio to achieve both tablet strength and rapid disintegration is limited, and designing an optimal formulation according to the active ingredients can be challenging. In addition, production may be temporarily interrupted owing to the adherence of wet powder to the inside of the mortar, which can hamper stable production. Therefore, optimization was performed by design of experiments to utilize the disaccharide trehalose as a binder for molded tablets. We formulated placebo tablets with high tablet strength and rapid disintegration. On examining the tablet interior, we confirmed the formation of solid bridges between particles and high porosity, suggesting that trehalose can be used as a binder for molded tablets. The viscosity of the trehalose saturated solution was lower than that of the polyvinyl alcohol (PVA) solution (3.8 wt%). Moreover, the trehalose formulation exhibited a significantly lower wet powder adhesion rate to the upper punch than the PVA formulation. This study provided valuable results for the future formulation design of molded tablets.

Keywords: design of experiment; molded tablet; optimization; porosity; trehalose.

MeSH terms

  • Polymers*
  • Polyvinyl Alcohol
  • Porosity
  • Powders
  • Solubility
  • Tablets
  • Trehalose*

Substances

  • Trehalose
  • Powders
  • Polymers
  • Polyvinyl Alcohol
  • Tablets