Effect of formulated ingredients on rapidly disintegrating oral tablets prepared by the crystalline transition method

Chem Pharm Bull (Tokyo). 2006 Feb;54(2):175-80. doi: 10.1248/cpb.54.175.

Abstract

The aim of this article was to determine the optimal ingredients for the rapidly disintegrating oral tablets prepared by the crystalline transition method (CT method). The effect of ingredients (diluent, active drug substance and amorphous sugar) on the characteristics of the tablets was investigated. The ingredients were compressed and the resultant tablets were stored under various conditions. The oral disintegration time of the tablet significantly depended on diluents, due to differences in the penetration of a small amount of water in the mouth and the viscous area formed inside the tablet. The oral disintegration time was 10-30 s for tablets with a tensile strength of approximately 1 MPa, when erythritol, mannitol or xylitol was used as the diluent. The increase in the tensile strength of tablets containing highly water-soluble active drug substances during storage was as large as that of tablets without active drug substances, while the increase in the tensile strength of tablets containing low water-soluble active drug substances was small. It was therefore found that highly water-soluble active drug substances were more suitable for the formulation prepared by the CT method than low water-soluble active drug substances. Irrespective of the type of amorphous sugar (amorphous sucrose, lactose or maltose) used, the porosity of tablets with 1 MPa of tensile strength was 30-40%, and their oral disintegration time was 10-20 s. The optimal ingredients for rapidly disintegrating oral tablets with reasonable tensile strength and disintegration time were therefore determined from these results.

MeSH terms

  • Absorption
  • Administration, Oral
  • Carbohydrates
  • Chemistry, Pharmaceutical / methods*
  • Crystallization
  • Crystallography, X-Ray
  • Excipients
  • Humidity
  • Lactose
  • Porosity
  • Solubility
  • Tablets*
  • Tensile Strength
  • Thermodynamics

Substances

  • Carbohydrates
  • Excipients
  • Tablets
  • Lactose