Wax beads as cushioning agents during the compression of coated diltiazem pellets

Eur J Pharm Sci. 2002 Nov;17(3):145-51. doi: 10.1016/s0928-0987(02)00164-1.

Abstract

Placebo particles were mixed with film-coated diltiazem pellets to evaluate them as cushioning agents during tabletting in order to protect the film coat from damage. The cushioning properties of alpha-lactose monohydrate granules, microcrystalline cellulose pellets and wax/starch beads were evaluated by comparing the dissolution profile of the coated pellets before and after compression (compression force 10 kN). Only the tablet formulations containing wax/starch beads provided protection to the film coat. However, the dissolution rate of tablets formulated with waxy maltodextrin/paraffinic wax placebo beads was too slow as the tablets did not disintegrate. Adding 50% (w/w) drum-dried corn starch/Explotab/paraffinic wax beads to the formulation was the optimal amount of cushioning beads to provide sufficient protection for the film coat and yield disintegrating tablets. Using a compression simulator, the effect of precompression force and compression time on the dissolution rate was found to be insignificant. The diametral crushing strength of tablets containing 50% (w/w) drum-dried corn starch/Explotab/paraffinic wax beads was about 25.0 N (+/-0.3 N), with a friability of 0.4% (+/-0.04%). This study demonstrates that adding deformable wax pellets minimizes the damage to film-coated pellets during compression.

MeSH terms

  • Compressive Strength
  • Diltiazem / chemistry*
  • Diltiazem / pharmacokinetics
  • Polymethacrylic Acids / chemistry*
  • Polymethacrylic Acids / pharmacokinetics
  • Solubility
  • Tablets, Enteric-Coated
  • Waxes / chemistry*
  • Waxes / pharmacokinetics

Substances

  • Polymethacrylic Acids
  • Tablets, Enteric-Coated
  • Waxes
  • methylmethacrylate-methacrylic acid copolymer
  • Diltiazem