Development and evaluation of a hot-melt coating technique for enteric coating

Abstract

Conventional enteric coating requires the use of organic based polymers which are equally hazardous to the environment and operating personnel. Hot-melt coating avoids the use of solvents and is a safer and time-saving process. The present study was designed to assess the efficacy of hot-melt coating (HMC) as an enteric coating technique. Pellets prepared by extrusion spheronization were selected as the core formulation for a model of the gastric irritant drug diclofenac sodium (DFS) because of their innate advantages over single-unit formulations. Stearic acid (SA) and palmitic acid (PA) were evaluated as enteric hot-melt coating materials. HMC was carried out in a specially modified coating pan by applying SA and PA in molten state onto preheated pellets to achieve a coating level of 5-15 %w/w. Hot-melt coated pellets were evaluated for disintegration pH and in vitro dissolution in the pH range 1.2 to 6.8, along with basic micromeritics. SEM of coated pellets showed a uniform and smooth coating. These results indicated that HMC of both SA and PA exhibited very good enteric coating ability. The coated pellets showed negligible drug release in acidic pH. As the pellets were subsequently transferred to a higher pH level, a gradual increase in release of the drug from the pellets was observed with increasing pH of the dissolution media. The release was dependent upon coating extent, providing sustained enteric release as opposed to abrupt release with mixed release kinetics.