Gamma scintigraphic evaluation of film-coated tablets intended for colonic or biphasic release

Int J Pharm. 2004 Feb 11;270(1-2):307-13. doi: 10.1016/j.ijpharm.2003.11.009.

Abstract

The gastrointestinal transit and in vivo drug release behaviour of a film-coated tablet formulation was investigated in five healthy human subjects using the technique of gamma scintigraphy. The film coating system consisted of a mixture of pectin, chitosan and HPMC in a ratio of 6:1:0.37 applied to 750 mg cores at a coat weight gain of 9%. The estimated mean values of the gastric emptying time (62+/-17 min), small intestinal transit time (219+/-53 min), ileocaecal junction lag time (79+/-30 min) and the colon arrival time (345+/-33 min), were similar to published values for the transit of similar sized tablets in humans. The amount of radioactive tracer released from the labelled tablets was minimal when the tablets were in the stomach and the small intestine. There was increased release of radioactivity when the tablets were in the colon due to increased degradation of the film coatings by pectinolytic enzymes resident in the colon. The pectin/chitosan/HPMC film coating system thus acts as a colonic delivery system.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetaminophen / chemistry
  • Administration, Oral
  • Adult
  • Chitin / analogs & derivatives*
  • Chitin / chemistry
  • Chitosan
  • Colon / diagnostic imaging
  • Colon / metabolism*
  • Delayed-Action Preparations
  • Drug Stability
  • Gastric Emptying
  • Gastrointestinal Transit
  • Humans
  • Lactose / analogs & derivatives*
  • Lactose / chemistry
  • Male
  • Methylcellulose / analogs & derivatives*
  • Methylcellulose / chemistry
  • Oxazines
  • Pectins / chemistry
  • Radionuclide Imaging
  • Tablets, Enteric-Coated / chemistry
  • Tablets, Enteric-Coated / pharmacokinetics*
  • Time Factors

Substances

  • Delayed-Action Preparations
  • Oxazines
  • Tablets, Enteric-Coated
  • Chitin
  • Acetaminophen
  • Pectins
  • Methylcellulose
  • Chitosan
  • MK 458
  • Lactose