A unique dosage form to evaluate the mechanical destructive force in the gastrointestinal tract.

ABSTRACT

The purpose of this study was to prepare tablets that could evaluate the destructive force in the gastrointestinal (GI) tract. Many factors are known to affect in vivo drug release from oral dosage forms. There is still relatively little information on the mechanical destructive force in the GI tract. Press-coated tablets with an extremely brittle outer layer were developed using a unique, highly hydrophobic Teflon powder that could be shaped with weak compression force. A marker drug contained in the tablets was released only when the tablets received a force larger than its predetermined crushing strength. We referred to this type of tablet as a 'destructive force dependent release system' (DDRS). A total of nine healthy, male subjects were orally administered the tablets under fed and/or fasting conditions. Tablets with a predetermined crushing strength of 1.50 N were crushed by all of the four subjects who took them under fed conditions and two of the five subjects under fasting conditions. Tablets with a crushing strength of 1.89 N were crushed by two of the six subjects who took them under fed conditions and none of the five subjects under fasting conditions. The range of mechanical destructive force in the human stomach was obtained.