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

The purpose of this study was to prepare tablets that could evaluate the de structive force in the gastrointestinal (GI) tract. Many Factors are known to affect in vivo drug release from oral dosage forms, There is still relat ively little information on the mechanical destructive force in the GI trac t. Press-coated tablets with an extremely brittle outer layer were develope d using a unique, highly hydrophobic Teflon powder that could be shaped wit h weak compression force. A marker drug contained in the tablets was releas ed only when the tablets received a force larger than its predetermined cru shing strength. We referred to this type of tablet as a 'destructive force dependent release system' (DDRS). A total of nine healthy, male subjects we re orally administered the tablets under fed and/or fasting conditions. Tab lets with a predetermined crushing strength of 1.50 N were crushed by all o f 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 conditio ns and none of the five subjects under fasting conditions. The range of mec hanical destructive force in the human stomach was obtained. (C) 2000 Elsev ier Science B.V. All rights reserved.