Article révisé par les pairs
Résumé : Previous published works have shown that hydrodynamically balanced systems (HBS) - i.e. sustained release oral dosage forms with a specific gravity lower than 1 and remaining buoyant on the gastric juice of the stomach - can have an enhanced gastrointestinal transit time. For this investigation, a double-layer sustained release compressed hydrophilic matrix was formulated in order to achieve a foreseeable and reproducible flotation of the tablet. A carbon dioxide generating blend was, for this purpose, added to one of the layers, this gas being entrapped in the gelified hydrocolloid as liberated by the action of the gastric medium. The in vivo behaviour of this floating tablet was then compared to a classical HBS capsule and to a similar but non-floating double-layer hydrophilic matrix on subjects alternatively in fasted or fed state. As these three dosage forms contain a riboflavin (RF) soluble derivative, it was possible to measure the RF urinary excretion rates and, consequently, to conclude that in vivo buoyancy is preponderant over bioadhesion for both floating capsules and tablets. These dosage forms also significantly increase the gastric residence time when compared to the non-floating dosage form. Compared to the classical HBS capsule, the floating tablet is showing in vivo equivalent floating properties when administered after a light meal and higher RF urinary excretion rates when administered to fasted subjects. © 1987.