Potential use of oral jelly formulations as supersaturable formulations: Acidified or alkalized jelly containing drugs with pH-dependent solubility

Abstract

This study evaluates the potential of oral jelly formulations as supersaturable drug delivery systems for drugs with pH-dependent solubility, particularly in overcoming changes in gastric pH due to aging or medications. We prepared an oral jelly formulation of dipyridamole, a basic drug, by acidifying the jelly to pH 3. The stability of the acidified jelly was assessed over 28 days, with no precipitation. For comparison, a drug suspension and a neutral jelly were also tested. In vitro dissolution tests were conducted using 200 mL of Japanese Pharmacopoeia (JP) test fluids 2 (pH 6.8). Additionally, in vivo intestinal administration studies, bypassing gastric dissolution, were performed in rats to assess dipyridamole absorption. The acidified jelly showed a rapid, supersaturated dissolution profile in vitro. In vivo, the area under the curve (AUC) of dipyridamole from the acidified jelly was about 13 times higher than that of the suspension or neutral jelly. An alkalized jelly of telmisartan, an amphoteric drug, was also prepared at pH 10, showing a supersaturable dissolution profile in vitro and enhanced absorption in vivo. Acidified and alkalized jellies effectively serve as supersaturable formulations for basic and amphoteric drugs, with potential to improve oral absorption even under elevated gastric pH.