In Vitro and Human Pharmacoscintigraphic Evaluation of an Oral 5-ASA Delivery System for Colonic Release

Publication date: Available online 16 October 2019Source: International Journal of PharmaceuticsAuthor(s): Anastasia Foppoli, Alessandra Maroni, Saliha Moutaharrik, Alice Melocchi, Lucia Zema, Luca Palugan, Matteo Cerea, Andrea GazzanigaAbstract5-aminosalicylic acid (5-ASA) is the most widely used drug for the treatment of ulcerative colitis. The benefits of targeted delivery of 5-ASA to the large intestine are well known, resulting in reduced systemic absorption and increased local concentrations at the disease site. In the present study, a 5-ASA colon delivery system based on the time-dependent strategy, exploiting the relatively consistent small intestinal transit time (SITT), was manufactured and evaluated in vitro as well as in vivo. The system was obtained by successive spray-coating of an immediate-release tablet core with low-viscosity HPMC and Eudragit® L. The enteric film was effective in preventing release during the acidic stage of the in vitro test, while the HPMC coating brought about reproducible lag phases prior to release in phosphate buffer medium. A γ-scintigraphy investigation pointed out that, following administration to fasted and fed volunteers, disintegration of the units never occurred prior to colon arrival. In all cases, a lag time preceded the appearance of the drug and its N-acetyl metabolite in the bloodstream, which was found to correlate with the time of disintegration in a linear mode. The plasma levels of the drug and metabolite as well as ...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research