Activated charcoal dispersion of carbon monoxide prodrugs for oral delivery of CO in a pill.

ABSTRACT: A novel orally bioavailable solid formulation to deliver a gaseous signaling molecule, carbon monoxide (CO), was developed by adsorbing oxalyl saccharin, a newly developed organic CO prodrug, in activated charcoal (AC). The resulting solid dispersion formulation addresses key developability issues of this CO prodrug. By taking advantage of the large surface area of AC, the paradoxical problem of low water solubility of the prodrug and the requirement of hydrolysis to release CO is resolved, and the need for an organic cosolvent is completely circumvented. The AC formulation also mitigates the adverse effect of low pH on the CO release yield, allowing steady CO release in simulated gastric and intestine fluids. This formulation allows encapsulation in normal and enteric-coated gel capsules,

SUBMITTER: Yang X 

PROVIDER: S-EPMC9060424 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature