Raft-forming gastroretentive tablets incorporating solidly dispersed Curcumin-Eudragit E100; in vitro and in vivo approaches for treatment of gastric ulcer.

Most common complications of the gastric ulcer are hemorrhage, perforation, ulcer penetration into adjacent organs, and gastric outlet obstruction which can be fatal if untreated. The present study aimed to improve gastric ulcer complications by using naturally occurring compound curcumin (Cur) and its modified complex with Eudragit E-100 (SD-Cur-Eud2). Solubility of Cur was enhanced by using first-generation solid dispersion (SD) technique and confirmed by physicochemical analysis. Optimized SD-Cur-Eud2 was used for the compression of gastroretentive raft tablets (SD-Cur-Eud2-RT) by direct compression method, and all quality control tests, in vitro floating time, raft resilience, in vitro dissolution studies, and dissolution efficiency were also observed. Stability studies were performed to estimate shelf life by using Rgui software. All the confirmatory tests of SD-Cur-Eud2-RT were found within limits according to pharmacopeial standards. 60–70% release of Cur within 6 h in acidic medium (pH = 1.2), 40–65% permeation on rat gastric mucosa, and 68% ulcer inhibition in Indomethacin® (IND) induced gastric ulcer. Furthermore, cumulative amount of diffused (CADD), flux (J_ss) and permeability coefficient (K_p) of Cur were six–tenfold increased with shelf life of 23 months. Fortunately, SD-Cur-Eud2-RT (50 mg/kg once daily) tablets exhibited better therapeutic effect on gastric ulcers in terms of ulcer index 2.5 ± 0.2 as compared to Omeprazole®. SD-Cur-Eud2-RT may be considered an alternative of already available proton-pump inhibitors for the treatment of gastric ulcers with minimum side effects. [ABSTRACT FROM AUTHOR]