Rebamipide D4

Rebamipide-d₄ is intended for use as an internal standard for the quantification of rebamipide by GC- or LC-MS. Rebamipide is a gastroprotective agent and mucin secretagogue.^1,2 It increases the levels of prostaglandin E₂ and COX-2 in rat gastric mucosa when administered at doses of 15 and 50 mg/kg per day. Rebamipide (30 and 100 mg/kg, i.p.) prevents the formation of gastric ulcers induced by absolute ethanol, sodium hydroxide, or hydrochloric acid in rats, an effect that can be blocked by the non-selective COX inhibitor indomethacin .³ It also increases the production of mucin 16 in stratified corneal epithelial cells in vitro when used at concentrations of 10 and 100 ?M.² Rebamipide (1% w/v) increases the levels of mucin-like substances in rabbit conjunctiva and cornea and, in a rabbit model of dry eye disease, reduces desiccation-induced corneal damage.⁴ Formulations containing rebamipide have been used in the treatment of peptic ulcer disease and dry eye disease.

1.Sun, W.H., Tsuji, S., Gunawan, E.S., et al.Induction of cyclooxygenase-2 in rat gastric mucosa by rebamipide, a mucoprotective agentPharmacol. Exp. Ther.295(2)447-452(2000) 2.Uchino, Y., Woodward, A.M., and Argüeso, P.Differential effect of rebamipide on transmembrane mucin biosynthesis in stratified ocular surface epithelial cellsExp. Eye Res.1531-7(2016) 3.Yamasaki, K., Kanbe, T., Chijiwa, T., et al.Gastric mucosal protection by OPC-12759, a novel antiulcer compound, in the ratEur. J. Pharmacol.142(1)23-29(1987) 4.Urashima, H., Takeji, Y., Okamato, T., et al.Rebamipide increases mucin-like substance contents and periodic acid Schiff reagent-positive cells density in normal rabbitsJ. Ocul. Pharmacol. Ther.28(3)264-270(2012)