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Rifaximin-d6 is intended for use as an internal standard for the quantification of rifaximin by GC- or LC-MS. Rifaximin is an antibiotic derived from rifamycin SV that inhibits the growth of a variety of Gram-positive and Gram-negative bacteria in vitro, including Staphylococcus, Streptococcus, Enterococcus, H. influenzae, and N. gonorrhoeae (MIC50s = ≤0.015, <0.12, 0.25-2, 0.25, and 0.25 μg/mL, respectively).1 It is a pregnane X receptor (PXR) agonist (EC50 = ~20 μM) that reduces colonic damage, rectal bleeding, and diarrhea in PXR-humanized, but not wild-type or Pxr-null, mice with inflammatory bowel disease (IBD) induced by dextran sulfate sodium .2,3 Rifaximin exhibits minimal intestinal absorption after oral administration and is, therefore, effective in eliminating bacteria in the gastrointestinal system.4,5 Formulations containing rifaximin have been used in the treatment of traveler's diarrhea caused by noninvasive E. coli, irritable bowel syndrome with diarrhea (IBS-D), and to reduce the risk of recurrence of overt hepatic encephalopathy.

1.Hoover, W.W., Gerlach, E.H., Hoban, D.J., et al.Antimicrobial activity and spectrum of rifaximin, a new topical rifamycin derivativeDiagn. Microbiol. Infect. Dis.16(2)111-118(1993) 2.Ma, X., Shah, Y.M., Guo, G.J., et al.Rifaximin is a gut-specific human pregnane X receptor activatorJ. Pharmacol. Exp. Ther.322(1)391-398(2007) 3.Cheng, J., Shah, Y.M., Ma, X., et al.Therapeutic role of rifaximin in inflammatory bowel disease: Clinical implication of human pregnane X receptor activationJ. Pharmacol. Exp. Ther.335(1)32-41(2010) 4.Alajbegovic, S., Sanders, J.W., Atherly, D.E., et al.Effectiveness of rifaximin and fluoroquinolones in preventing travelers' diarrhea (TD): A systematic review and meta-analysisSyst. Rev.1:39(2012) 5.Song, M., and Ang, T.L.Second and third line treatment options for Helicobacter pylori eradicationWorld J. Gastroenterol.20(6)1517-1528(2014)

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