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NDA 21-636 Zegerid omeprazole Powder for Oral Suspension DESCRIPTION The active ingredient in Zegerid omeprazole powder for oral suspension, is a substituted benzimidazole, 5- methoxy-2-[[ 4-methoxy-3, 5-dimethyl-2-pyridinyl methyl]sulfinyl]-1H-benzimidazole, a racemic mixture of two enantiomers that inhibits gastric acid secretion. Its empirical formula is C H N O S, with a molecular weight of 17 19 3 3 345.42. The structural formula is: Omeprazole is a white to off-white crystalline powder which melts with decomposition at about 155°C. It is a weak base, freely soluble in ethanol and methanol, and slightly soluble in acetone and isopropanol and very slightly soluble in water. The stability of omeprazole is a function of pH; it is rapidly degraded in acid media, but has acceptable stability under alkaline conditions. Zegerid Powder for Oral Suspension is supplied in unit dose packets as an immediate release formulation to be constituted with water for oral administration. Each packet contains 20 mg of omeprazole and the following excipients: sodium bicarbonate, sucrose, sucralose, xanthan gum, xylitol, and flavorings. CLINICAL PHARMACOLOGY Omeprazole is acid labile and thus rapidly degraded by gastric acid. Zegerid Powder for Oral Suspension is an immediate-release formulation that contains sodium bicarbonate to protect omeprazole from acid degradation. Pharmacokinetics: Absorption When Zegerid is administered on an empty stomach 1 hour prior to a meal, absorption of omeprazole is rapid, with mean peak plasma levels of omeprazole occurring at around 30 minutes range 10 to 90 minutes after a single dose or repeated once-daily administration see figures below . Mean Plasma Omeprazole Concentrations Days 1 and 7 Day 1 Day 7 The AUC 0-inf ng*hr/mL was 1446 after 7 days of 20 mg daily doses and the Tmax was approximately 30 minutes. Following single or repeated once daily dosing, peak plasma concentrations of omeprazole from Zegerid