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Levofloxacin is a synthetic broad spectrum antibacterial agent for oral administration. Chemically, levofloxacin, a chiral fluorinated carboxyquinolone, is the pure (-)-(S)-enantiomer of the racemic drug substance ofloxacin. The chemical name is (-)-(S)-9-fluoro-2 ,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl) -7-oxo-7H-pyrido[1,2,3-de]-1, 4-benzoxazine-6-carboxylic acid hemihydrate.

Its empirical formula is C₁₈H₂₀FN₃O₄•½H₂O and its molecular weight is 370.38. Levofloxacin is a light yellowish-white to yellow-white crystal or crystalline powder. The molecule exists as a zwitterion at the pH conditions in the small intestine.

The data demonstrates that from pH 0.6 to 5.8, the solubility of levofloxacin is essentially constant (approximately 100 mg/ml). Levofloxacin is considered soluble to freely soluble in this pH range, as defined by USP nomenclature. Above pH 5.8, the solubility increases rapidly to its maximum at pH 6.7 (272 mg/ml) and is considered freely soluble in this range. Above pH 6.7, the solubility decreases and reaches a minimum value (about 50 mg/ml) at a pH of approximately 6.9.

Levofloxacin has the potential to form stable coordination compounds with many metal ions. This in vitro chelation potential has the following formation order: Al⁺³>Cu⁺²>Zn⁺²>Mg⁺²>Ca⁺².

Levaquin tablets are available as film-coated tablets and contain the following active ingredients: 250 mg (as expressed in the anhydrous form): hydroxypropyl methylcellulose, crospovidone, microcrystalline cellulose, magnesium stearate, polyethylene glycol, titanium dioxide, polysorbate 80 and synthetic red iron oxide. 500 mg (as expressed in the anhydrous form): hydroxypropyl methylcellulose, crospovidone, microcrystalline cellulose, magnesium stearate, polyethylene glycol, titanium dioxide, polysorbate 80 and synthetic red and yellow iron oxides.