Effects of magnesium-aluminum hydroxide and calcium carbonate antacids on bioavailability of ofloxacin

Abstract

The effects of 15-and 5-ml doses of magnesium-aluminum hydroxide (MAH) and calcium carbonate (CC) antacids, respectively, on the bioavailability of ofloxacin after single oral 400-mg doses of ofloxacin were investigated in a 32-subject, randomized, crossover, open-label study. On four separate occasions, subjects received ofloxacin alone or antacid 24 h before, 2 h before, or 2 h after ofloxacin administration (n = 16 for each antacid). CC administration had no significant effect on the rate and extent of ofloxacin absorption regardless of the timing of antacid administration. A small but significant negative effect of MAH administration 2 h before ofloxacin administration was noted as evidenced by area under the curve and peak concentration in plasma data. Simultaneous administration of ofloxacin with either antacid was not investigated in this study. It appears that MAH and CC antacids in the doses used in this study generally do not interfere in a clinically significant manner with the bioavailability of ofloxacin, provided that an interval of at least 2 h separates the administration of these products.Ofloxacin is a synthetic carboxyquinolone antimicrobial agent which exhibits broad-spectrum in vitro bactericidal activities against gram-positive and gram-negative aerobes (8). The clinical efficacy of ofloxacin has been documented in patients with respiratory tract, upper and lower urinary tract, gonococcal and nongonococcal urethritis, and skin and soft tissue infections (8,14).Coadministration of some antacids and sucralfate has resulted in diminished absorption of several of the carboxyquinolones. This phenomenon has been reported to be due to the formation of insoluble chelates in the gastrointestinal tract (5-7, 9-12). Although the majority of these interaction studies have investigated the quinolone ciprofloxacin, four reports have suggested the existence of a similar interaction between antacids and ofloxacin (7,12; G. Hoffken 19:848-850, 1987).This study was designed to rigorously characterize the interaction potential between ofloxacin and two commonly used antacid preparations: (i) magnesium-aluminum hydroxide (Maalox; Rorer Pharmaceutical Corp., Fort Washington, Pa.) and (ii) calcium carbonate (Titralac; 3M Riker, St. Paul, Minn.).The study was approved by the Human Subjects Research Committee, Hennepin County Medical Center. Thirty-two normal, healthy male volunteers who participated in the study were between the ages of 18 and 40 years, and all subjects gave written, informed consent prior to participation. The patients were healthy, as determined by comprehensive medical history, physical examination, electrocardiography, and laboratory profiles. None of the subjects was taking medications within 1 week before or during the study. None of the subjects had a history or current evidence of * Corresponding author. significant renal, hepatic, cardiovascular, hematologic, neurologic, psychiatric, respiratory, or metabolic disease.A parallel study design was followed wherein 16 subjects were rando...

Effect of an antacid containing magnesium and aluminum on absorption, metabolism, and mechanism of renal elimination of pefloxacin in humans

“…However, when the order of intake was changed and ciprofloxacin was given 2 h before the antacid, no absorption impairment was observed (18). Similar results were reported for ofloxacin (5).…”

“…Pefloxacin is a newer quinolone carboxylic acid derivative with a broad spectrum of activity (3). A decrease in the bioavailability of several quinolones after concomitant intake of magnesium-aluminum hydroxide has recently been described elsewhere (5,9,13,18,19) and reviewed (4,24). However, the extent of this interaction among individual quinolones, was quite different, which makes a prediction of the extent of the effect of the antacid on new derivatives difficult.…”

Roles of divalent cations and pH in mechanism of action of nitroxoline against Escherichia coli strains

“…On the other hand, such a complexation between NIT and metal ions would also limit the absorption of this compound by the human gastrointestinal tract because of the formation of insoluble chelates. Indeed, a reduced bioavailability has especially been shown for quinolones in the presence of magnesium, iron, and aluminum, which are commonly found in antacids (17,29,48).…”

“…Inasmuch as there have been many reports in the literature indicating that different metal ions affect the antimicrobial activities (1, 6, 15, 21, 39), bacterial uptake (12), and bioavailabilities (17,29,48) of numerous antibiotics, we were interested in studying how some metal ions affect the activity of NIT against E. coli strains.…”

Precipitated Calcium Carbonate Nano-Microparticles: Applications in Drug Delivery

“…Due to its high biocompatibility, CaCO 3 is also employed in many pharmaceutical (anti-acid, dietary supplement for child and postmenopausal women), biological (scaffolds for cellular and bacterial growth) and biomedical (bioactive material for drug delivery, base for orthodontic cements) applications. [5][6][7][8][9] Its particles can be found as three different polymorphs (vaterite, µ-CaCO 3 , aragonite, λ-CaCO 3 , and calcite, β-CaCO 3 ) in a wide variety of size, shape and crystalline structure of different properties and characteristics.…”