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PubMed2001

Cefuroxime antacid interactions.

Cefuroxime sodium a second generation semi-synthetic cephalosporin is effective for treating meningitis, lower respiratory tract infections, gonorrhea, bone and joint infections and is approved for surgical prophylaxis. There are number of synergistic and as well as antagonistic drug interactions reported for this antibiotic. Withstanding to gastric irritations caused by this antibiotic, antacids may possibly be co-administered with cefuroxime, which may result in severe adverse drug interaction. The present work describes the effect of magnesium carbonate, magnesium hydroxide, magnesium trisilicate, megaldrate powder, sodium bicarbonate, aluminum oxide and simethicone suspension on the in vitro availability of cefuroxime sodium. The mechanism of interaction between antibiotic and antacids was also studied.

Journal Article↗
PubMed1990

Stability of nizatidine in extemporaneous oral liquid preparations.

The stability of nizatidine in extemporaneous oral liquid preparations stored at room and refrigerated temperatures was studied. Preparations containing nizatidine in a final concentration of approximately 2.5 mg/mL were made by mixing the contents of a 300-mg nizatidine capsule with commercial juices (Gatorade, Stokely-Van Camp; Cran-Grape, Ocean Spray; apple juice, Sundor Brands; and V8 vegetable juice, Campbell Soup) and with aluminum hydroxide-magnesium hydroxide suspension (Maalox, Rorer). A control solution was prepared in water. Samples of each preparation were stored at 15-30 degrees C and at 5 degrees C. Initially and after 4, 8, 24, and 48 hours of storage, the samples were visually inspected, tested for pH, and analyzed in triplicate by high-performance liquid chromatography for nizatidine content. No appreciable changes in appearance or pH occurred. The only extemporaneous preparations with greater than 10% loss of nizatidine potency at 48 hours were the Cran-Grape and V8 preparations at room temperature. There was no correlation between pH of the preparations and changes in drug concentration. In the Maalox and V8 preparations, the drug powder did not dissolve uniformly. In all the preparations tested, nizatidine was stable for at least eight hours at refrigerated and room temperatures. In all except the Cran-Grape and V8 preparations, the drug was stable for 48 hours under both storage conditions.

Administration, Oral↗
PubMed1985

[Protective effect of two antacids in acute acetylsalicylic acid-induced injuries to the human gastric mucosa].

The present study deals with the protective effect of a pretreatment period with antacids (preparation A = gastropulgit) 50; 1 bag with suspension corresponding to 12.5 g contains: 1 g attapulgite, 1.8 g aluminium hydroxide-magnesium carbonate gel and 0.7 g sorbitol. Reference preparation B = commercial product; 1 bag with suspension corresponding to 10 ml contains: 600 mg magnesium hydroxide and 9 g aluminium hydroxide gel) on the acute acetylsalicylic acid (ASA)-induced lesions of gastric mucosa in man. 8 healthy volunteers received in a double-blind crossover design 1 or 2 bags of the antacids or placebo 15 min prior to 1500 mg p.o. of ASA. Endoscopy was performed 2 h later. In the placebo experiments ASA caused severe lesions in all volunteers (placebo values, study with preparation A: 2.9 +/- 0.1; study with preparation B: 2.8 +/- 0.2). Pretreatment with either one bag reduced the ASA-injuries to 2.2 +/- 0.3) (preparation A) and 2.1 +/- 0.3 (preparation B) (not significant compared with placebo). By contrast, a significant protection of human gastric mucosa against ASA could be achieved with 2 bags of preparation A, but not with 2 bags of preparation B (1.5 +/- 0.3, p less than 0.05; 1.9 +/- 0.3, p less than 0.05). The majority of the volunteers reported less discomfort evoked by ASA under the higher antacid doses.

Adult↗
PubMed1983

Studies on the in vitro interaction of D-penicillamine with antacids.

Interactions of D-penicillamine with various antacids (aluminum hydroxide-magnesium hydroxide, AH-MH; aluminum hydroxide-calcium carbonate, AH-CC; dihydroxy sodium aluminum carbonate, DSAC; aluminum hydroxide, AH) were studied in vitro. Only a small binding to AH-MH (29.2 +/- 7.2 mumol/g antacid) and AH (13.6 +/- 4.0 mumol/g antacid) and no adsorption at all to AH-CC and DSAC were observed. Bile salts and bicarbonate as well as the pH did not influence binding. Although extrapolations from in vitro studies to in vivo conditions are hazardous, clinically relevant interactions of D-penicillamine with antacids in patients ingesting both drugs in the usual dose range simultaneously appear unlikely.

Adsorption↗
PubMed1993

Trabecular bone density in a two year controlled trial of peroral magnesium in osteoporosis.

Since magnesium regulates calcium transport, and magnesium replacement in magnesium-deficient postmenopausal patients resulted in unexpected improvement in documented osteoporosis, we investigated the effect of magnesium treatment on trabecular bone density in postmenopausal osteoporosis. Thirty-one postmenopausal patients (mean age +/- SD = 57.6 +/- 10.6 years), consecutively admitted to the Back Rehabilitation Unit with musculoskeletal pain of non-malignant origin and bone density values of < or = 1.19 g/cm3 (measured by Compton Bone Densitometer), received two to six tablets daily of 125 mg each of magnesium hydroxide (Magnesium Magma USP/; 'Mazor', Israel) for 6 months and two tablets for another 18 months in a 2 year, open, controlled therapeutic trial. Twenty-three symptom-free postmenopausal women (mean +/- SD = 61.2 +/- 6.2 years) whose bone density was concurrently assessed at the same laboratory and who were found to have osteoporosis but refused treatment, served as controls. No new fractures occurred. Twenty-two patients (71 per cent) responded by a 1-8 per cent rise of bone density. The mean bone density of all treated patients increased significantly after 1 year (P < 0.02) and remained unchanged after 2 years (P > 0.05). The mean bone density of the responders increased significantly both after one year (P < 0.001) and after 2 years (P < 0.02), while in untreated controls, the mean bone density decreased significantly (P < 0.001). The disparity between the initial mean bone density and bone density after one year in all osteoporotic patients and in the responders differed significantly from that of the controls (both P < 0.001).(ABSTRACT TRUNCATED AT 250 WORDS)

Bone Density↗
PubMed1993

Characterization of antacid compounds containing both aluminum and magnesium. II. Codried powders.

The composition and antacid properties of six samples of codried antacids containing both aluminum and magnesium were determined. Aluminum hydroxide-magnesium carbonate codried gel and aluminum hydroxide-magnesium hydroxide codried gel were non-homogeneous, as the samples contained combinations of hydrotalcite, amorphous aluminum hydroxide, magnesium hydroxide, magnesium hydroxycarbonate, and magnesium carbonate. All samples passed the preliminary antacid test and had high acid neutralizing capacities. However, the rate of acid neutralization varied between samples. In some cases the rate of acid neutralization at a dose of 400 mg was too slow to raise the pH to 3.0 as required by the Rossett-Rice test.

Aluminum↗
PubMed1983

Plasma aluminium levels in patients on maintenance haemodialysis fall when oral aluminium hydroxide is withdrawn.

In 25 patients on maintenance haemodialysis the mean predialysis plasma aluminium level fell on two occasions when oral aluminium hydroxide was withdrawn for seven and twelve weeks. Substitution of half the prescribed dose of aluminium hydroxide with magnesium hydroxide led to a significant lowering of predialysis plasma aluminium levels over seven months, with no change in plasma phosphate levels. Oral magnesium hydroxide was associated with a mild rise in plasma magnesium levels.

Administration, Oral↗
PubMed1993

Lack of effect of magnesium-aluminium hydroxide on the absorption of theophylline given as a pH-dependent sustained release preparation.

Antacids can modify the pharmacokinetic parameters of sustained-release preparations of theophylline by changing the gastric pH. Though this has been studied with various theophylline/antacid combinations, the specific preparations investigated here have not previously been tested. The objective of the study was to assess any change in the availability of theophylline from a sustained-release preparation (SR), induced by the coadministration with an antacid. The study was designed as a double-blind randomized crossover trial in the Pneumology Departments of three general hospitals. Fifteen patients were studied. They all had stable asthma treated with theophylline and no major organ failure or gastro-intestinal lesions requiring the use of antacids. The antacid (aluminium hydroxide 800 mg and magnesium hydroxide 800 mg), or placebo, tid, was added to a stable regimen of theophylline SR bid, for 4 days, in crossover fashion. Plasma theophylline concentrations were measured before and 1, 2, 3, 4, 6, 8, 10, 12, 16 and 24 h after the morning dose of Armophylline on the fourth day of each treatment period; the maximum plasma concentration (Cmax), and time to Cmax (tmax) were noted, and the area under the 24-h time-concentration curve (AUC0-24) and mean plasma concentration (Cmean) were computed. Peak expiratory flows on the same day, before and 3, 6 and 12 h after the morning dose of Armophylline were also measured. There was no change in any of the parameters studied. The addition of the antacid to theophylline, each given according to standard clinical practice, did not modify the pharmacokinetics of the latter.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed2006

pH-independent drug release of an extremely poorly soluble weakly acidic drug from multiparticulate extended release formulations.

Extended release mini matrix tablets for 8-Prenylnaringenin (8-PN), an extremely poorly soluble weakly acidic drug, were developed by using polyvinylacetate/polyvinylpyrrolidone as matrix former. Mini matrix tablets were manufactured by direct compression or wet granulation technique. With conventional modified release formulations, the drug demonstrated pH-dependent release due to pH-dependent solubility of the drug substance (i.e., increasing solubility at higher pH-values). In order to achieve pH-independent drug release two classes of pH-modifying agents (water-soluble vs. water-insoluble) were studied with respect to their effect on the dissolution of 8-PN. Addition of water-soluble salts of weak acids (sodium carbonate and sodium citrate) failed in order to achieve pH-independent 8-PN release. In contrast, addition of water insoluble salts of a strong base (magnesium hydroxide and magnesium oxide) was found to maintain high pH-values within the mini matrix tablets during release of 8-PN at pH 1 over a period of 10 h. The micro-environmental conditions for the dissolution of the weakly acidic drug were kept almost constant, thus resulting in pH-independent drug release. Compound release from mini matrix tablets prepared by wet granulation was faster compared to the drug release from tablets prepared by direct compression.

Calcium Phosphates↗
PubMed1990

Assessment of antacid characteristics of drugs containing a combination of aluminium and magnesium salts using the "artificial stomach" model.

Antacid characteristics of three drugs containing aluminium and magnesium salts (combination of clay with aluminium and magnesium hydroxides, aluminium and magnesium hydroxide mixture and hydrotalcite) have been studied in a dynamic situation simulated by the "artificial stomach" model, simultaneously taking into account both gastric fluxes, a constant secretory flux and variable emptying fluxes. Therapeutic doses of the drugs were added 1. to 100 ml of 0.1 N HCl, without or with 1% or 5% meat extract, and 2. 100 ml of pooled human gastric juice (96 mmol/l, pH 1.1). In addition, antacid activity of 0.5 g aluminium and magnesium hydroxides, taken alone or in combination, were evaluated when added to 100 ml of 0.1 N HCl. In aqueous HCl solution or in human gastric juice, the three antacid drugs exhibited 1. a neutralising activity characterised by pH-rise and 2. a buffering capacity close to pH 3.8. In addition, hydrotalcite exhibited also buffering capacity at pH 1.2. The antacid-induced capacity, expressed as H+ mmol, to recover initial pH were very similar, indicating that antacid physiochemical properties are similar in HCl solution or in gastric juice. H+ consumption depended upon emptying fluxes. The same antacid characteristics were observed when antacids were mixed with 1% meat extract while 5% meat extract resulted in a modification of antacid characteristics. Therefore the antacid capacities of respective mixtures were of smaller magnitude (50-60%) than the sum of the activities of antacids plus meat extracts.(ABSTRACT TRUNCATED AT 250 WORDS)

Aluminum Hydroxide↗
PubMed1991

Investigation of the possible influence of the absorption of vinpocetine with concomitant application of magnesium-aluminium-hydroxide gel.

The concomitant application of magnesium-aluminium-hydroxide gel does not influence the absorption of vinpocetine (CAS 42971-09-5). The pharmacokinetics of vinpocetine under the influence of a concomitant application of magnesium-aluminium-hydroxide gel was investigated. 18 healthy male volunteers were included in the study. Vinpocetine was administered in the galenic form of a film-coated tablet in a dosage of 20 mg t.i.d. over 10 days. On days 5 and 6 of the study, blood samples were taken at 16 different moments over 24 h and analyzed as to their vinpocetine content. Starting with the 6th day of the study, the patients were administered in addition 1 sachet of an magnesium-aluminium-hydroxide gel 4 times a day. On day 9 of the trial, blood samples were taken again over 24 h. The parameters examined were AUC, Cmin, Cmax, tmax and Mean Residence Time. The results as to these parameters of day 5 were compared with those of day 9. As a further parameter, apovincaminic acid plasma levels were determined. There was no difference as to the vinpocetine amount absorbed with or without concomitant application of magnesium-aluminium-hydroxide gel. Apovincaminic acid plasma levels were lowered by approx. 11% when associated with the antacid.

Adult↗
PubMed1981

Effect of antacids on the bioavailability of diflunisal in the fasting and postprandial states.

Diflunisal is long-acting salicylate derivative. We examined the effect of single concomitant doses of three antacids on diflunisal bioavailability under fasting or fed conditions (30 min after finishing a standard meal). With the use of an open, randomized, and balanced design, one 250-mg diflunisal tablet was given to each of 12 healthy men under six conditions: fasted, no antacid; fed, no antacid; fasted, 15 ml of aluminum hydroxide gel; fed, 15 ml of aluminum hydroxide gel; fasted, 10 ml magnesium hydroxide suspension; and fed, 15 ml of an aluminum hydroxide/magnesium hydroxide mixture. Diflunisal plasma 0- to 48-hr area uiven to each of 12 healthy men under six conditions: fasted, no antacid; fed, no antacid; fasted, 15 ml of aluminum hydroxide gel; fed, 15 ml of aluminum hydroxide gel; fasted, 10 ml magnesium hydroxide suspension; and fed, 15 ml of an aluminum hydroxide/magnesium hydroxide mixture. Diflunisal plasma 0- to 48-hr area uiven to each of 12 healthy men under six conditions: fasted, no antacid; fed, no antacid; fasted, 15 ml of aluminum hydroxide gel; fed, 15 ml of aluminum hydroxide gel; fasted, 10 ml magnesium hydroxide suspension; and fed, 15 ml of an aluminum hydroxide/magnesium hydroxide mixture. Diflunisal plasma 0- to 48-hr area under the time curve (AUC), peak plasma concentrations, and 0-to 96-hr urinary excretion were determined. Food (alone) decreased peak plasma concentrations by 16% (P less than 0.05) but did not affect AUC or urinary excretion. Under fasting conditions, aluminum hydroxide reduced AUC by 26% (P less than 0.01), peak plasma concentrations by 46% (P less than 0.01), and urinary excretion by 14% (P less than 0.05). Magenisuum hydroxide suspension (in the fasting state) increased the early plasma concentrations (by 130% at 0.5 hr and 64% at 1 hr, P less than 0.05) and increased AUC by 10% (P less than 0.05) but had no effect on urinary excretion. In the fed state neither aluminum hydroxide nor the aluminum hydroxide/magnesium hydroxide mixture had any detectable effect.

Adult↗
PubMed1978

The effect of oral local anaesthetic and alkali on basal and food-stimulated serum gastrin levels in patients with duodenal ulcer.

Twelve patients with duodenal ulcers were each given on separate days and in random order an oral local anaesthetic (oxethazaine), an alkali (aluminium hydroxide and magnesium hydroxide), a combination of local anaesthetic and alkali (Mucaine), and a similar volume of water (control) followed one hour later by a solution of meat extract (Oxo). The effect of these treatments on serum gastrin levels was measured. None of the treatments altered the normal basal gastrin levels. The gastrin response to ingestion of protein extract was significantly lower in patients who had been pre-treated with local anaesthetic than those who had received alkali, with or without local anaesthetic, or water.

Administration, Oral↗
PubMed1988

Bile salt binding properties of commonly used gastrointestinal drugs: maalox, carafate, and questran.

We have validated a method to measure bile salt binding by Maalox (aluminum hydroxide and magnesium hydroxide), Carafate (sucralfate), and Questran (cholestyramine) in vitro. The method used in this study involves a correction for adherent water volume and thus provides a correct measure of bile salt binding. With this approach, we described the binding properties of Maalox, Carafate, and Questran. The bile salt binding capacities of Carafate and Maalox are limited and do not have physiological or pharmacological significance. On the other hand, we found that Questran has substantial bile salt binding capacity. At the recommended dosage, Questran could deplete the total bile salt pool. We also found that Carafate, although not used as an antacid, has buffering capacity (maintaining a pH of solution in the range 4.2-4.8) which might contribute to its effectiveness as an ulcer treatment drug.

Aluminum Hydroxide↗
PubMed1992

The effect of antacid on aspirin pharmacokinetics in healthy Thai volunteers.

The effect of antacid on aspirin pharmacokinetics and bioavailability was determined in 10 healthy adult male and female volunteers, aged 20-45 years old. Each subject received 650 mg of aspirin orally after an overnight fast. The wash out period was 14 days and then all subjects were given 650 mg of aspirin 10 minutes after antacid (aluminium hydroxide and magnesium hydroxide). Plasma aspirin, salicylate and salicyluric acid levels were determined by a specific high performance liquid chromatographic analysis. Individual plasma profiles were analysed using compartmental and non-compartmental methods. The results show that antacid affected the relative bioavailability of aspirin since the mean peak concentration (Cmax) of aspirin was significantly higher when antacid was given. However, the time to reach peak concentration (Tmax) and the area under the plasma concentration-time curve (AUC) showed no significant difference between the two treatments. It was, therefore, not possible to conclude that the non-bioequivalence was caused by a difference in rate or amount of aspirin absorption, or both. No significant difference was observed in Cmax, Tmax, AUC, t1/2, Ka, Kel of salicylate and salicyluric acid. However, the rate of total salicylate absorption was increased since the absorption rate constant (Ka) was higher when antacid was given. This may provide a more rapid effect of the drug.

Adult↗
PubMed1985

[Histo-autoradiographic study of the secretion of gastric mucus in the rat stomach. II. Role of feeding and its combination with an antacid].

The authors use the technique of histoautoradiography after injection of glucose 3H to study the production and excretion of acid mucus in the fundus mucosa of the rat stomach. They demonstrate the effect of fasting, of eating and of eating combined with a topical agent consisting of 3 active principles: beidellitic montmorillonite, aluminum hydroxide and magnesium hydroxide. Eating stimulates the excretion of mucus during the digestive phase. Gelox combined with food allows for the late creation (6 to 12 hours after the meal) of an abundant layer of protective mucus. This topical action on the secretion of acid mucus favourises the physiological protection of the gastric mucosa.

Aluminum Hydroxide↗
PubMed1980

The effect of antacids on the occurrence of bile acid and aspirin-induced gastric lesions in rats.

Taurodeoxycholic acid increases the incidence of aspirin induced gastric bleeding in rats and in vitro is well bound by Aludrox (aluminium hydroxide) and poorly bound by Maalox (aluminium hydroxide and magnesium hydroxide). We studied the relevance of this binding, as demonstrated in vitro, by observing the effect of the antacids on the occurrence of taurodeoxycholic acid and aspirin-induced bleeding in vivo in rats. Six groups of fasting male Sprague-Dawley rats (n = 24) were intubated and given either water, Aludrox or Maalox and, 30 min later, aspirin or aspirin plus taurodeoxycholic acid. 4 h later the stomachs were examined and rats were scored positive if a lesion greater than 1 mm across was found (incidence of bleeding); a lesion scoring system was also used (severity of bleeding). The incidence of bleeding was increased from 63% with aspirin to 92% with aspirin plus taurodeoxycholic acid (P less than 0.05). The incidence was reduced to 33% and 67% respectively by Aludrox and to 29% (P less than 0.05) and 71% by Maalox. The severity of bleeding (median lesion score, quartiles in parentheses) was increased from 3 (1;6.5) (aspirin) to 10.5 (6;15) (aspirin plus taurodeoxycholic acid); P less than 0.001. These were reduced to 0.5 (0;3); P less than 0.02 and 5 (0.5;9.5); P less than 0.05 respectively by Aludrox and to 0 (0;3); P less than 0.02 and 3 (2;8); P less than 0.02 by Maalox. The severity of bleeding was reduced by both antacids but the effect appeared to be mainly on the aspirin rather than the bile acid component of the damage.

Aluminum Hydroxide↗