Magnesium aluminum hydroxide gel in the antacid therapy of peptic ulcer.
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Aluminum Hydroxide↗
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Effect of an aluminium-hydroxide containing antacid on the oral bioavailability of pirenzepine.
The effect of an antacid containing aluminium-hydroxide, magnesium-hydroxide and calcium carbonate (Trigastril) on the bioavailability of orally administered pirenzepine (Gastricur) was evaluated in 10 subjects in a double-blind single dose cross-over study. Pirenzepine was assayed in plasma by a highly sensitive high-performance liquid chromatographic method. A 2-compartment model was taken as a basis for the calculation of the plasma concentration curves and the pharmacokinetic parameters. The oral bioavailability of a 50 mg pirenzepine tablet concomitantly administered with 10 ml of the antacid gel preparation was slightly but not significantly greater than that of pirenzepine in the presence of a placebo gel. This was reflected by a mean increase of 18-28% in area under the curve (AUC 0-32, AUC 0-infinity, resp.) and of 26% in Cmax-values. There was no significant difference in the biological half-life of pirenzepine between the two treatments (10.1-9.4 h).
Administration, Oral↗
The pharmacokinetics and tissue penetration of the fluoroquinolones.
There are marked differences among the pharmacokinetic properties of the quinolones. Absorption of norfloxacin, ciprofloxacin, and enoxacin is incomplete, whereas the bioavailability of pefloxacin, ofloxacin and fleroxacin is almost 100%. With the exception of norfloxacin the quinolones can be taken orally or administered by the parenteral route. Maximum serum concentrations vary between 1.5 and 10.7 micrograms/ml depending on the dose and antibiotic given. Respective AUC's of 78 and 5.5 micrograms/ml-h are observed following the administration of 400 mg of either fleroxacin or norfloxacin. Protein binding is low (less than or equal to 30%) and apparent volume of distribution is between 1.5 and 3.1 liters/kg. Pefloxacin undergoes extensive metabolism in the liver (85%) while less than 5% of ofloxacin is transformed. Norfloxacin and ciprofloxacin have the shortest half-lives (+/- 4h), while fleroxacin and pefloxacin have the longest (10-12h). In renal failure, no adjustments are necessary with pefloxacin, while major modifications in dosing interval and/or doses are needed when ofloxacin is given. The pharmacokinetics of the quinolones is disturbed in elderly subjects and cystic fibrosis patients. Concurrent administration of antacids which contain aluminum hydroxide or magnesium hydroxide leads to reduced absorption, while probenecid blocks the tubular secretion of some quinolones. These drugs diffuse rapidly in extravascular fluid, saliva, urine, kidney, prostate, bile and peritoneal fluid. Slightly lower levels can be detected in fibrin clots, cerebrospinal fluid and the heart. Ciprofloxacin offers the best therapeutic ratio (concentration serum-tissue/minimum inhibitory concentration) against Pseudomonas aeruginosa.
4-Quinolones↗
[Treatment of duodenal ulcer with the Bulgarian preparation gastralgin].
The effect of the new Bulgarian preparation gastralgin was studied in 20 patients with duodenal ulcer. The preparation was given three times daily in the course of 20 days--I bag, 1/2 to 1 hour before meals and in the evening before going to bed. Gastralgin contains in one bag--alginic acid 0.500, sodium alginate 0.500, aluminium hydroxide 0.200, magnesium hydroxide 0.100, calcium carbonate 0.500 and corrigent up to 7g. Favourable effect on the separate symptoms was attained in 50 to 80% after the treatment, epithelialization of the ulcer in 40% and reduction of its size in 25%. No change in gastric secretion was observed. Gastralgin, with its therapeutic effect, is equivalent to the preparations almagel and flatugel and their improved variants. The preparation is well tolerated and gives no adverse effects, hence it is recommended for the treatment of duodenal ulcer.
Adult↗
Clinical evaluation of triletide versus antacids in the treatment of duodenal ulcer out-patients.
Thirty out-patients with endoscopically assessed, active duodenal ulcer of mild to moderate intensity were randomly assigned to 8-weeks' treatment with either antacids (0.8 g/day each of aluminium hydroxide and magnesium hydroxide), triletide (1.5 g/day) or a combination of the two treatments. Every other week, the intensity of subjective symptoms and of objective signs was scored and recorded, and the endoscopic outcome assessed at the 8th week. Three patients on antacids alone and 1 on triletide alone were withdrawn at the 4th week because of therapeutic failure. Symptoms and signs improved in the three groups significantly faster, to a significantly greater extent, and in more patients with triletide, alone or in combination, than with antacids. Endoscopic evidence of therapeutic response was detected in significantly more patients given triletide, alone or in combination, in comparison with the group who had antacids. A significant influence on promoting ulcer healing could be attributed to triletide (p less than 0.05, multiple linear regression) and not to antacids. Tolerance was complete in all patients. It is concluded that triletide appears to be equally well tolerated as, but significantly more effective than, antacids in relieving symptoms and promoting healing in patients with mild to moderate duodenal ulcer.
Adult↗
The neutralizing capacity and sodium content of antacid brands on the Kenyan market.
Seventeen brands of antacid products available on the Kenya market were investigated for their acid neutralising capacity and sodium content. Thirteen tablet products gave neutralising capacity per tablet of between 4.7 to 14.12 mMol hydrochloric acid. The neutralising capacities for the suspensions ranged between 11.97 to 34.32 mMol hydrochloric acid for 10ml suspension. The lowest neutralising capacities were obtained for products based on compound magnesium trisilicate and higher capacities for those containing magaldrate, or magnesium hydroxide or magnesium carbonate in combination with other ingredients. The fastest rate of neutralization was obtained with preparations containing carbonates and the lowest by compound magnesium trisilicate. The sodium content for the preparations was between < 0.001 mEq to 0.732 mEq sodium per minimum recommended dose. The study shows a high degree of variation in both the acid neutralising capacities and the sodium content of the different brands investigated.
Antacids↗
[Changes in the transmural electric potential difference in the region of stomach ulcer. Local effect of sucralfate, aluminum hydroxide and magnesium trisilicate].
In three groups of six patients with gastric ulcer, sucralfate, aluminium hydroxide and magnesium trisilicate, respectively was applied to the ulcer under endoscopic vision. Prior to, two and four hours after application of these substances, the transmural electrical potential difference (p.d.) was measured in the region of the bed of the ulcer, the margin of the ulcer, the antrum on the lesser curvature side, and in the pool of juice; additionally, the degree of adherence of the substances to the floor of the ulcer was recorded. After sucralfate, the increase in p.d. in the bed of the ulcer was clearly greater two and four hours post-application than after the two antacids tested, and adherence to the ulcer was also more marked and longer lasting. These findings confirm the superior local protective effect of sucralfate in the bed of the ulcer on the basis of its physico-chemical properties, as compared with the antacids tested. These clinico-experimental findings correlate with the efficacy of sucralfate in ulcer disease as demonstrated in clinical studies.
Action Potentials↗
Magnesium-aluminum hydroxide suspension for the treatment of dermal capsaicin exposures.
OBJECTIVES: To determine whether magnesium-aluminum-hydroxide-simethicone suspension (MgAl) is an effective treatment for dermal capsaicin exposures. METHODS: The authors performed a double-blind, randomized, controlled, pilot study comparing the effect of MgAl with that of saline in the treatment of dermal capsaicin exposures. Ten volunteers were sprayed with a commercial defensive spray containing 10% capsaicin on the flexor surface of both forearms. A dressing embedded with MgAl (Maalox) suspension was randomly applied to one arm and a saline-embedded dressing was applied to the other arm. Pain was assessed on a 10-cm visual analog scale at 0, 10, 20, 30, 60, 90, and 120 minutes. RESULTS: Mean pain scores were significantly lower in the MgAl group as compared with the saline (S) group at 10, 20, and 30 minutes. Differences in pain scores were not statistically significant at times 60, 90, and 120 minutes. CONCLUSIONS: During the initial 30 minutes of treatment, there was a statistically significant decrease in pain scores with MgAl as compared with saline treatments. Although the difference in means may have questionable clinical significance, MgAl is cheap and readily available, and has minimal side effects. Thus, MgAl may be an appropriate treatment for dermal capsaicin exposure.
Administration, Cutaneous↗
Double-blind clinical, endoscopic and histological comparison of hydrotalcite/dimethicone suspension and magnesium hydroxide/aluminum hydroxide suspension in the treatment of symptomatic gastritis.
A double-blind, randomized trial was undertaken to compare the clinical, endoscopic and histological response to 6-weeks' treatment with hydrotalcite/dimethicone suspension or magnesium hydroxide/aluminum hydroxide suspension in 36 patients with symptomatic gastritis. Significantly more patients (P less than 0.05) showed symptomatic improvement in the antacid-treated group than in the hydrotalcite/dimethicone-treated group and more had a reduction in histological inflammatory scores (P less than 0.01), although there was little correlation between histology and symptoms. There was no evidence from this study that the bile acid binding and anti-foaming properties of hydrotalcite/dimethicone suspension were of any benefit in the treatment of patients with symptomatic gastritis.
Adult↗
Influence of antacid administrations on aspirin absorption in patients with chronic renal failure on maintenance hemodialysis.
In order to investigate the possible interaction between oral aspirin and antacids in uremic patients on chronic hemodialysis, we administered to 5 uremic patients: (1) aspirin alone; (2) aluminum-magnesium hydroxide with aspirin; (3) aluminum-magnesium hydroxide followed (two hours) by aspirin; (4) calcium carbonate simultaneously with aspirin; and (5) calcium carbonate followed (two hours) by aspirin. In all the occasions, aspirin was given two hours after a standard lunch. Both antacid preparations induced comparable changes in aspirin mean peak plasma concentration (Cmax), if given simultaneously with aspirin, whereas no difference was found in other pharmacokinetic parameters. When antacids were followed (two hours) by aspirin, both Cmax and time of maximum concentration (Tmax) were significantly altered in respect to the value with aspirin alone. No changes in the time course of post aspirin serum thromboxane B2 were detected when aspirin and antacids were administered simultaneously, but the inhibition of serum thromboxane B2 was delayed when antacids were followed (two hours) by aspirin. These results indicate that the administration of antacids to uremic patients interferes with absorption of oral aspirin. This interference can be minimized if aspirin and antacids are given simultaneously.
Absorption↗
Diagnosis of magnesium-induced diarrhea.
BACKGROUND: There is no specific method of diagnosing magnesium-induced diarrhea. Therefore, the frequency and clinical importance of diarrhea caused by magnesium are unknown. The purposes of this study were to establish a method for diagnosing magnesium-induced diarrhea and to apply it to patients with chronic diarrhea. METHODS: We measured fecal output of soluble magnesium and fecal magnesium concentration in 19 normal subjects with formed stools (15 collection periods), with non-magnesium-induced diarrhea (36 collection periods), and with diarrhea induced by magnesium hydroxide alone (11 collection periods) or in combination with phenolphthalein (3 collection periods), and in 359 patients with chronic diarrhea. RESULTS: The upper limits of fecal output of soluble magnesium and fecal magnesium concentration in normal subjects were 14.6 mmol per day and 45.2 mmol per liter, respectively. When normal subjects had diarrhea due to the ingestion of magnesium hydroxide alone or in combination with phenolphthalein, fecal magnesium output was always abnormally high. For each millimole increase in fecal magnesium output, fecal weight increased by approximately 7.3 g. The fecal magnesium concentration was very high when magnesium was the only cause of diarrhea but only moderately elevated when diarrhea was induced by magnesium hydroxide plus phenolphthalein. Biochemical and clinical evidence indicated that excessive ingestion of magnesium was an important cause of chronic diarrhea in 15 of the 359 patients with chronic diarrhea (4.2 percent), if not the only cause. CONCLUSIONS: Quantitative fecal analysis for soluble magnesium is an accurate method of diagnosing magnesium-induced diarrhea. Some patients with chronic diarrhea ingest excessive amounts of magnesium (in antacids or food supplements), and physicians may fail to discover this before embarking on an expensive and invasive diagnostic evaluation.
Adult↗
Effect of antacids on activity of oral hypoglycemics.
The effect of some antacids on the dissolution and hypoglycemic activity of acetohexamide, tolazamide, and tolbutamide tablets was investigated, as was the adsorption of the three drugs onto the antacids. The dissolution rates of the three drugs in the presence of magnesium oxide, aluminum hydroxide, magnesium carbonate, and calcium carbonate increased (0.5-1 hr) and then plateaued or decreased (1-3 hr). Magnesium trisilicate directly suppressed the dissolution of the three drugs. The antacids reduced the hypoglycemic activity of tolbutamide in the following order:magnesium trisilicate greater than magnesium oxide greater than aluminum hydroxide greater than magnesium carbonate greater than calcium carbonate. The same order occurred for the first three antacids with acetohexamide and tolazamide. Decreased hypoglycemic activity of the drugs may have been due to their adsorption to the coadministered antacids.
Adsorption↗
Effect of food and various antacids on the absorption of tenoxicam.
1 Twelve healthy volunteers received a single oral dose of tenoxicam 20 mg on six occasions separated by 3 weeks. 2 The six occasions were: fasted overnight; postprandial; fasting and 15 ml aluminium hydroxide gel; postprandial and 15 ml aluminium hydroxide gel; fasting and 15 ml aluminium and magnesium hydroxide gel; postprandial and 15 ml aluminium and magnesium hydroxide gel. 3 Twenty plasma samples were collected over 15 days following dosing with tenoxicam. 4 The following kinetic parameters for plasma tenoxicam were compared: peak concentrations, time taken to reach peak concentrations, area under the plasma concentration-time curve (AUC) and half-life of elimination. 5 Food lengthened the time taken to reach peak tenoxicam concentrations (5.82 +/- 4.6 vs 1.84 +/- 1.0 h in the fasting state; P less than 0.02) and marginally reduced the peak concentrations achieved. AUC was not affected by any of the different regimens. 6 These effects of food on tenoxicam bioavailability are unlikely to be of clinical significance during chronic dosing with the drug.
Adult↗
The effect of antacid and ranitidine on droxicam pharmacokinetics.
Droxicam is a nonsteroidal anti-inflammatory drug that is a pro-drug of piroxicam. The influence of concomitant administration of antacid or ranitidine on droxicam pharmacokinetics has been investigated. On three separate phases, 15 healthy volunteers received a single oral 20-mg dose of droxicam either alone, with antacid (400 mg aluminum hydroxide + 400 mg magnesium hydroxide, three times/day), or with ranitidine (300 mg, two times/day) for 6 days. Piroxicam, the active substance from droxicam, was quantified by high-performance liquid chromatography. The pharmacokinetic parameters for droxicam given alone were: maximum peak plasma concentration (Cmax) = 1.53 +/- .21 micrograms/mL (mean +/- SD), time to peak concentration (Tmax) = 7.5 +/- 2.1 hr, t1/2a = 1.38 +/- .82 hour, t1/2el = 53.3 +/- 11.9 hr, Cl/F = 2.98 +/- .71 mL/min, volume of distribution (Vd/F) = 13.2 +/- 1.8 L and area under the curve (AUC) = 117.6 +/- 26.8 micrograms/hour/mL. The subject effect was significant for all the pharmacokinetic parameters except for the absorption half-life (P < .05). Concomitant antacid or ranitidine administration had no significant effect on any of the droxicam pharmacokinetic parameters. The results of this study suggest that antacid or ranitidine do not significantly alter the oral absorption or pharmacokinetic disposition of single-dose droxicam.
Administration, Oral↗
Studies on the lead-catalyzed synthesis of aldopentoses.
The object of this work was to find an efficient means of synthesizing ribose in a manner that could be considered prebiotic. The starting point for synthesis was an aqueous solution of formaldehyde. Heretofore the most frequently used catalyst for this purpose has been calcium hydroxide. Unfortunately this system produces a wide array of products in addition to ribose which constitutes 1% or less of the final product. Attempts were made to find more mild conditions under which the formaldehyde could be reacted. Magnesium hydroxide suspensions were used for this purpose. Formaldehyde does not yield any sugars when incubated in magnesium hydroxide suspensions alone. However, if the magnesium hydroxide suspension was supplemented with doubly charged lead salts and catalytic amounts of any intermediate in the prebiotic pentose pathway, aldopentoses accounted for 30 per cent or more of the final product. The presence of lead in the incubation mixture also accelerated a number of other reactions including the interconversion of the four common aldopentoses, ribose, arabinose, lyxose and xylose.
Acetophenones↗
Effect of excipients on PLGA film degradation and the stability of an incorporated peptide.
The effect of pH modifying excipients on the chemical stability of a model peptide (VYPNGA) and the degradation of poly(dl-lactide-co-glycolide)(PLGA) was studied in PLGA films under accelerated storage conditions. pH modifiers included a basic amine (proton sponge), a basic salt (magnesium hydroxide) and two pH buffers (ammonium acetate and magnesium acetate). Changes in film pH were monitored using (13)C NMR, peptide degradation products were quantified by LC/MS/MS and PLGA degradation was analyzed by TGA, DSC and SEC. Inclusion of pH modifiers had little impact on PLGA degradation. The proton sponge affected an initial decrease in pH but reduced peptide deamidation and chain cleavage relative to an unbuffered control. Magnesium hydroxide produced an initial increase in pH but also showed increased peptide deamidation. Ammonium acetate decreased pH and increased peptide chain cleavage, presumably due to increased PLGA hydrolysis. Magnesium acetate buffer increased the initial pH but resulted in increased peptide loss. The extent of peptide acylation increased in all formulations, most notably in the proton sponge modified films. The effectiveness of pH modifiers in PLGA formulations under storage conditions is dependant on both the mechanism of pH alteration and the peptide degradation reaction of interest.
Acylation↗
Effect of composition on the neutralizing properties of antacid preparations.
11 antacid mixtures made up to simulate the preparations available on the market were prepared. These mixtures contain aluminium hydroxide gel, calcium carbonate, magnesium hydroxide and magnesium trisilicate. The antacid properties of the mixtures obtained were characterized by total acid consuming capacity, rate of neutralization and duration of action. It was indicated that the composition of the mixtures influenced their neutralizing properties; an interaction between constituents of these preparations was noted.
Aluminum Hydroxide↗
TREATMENT OF THE CONSTIPATION-GAS SYNDROME IN GERIATRIC PATIENTS: USE OF A MAGNESIUM HYDROXIDE-SIMETHICONE EMULSION.
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Cathartics↗