ABSTRACT
A carbonated hydrocalumite was synthesized by the microwave method for being used as antacid. The gel was formed using Ca and Al nitrate solutions in a basic medium (NaOH+Na2CO3), then, this gel was aged and heated in a domestic microwave for 2.5 min (1250 W). The obtained white solid was washed with distilled water, dried in an oven at 100 °C for 18 h and characterized by different techniques such as: X-ray diffraction (XRD), Fourier transformed infrared spectroscopy (FT-IR), BET surface area measurements, scanning electron microscopy (SEM) and energy dispersive X-ray spectroscopy (EDX). Finally, the carbonated hydrocalumite was tested as antacid by using a synthetic gastric juice and its activity was compared with a commercial antacid formulated with hydrotalcite. Results showed that the carbonated hydrocalumite was more effective than that commercial antacid.
Subject(s)
Antacids/chemical synthesis , Microwaves , Aluminum Compounds/chemistry , Antacids/chemistry , Calcium Compounds/chemistry , Carbonates/chemistry , Gels/chemical synthesis , Gels/chemistry , Microscopy, Electron, Scanning , Nitrates/chemistry , Spectrometry, X-Ray Emission , Spectroscopy, Fourier Transform Infrared , X-Ray DiffractionSubject(s)
Antacids/history , Antacids/adverse effects , Antacids/chemical synthesis , Antacids/chemistry , Antacids/therapeutic use , Histamine H2 Antagonists/therapeutic use , History, 16th Century , History, 17th Century , History, 18th Century , History, 19th Century , History, 20th Century , HumansABSTRACT
A new series of 2-[(2-aminobenzyl, 4-aminobenzyl, and alpha-methylbenzyl) sulfinyl]-N-(4-pyridinyl)-3-pyridinecarboxamides. was synthesized and evaluated for gastric antisecretory activities. Several of the compounds synthesized exhibited potent inhibitory activities against [14C]aminopyrine accumulation stimulated by dibutyryl cyclic AMP in isolated rabbit parietal cells and histamine-induced gastric acid secretion in pylorus-ligated rats by intraduodenal administration. In particular, the more polar diastereoisomer of 2-[(4-methoxy-alpha-methylbenzyl)sulfinyl] -N-(4-pyridinyl)-3-pyridinecarboxamide (13b) showed in vivo inhibitory activity equivalent or superior to that of omeprazole and was a more selective (H+/K+)-ATPase inhibitor than omeprazole.
Subject(s)
Antacids/chemical synthesis , Antacids/pharmacology , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/pharmacology , Gastric Mucosa/drug effects , Gastric Mucosa/metabolism , Niacinamide/analogs & derivatives , Proton Pump Inhibitors , Animals , Gastric Acid/metabolism , Male , Niacinamide/chemical synthesis , Niacinamide/pharmacology , Parietal Cells, Gastric/drug effects , Parietal Cells, Gastric/metabolism , Pyridines/chemical synthesis , Pyridines/pharmacology , Rabbits , Rats , Rats, Wistar , Secretory Rate/drug effects , Structure-Activity RelationshipABSTRACT
In order to study structure-activity relationships of dual histamine H2 and gastrin receptor antagonists as well as to improve their low oral absorbability, their prototype benzodiazepine gastrin receptor antagonistic moieties were altered to a conformationally flexible noncyclic dipeptide equivalent. This skeletal modification significantly potentiated the binding affinity of hybrid compounds for the histamine H2 receptor, whereas their affinity for the gastrin receptor and receptor selectivity over the CCK-A receptor varied widely with the substituents on the gastrin moiety. Among them, [3-[3-(3-piperidin-1-ylmethylphenoxy)propylcarbamoyl]p ropyl carbamic acid 3-[3-([(3-methoxyphenyl)[(methylphenylcarbamyl)methyl]carbamoyl]me thyl)ureido]benzyl ester (7a) showed the highest dual histamine H2 and gastrin receptor antagonistic activities. It also displayed distinct gastric acid antisecretory activity in vivo for two assays, namely, Schild's rat method by i.d. administration and the rat pylorus ligation method by oral administration. With the latter case, dose-response relationships were observed for the first time, suggesting its substantially improved oral absorbability. However, 7a did not display distinct in vivo gastric acid antisecretory activity for the assay with Heidenhain pouch dogs.
Subject(s)
Benzodiazepines/chemical synthesis , Benzodiazepines/pharmacology , Histamine H2 Antagonists/chemical synthesis , Histamine H2 Antagonists/pharmacology , Receptors, Cholecystokinin/antagonists & inhibitors , Absorption , Administration, Oral , Animals , Antacids/chemical synthesis , Antacids/pharmacokinetics , Antacids/pharmacology , Benzodiazepines/pharmacokinetics , Dogs , Gastric Acid/metabolism , Gastric Mucosa/drug effects , Gastric Mucosa/metabolism , Guinea Pigs , Histamine H2 Antagonists/pharmacokinetics , Molecular Conformation , Rats , Receptor, Cholecystokinin A , Receptors, Cholecystokinin/metabolism , Structure-Activity RelationshipABSTRACT
Aluminium phosphate was precipitated from AlCl3-H3PO4 and NaOH, NH3H2O and NaHCO3--Na2CO3 mixture up to different pH values. The precipitates were dried at room temperature, 40 degrees and 105 degrees and their neutralizing properties (rate of neutralization and acid-consuming capacity) against 0.l N HCl were investigated. It was found that these properties depend on the nature of the reagents used for the formation of AlPO4, the pH and also the temperature of drying. The best antacid properties shows the AlPO4 preperation obtained from AlCl3-H3PO4 and NaHCO3-Na2CO3. For comparison, the therapeutic preparate "Aluphos" was also investigated.
