ABSTRACT
Sucralfate, a basic aluminum salt of sucrose sulfate, has been shown to accelerate the healing of peptic ulcers. We studied its binding to normal and ulcerated rat mucosa after gastric and duodenal ulcers had been induced by acetic acid. Sucralfate adhered to ulcerated mucosa for over 6 hours, in the presence and absence of antacid. Food, eaten 1 hour after sucralfate administration, did not appear to alter its selective binding to ulcer sites, but did reduce the amount of sucralfate bound to healthy tissue. The results suggest that sucralfate has a greater affinity for ulcerated mucosa than normal mucosa.
Subject(s)
Aluminum/pharmacology , Antacids/pharmacology , Anti-Ulcer Agents/pharmacology , Duodenal Ulcer/drug therapy , Food , Stomach Ulcer/drug therapy , Animals , Gastric Mucosa/drug effects , Intestinal Mucosa/drug effects , Male , Rats , Rats, Inbred Strains , SucralfateABSTRACT
A magnesium chelate of dicumarol was prepared by reacting a suspension of dicumarol and magnesium oxide in 50% water-methanol. GLC, thermogravimetric, and elemental analyses showed that this compound has a 2:1 ligand-metal stoichiometry with 2 moles of water associated with the complex. Although the chelate does not melt, two endothermic peaks at 205 and 274 degrees were observed in the thermogram, in contrast to a single endothermic peak corresponding to a melting point of 288 degrees for dicumarol. IR spectroscopy indicated that the magnesium is bonded between the carbonyl at C-2 and the oxygen at C-4' (or vice versa).
Subject(s)
Dicumarol/chemical synthesis , Magnesium , Carbon/analysis , Chemical Phenomena , Chemistry , Chromatography, Gas , Densitometry , Differential Thermal Analysis , Hydrogen/analysis , Magnetic Resonance Spectroscopy , Spectrophotometry, Atomic , Spectrophotometry, InfraredSubject(s)
Pharmaceutical Preparations/administration & dosage , Animals , Biological Availability , Chemistry, Pharmaceutical , Dialysis , Drug Stability , Humans , Intestinal Absorption , Kinetics , Mathematics , Models, Chemical , Pharmaceutical Preparations/metabolism , Salts/adverse effects , Salts/chemical synthesis , Salts/pharmacology , Solubility , Structure-Activity Relationship , TasteABSTRACT
A high-speed liquid chromatographic method for analysis of sulfasalazine (salicylazosulfapyridine) in bulk powder and tablet dosage form is presented. Analysis is accomplished with a reverse-phase partition column and 10% 2-propanol in pH 7.7 phosphate buffer as the mobile phase. The method of analysis utilizes a simple, one-step, solubilization procedure with dimethylformamide, addition of an internal standard, and chromatography. The method is specific for sulfasalazine in the presence of starting materials, degradation products, or by-products from its manufacture.
Subject(s)
Sulfasalazine/analysis , Chromatography, High Pressure Liquid , Drug Contamination , Methods , Powders/analysis , Tablets/analysisABSTRACT
A sensitive analysis of pentaerythritol in plasma has been devised, based on the formation of its tetra-p-methoxybenzoate derivative and high-performance liquid chromatography employing an ultraviolet photometric detector. The method permits analysis of pentaerythritol in the ppm range.
