Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Food or edible as carrier for pharmaceutical
Patent
1989-12-05
1991-11-26
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Food or edible as carrier for pharmaceutical
514819, 514820, A61K 928
Patent
active
050681095
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL BACKGROUND
Upper abdominal dyspepsia is symptomatic of a variety of diseases such as ulcers, biliary conditions, pancreatitis and gastrooesophageal reflux. However, the symptoms (heartburn, regurgitation and epigastric pain) often associated with such conditions may also occur without apparently being attributable to any specific clinical conditions observed by X-ray or endoscopic analyses.
Thus, the symptoms are very common, at least once in a while, even among otherwise healthy individuals. It is estimated that about 50-60% of the adult population in the United States suffer from one form or another of acute upper gastrointestinal distress. The short-term or prolonged use of antacids is therefore widespread.
The antacid effect of most of the antacid compositions currently in use resides in their ability to neutralize gastric acids, resulting in an increased pH of the gastric contents. The acid neutralizing effect of such conventional antacids is known to be brief in vivo, which is ascribable to two principal causes: the normal gastric emptying rate which causes the composition to be transferred to the intestines before its acid neutralizing and buffering capacities have been exhausted, and "acid rebound" or increased acid secretion induced by increased release of gastrin from the so-called G cells of the antrum which are pH sensitive, the increased production of gastrin occurring at a pH of the gastric contents of about 4-5 or more. For these reasons, the acidity of the gastric contents will usually have reached its normal level 1-2 hours after ingestion of the antacid so that a dosage regimen involving the ingestion of repeated antacid dosages may be required, in particular for the long-term treatment of gastric conditions such as ulcers, rather than for short-term relief of dyspepsia.
The currently employed antacids usually contain one or more alkali metal or alkaline earth metal salts, aluminum salts or, less usually, bismuth salts as acid neutralizing agents. The most commonly employed mineral salts are sodium bicarbonate, calcium carbonate, aluminum salts or magnesium salts.
Sodium bicarbonate is known as a potent, effective and rapid-acting antacid which, however, only exhibits a short-term effect. It is a systemic antacid which is not recommended for prolonged use or in large doses as systemic absorption of the sodium ion in large quantities may cause alkalosis which is characterized by elevated levels of carbon dioxide and an increased pH in the plasma. Symptoms of alkalosis include headache, mental confusion and anorexia.
Calcium carbonate which is a non-systemic gastric antacid is known to cause rapid, prolonged and effective neutralization of gastric acid, but is not recommended as an antacid, primarily because of its "acid rebound" effect. Studies have shown that oral administration of an isotonic calcium chloride solution results in increased gastric acid secretion both in healthy individuals and, particularly, in ulcer patients (50-75%). In another study, free calcium in the stomach has been found to release gastrin which in turn, as described above, induces the formation of gastric acid. Apart from acid rebound, it may cause hypercalcaemia and constipation.
The most commonly employed aluminum salts are the hydroxide, carbonate or phosphate, primarily the hydroxide. Its acid neutralizing capacity is lower than that of other conventional antacids, and it may cause constipation. Aluminum salts are therefore often combined with magnesium salts, such as the oxide, hydroxide, carbonate and trisilicate, which have a higher acid neutralizing capacity than the aluminum salts, but which may also cause diarrhoea. In combination preparations, the two components are balanced to offset the effect of either on gastrointestinal functions. A combination of aluminum and magnesium hydroxide gels is present in many commercial antacids. Recently, aluminum has become suspected of contributing to the development of presenile dementia (Alzheimer's disease) for which reason its use as an antacid should
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Foldager Jorgen
Kjornos Kim
Toftkjor Helle
Farma Food A/S
Page Thurman K.
Phelan D. Gabrielle
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