Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-06-15
1997-08-12
Geist, Gary
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
424605, 424653, 424683, 424684, 424686, 424687, 424690, 424692, 514370, 514471, 514544, 514547, 514549, A61K 31415
Patent
active
056566522
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/GB92/02347, filed Dec. 17, 1992.
This invention relates to the treatment of gastric disorders and pharmaceutical compositions for use therein. More particularly the invention relates to the local treatment of gastric disorders, especially acute gastric disorders such as acid indigestion, heartburn and gastritis, and gastric and peptic ulcer, using orally administrable pharmaceutical compositions comprising a histamine H.sub.2 -receptor antagonist contained within a drug delivery system. Compositions for use in the invention are specifically adapted to provide local delivery across the stomach wall to the H.sub.2 -receptor on the parietal cell receptor.
Histamine H.sub.2 -receptor antagonists, for example cimetidine, ranitidine, nizetidine and famotidine, reduce acid secretion by acting directly on the acid-secreting parietal cell located within the gastric gland of the stomach wall.
Although histamine H.sub.2 -receptor antagonists are remarkably effective in the treatment of many gastric disorders, in particular peptic and gastric ulcers, there exist certain patient groups which do not respond to treatment. In addition, the time lapse between dosing and onset of action, limits the potential benefit of histamine H.sub.2 -receptor antagonists in the treatment of acute, self-limiting gastric disorders.
Histamine H.sub.2 -receptor antagonists are of potential benefit in the self-medication of acute, self-limiting gastric disorders such as hyperacidity. However, their slow onset of action is unlikely to meet the consumer requirement for rapid relief of symptoms.
Moreover, it will be appreciated that use of high dose levels in an attempt to achieve rapid relief of symptoms is not appropriate for non-prescription use. Indeed, a reduction from the standard therapeutic dose would be desirable for self-medication.
Co-administration of histamine H.sub.2 -receptor antagonists and other pharmaceutically active materials, including antacids, has been investigated. The rationale for co-administration with antacid is that the antacid brings about rapid relief from the symptoms of excess stomach acidity by neutralisation whereas the histamine H.sub.2 -receptor antagonist acts independently by inhibiting secretion of acid from the parietal cell.
However, it is well known (Bodemar G. et al., Lancet, 1, 444-445, 1979; Mihaly G. W. et al., B. M. J., 285, 998-9, 1982; Lin. J. H. et al., B. J. Clin. Pharmacol. 24, 551-3, 1987) that when histamine H.sub.2 -receptor antagonists are co-administered with antacids, especially antacids with high acid-neutralising capacity, a substantial reduction in the plasma bioavailability of the histamine H.sub.2 -receptor antagonist is frequently observed. Histamine H.sub.2 -receptor antagonist--antacid combinations are therefore generally contraindicated.
EP-A-0 193 400 (Reckitt and Colman) described pharmaceutical compositions comprising mixtures of a histamine H.sub.2 -receptor antagonist and sodium polyacrylate in the weight ratio 10:1 to 1:10. The compositions are described for use in the treatment of gastritis or gastroduodenal ulcers. The compositions may include an antacid. Use of antacid is described as resulting in a reduction in the viscosity of the liquid compositions, thereby providing some degree of viscosity control in the design of readily pourable liquid preparations.
According to EP-A-0 193 400, the synergistic effect between the histamine H.sub.2 -receptor antagonist and polyacrylate affords the possibility of lower doses of the histamine H.sub.2 -receptor antagonist being used with a resultant reduction in side-effects. EP-A-0 193 400 discloses a normal unit dosage of histamine H.sub.2 -receptor antagonist in the range 800 to 10 mg in the case of cimetidine and in the range 150 to 5 mg in the case of ranitidine.
Current treatments using histamine H.sub.2 -receptor antagonists act systemically, i.e. the histamine H.sub.2 -receptor antagonist is delivered to the parietal cell receptor from the blood.
International Patent Publication No. WO 92/001
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Frazier Barbara S.
Geist Gary
King William T.
Lentz Edward T.
SmithKline Beecham Plc
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