Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1984-07-20
1986-01-21
Phillips, Delbert R.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
2601125R, A61K 3700, C07C10352
Patent
active
045658056
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to the art of pharmacology and, more specifically, to a novel pharmaceutical preparation for the treatment of peptic ulcer.
BACKGROUND OF THE INVENTION
It is known in the art that various preparations can be employed in gastroenterology for the treatment of peptic ulcer such as anticholinergic agents--atropine, glycopyrolate, antacids--aluminium hydroxide, calcium carbonate and the like (cf. Cristensen et al., Gastroenterology. 1977, v. 73, pp. 1170-1178).
The antiulcerous effect of anticholinergic preparations and antacids is based on their ability of lowering acidity of the gastric juice, wherefore these preparations are administered in high doses. The use of such doses of the preparations is accompanied by the development of numerous side effects.
At present cymethidin is considered to be the most effective preparation for the treatment of peptic ulcer; its effect is based on blocking H.sub.2 -receptors of histamine (cf. Brimblecombe et al., Gastroenterology, 1978, v. 74, pp. 339-347). As the same time cymethidin gives a number of side effects: it causes endocrinous changes; being an antiandrogen, it affects metabolism of pharmaceutical preparations in liver.
Described in the literature is a peptide having the following structure: Tyr-D-Ala-Gly-Phe-Leu-Arg (Chavkin, Goldstein, Proc. Natl. Acad. Sci. USA. 1981, v. 78, pp. 6543-6547). However, its possible applications have not been specified.
DISCLOSURE OF THE INVENTION
The pharmaceutical preparation according to the present invention is novel and hitherto unknown from the literature.
The present invention is directed to the utilization of a novel pharmaceutical preparation for the treatment of peptic ulcer which provides an accelerating effect on processes of ulcer healing, has a low toxicity, a broad spectrum of therapeutic action and causes no side effects.
This object is accomplished by the use of a pharmaceutical preparation for the treatment of peptic ulcer comprising an active ingredient and a pharmaceutically acceptable vehicle which contains, as the active ingredient, a peptide of the following structure:
The preparation according to the present invention can be administered in diverse pharmaceutical forms (injections, solutions, tablets and the like). It is preferable to use the preparation according to the present invention in the form of injectable solutions with a content of the active principle of 0.1-0.5% by weight. As the pharmaceutically acceptable vehicle the preparation preferably contains bidistilled water or a 0.9% aqueous solution of sodium chloride.
The preparation according to the present invention in the form of tablets preferably contains the active ingredient in an amount of 10 to 50 mg per tablet. As the pharmaceutically acceptable vehicle for tablets it preferably contains starch, glucose or lactose.
The preparation of this invention provides an accelerating effect on processes of healing of peptic ulcer of the duodenum and stomach. Physiological effects of the preparation according to the present invention are revealed in acceleration of scarring at the site of ulcer.
The preparation is characterized by a low toxicity, a small single dose, and an effective therapeutic action. The preparation is adapted for the treatment of peptic ulcer.
BEST MODE OF CARRYING OUT THE INVENTION
The preparation for the treatment of peptic ulcer according to the present invention was experimentally tested on animals and clinically on humans.
The effectiveness of the preparation was studied on an experimental model of a cystamine duodenal ulcer in rats and on a model of gastric ulcers in rats caused by immobilization for 24 hours.
Duodenal ulcers were induced by means of a subcutaneous administration of cystamine hydrochloride in a single dose of 350 mg/kg.
The preparation according to the present invention was also subcutaneously administered twice a day in a physiological solution. In the experiments 350 male rats of the V-starline of a 150-200 g mass were used. The animals were sla
REFERENCES:
Chankin et al., Proc. Natl. Acad. Sci., USA, 78, No. 10, 6543-6547 (1981).
Azmuko Andrei A.
Bespalova Zhanna D.
Bulgakov Sergei A.
Ivanov Vladimir N.
Medvedev Oleg S.
Moezie F. T.
Phillips Delbert R.
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