Pharmaceutical composition having antiacoholic activity

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...

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514810, 514811, A61K 3119

Patent

active

055591523

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/RU92/00134 filed Jul. 6, 1992.


FIELD OF THE INVENTION

The present invention relates to medicine, in particular to a new drug having antialcoholic activity, stimulating energy metabolism and acid-forming and secretory functions of stomach mucosa, having radioprotective and anticholera activities.


BACKGROUND OF THE INVENTION

Known is alco-zelzer which is a widely used antialcoholic drug containing citric acid and having antitoxic activity; said drug is administered during the periods of acute alcoholic intoxication. Nevertheless alco-zelzer may be administered only occasionally to treat alcohol intoxication at home. Long-term chronic application of alco-zelzer to provide regular detoxication of alcohol addicted patients causes serious complications due to the presence of aspirin; such complications include dyspepsia, pathogenic changes in stomach mucosa, disfunctioning of nervous system and hemocoagulation. Besides alco-zelzer fails to reduce alcohol dependence and shows no alcoprotective activity, i.e. said drug cannot be used to prevent alcohol intoxication.
Known is an antialcoholic composition based on biological materials comprising citric and succinic acids as well as more than 80 different natural components (GB 2 198 041, DE 3 641 495). Said composition used as an additive for alcoholic drinks and beverages has antitoxic activity and reduces alcohol dependence, nevertheless it shows no alcoprotective effect, its manufacturing is expensive and has limited sources of raw materials, moreover standard norms can hardly be set for such a composition.
Alcoholism is known to be accompanied by worsened appetite which is one of the main symptoms of the disease appearing as a result of lessened acid-forming and secretory function of stomach mucosa, as well as by asthenia.
Known is a method for stimulating energy metabolism and hydrochloric acid secretion by stomach mucosa by using succinic acid ("Terepevticheskoje dejstvie jantarnof kisloty") (Therapeutic Effect of Succinic Acid), the USSR Academy of Sciences, collected articles, 1976, Puschino, pp. 49-55; pp. 106-107). Nevertheless said effects are unstable and accompanied by lessened functional activity.
The diagnostics of acid-forming and secretory function of stomach widely employs such drugs as histamine and pentahistamine. The use of histamine is nevertheless limited due to frequent complications such as nettle-rash, larynx edema, anaphylactic shock. Pentahistamine administration causes sialorrhea, nausea, stomach pains, hypotensia, followed by lessening of acid-forming and secretory function of stomach, as well as worsened appetite.
Presently different antibiotics and vaccines are used to prevent cholera. But antibiotics are toxic, have low-effectiveness and their administration fails to limit the spreading of cholera. The administration of vaccines often causes allergic and toxic complications, the use of said vaccines is limited due to a relatively long period of formation of specific immunity as well as due to a relatively short period of effective protection. Therefore when an endemic center of cholera emerges these vaccines appear to give an unsatisfactory effect.
Known is a wide range of radioprotectors represented by compounds of different classes. But said compounds are toxic and have to be used in high dosages. In recent years much effect has been taken to find radioprotectors among natural metabolites. In particular, radioactive effect of succinic acid has been discovered, but the dosages needed to attain such effect are very high ("International Journal of Radiation Biology", 1987, No. 4, v. 51, Taylor & Francis, Great Britain, pp. 611-617; "Radiobiologia", 1990, No. 5, V. 30, Nauka Publishers, Moscow, pp. 704-706).
It should be noted that the present state of the art does not know absolutely safe drugs (badly needed in acute stages of alcoholism) which could show both alcohol-detoxifying and alcoprotective activities, reduce alcohol dependence, increase energy metabolism, acid-forming secretory function

REFERENCES:
Ronai, E. et al. "The Inhibitory Effect . . . " Int. J. Radiat, Bio., 1987 vol. 51, No. 4611617 pp. 3611-3617.
Ivnitski, Y. Y. et al. "Protection of Mice. . . " Radiobiology, Academy of Science of USSR, vol. 30, 5 ed., 1990, pp. 704-706.
Freidman, S. L. et al. "Comparison of Effect. . . " Succinic Acid Therapeutic Effect, Academy of Science of the USSR, 1976, pp. 49-55, pp. 106-110.
Mochizuki et al., "Intoxication-free alcohol beverages", Chemical Abstracts 108:93106, 1990.

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