Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1993-06-21
1998-03-03
Scheiner, Toni R.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
514957, A61K 3800
Patent
active
057234396
DESCRIPTION:
BRIEF SUMMARY
THE FIELD OF TECHNOLOGY
The present invention pertains to a new pharmaceutical aerosol composition and employment thereof for treatment and prevention of viral diseases.
DESCRIPTION OF PRIOR ART
At present, a number of therapeutic substances are known such as amantadine (Douglas, R. G.--Respiratory Diseases., 1979, pp. 413-425. In: "Antiviral Agents and Viral Diseases of Man", Raven Press, New York, G. Galasso, ed.), ribavirin (Douglas, R. G.--Ibidem, pp. 425-428), and biologically active polypeptides such as interferon (Scott et al., Brit. Med. J., 1982, v. 284, p. 1822) which are capable of inhibiting an infectious process induced by orthomyxo--(influenza viruses) and paramyxoviruses. Their therapeutic effect is due to the capacity to block reproduction of the above-mentioned viruses. Therapeutically, they are employed in different medicinal forms: tablets, capsules, solutions for injections, and aerosols, the latter being most preferable. This is explained by the fact that in viral-bacterial respiratory diseases the broncho-pulmonary epithelium is primarily affected, therefore the employment of the active substance through the respiratory tract in the form of micronized particles of no more than 200 .mu.m in size will be most effective. The application of the aerosol form of medicinal substances of the amantadine series is known, however, the above-mentioned therapeutic substances are active only against influenza type A viruses but not against influenza type B viruses, paramyxoviruses, and many other viruses, that is, they show a selective therapeutic effect.
Attempts are known to have been made to create antiviral medicinal drugs based on aprotinins, inhibits of proteinases (Zhirnov, O. P.--J. Med. Virol., 1987, 21:p.161-167). Aprotinins are natural low molecular polypeptides inhibiting a wide range of proteinases. There are officinal aprotinin preparations: Gordox (Gedeon Richter), Contrycal (Germed), Trasylol (Bayer AG), Antagosan (Behring). The antiviral and therapeutic effect (inhibition of pulmonary pathology, prevention of animal deaths) was achieved by parenteral (intraperitoneal) inoculation of aprotinin. A sufficiently high dose of aprotinin preparation was from 10,000 to 15,000 kallikrein-inhibiting units (KIU) (animal/day). When inoculated parenterally, aprotinin polypeptides are absorbed into the blood channel where, binding with various blood proteins, they change their physico-chemical (charge, ionization degree, molecular weight, conformation structure) and functional characteristics. Such protein complexing may result in masking and inhibition of aprotinin activity and blocking of the passage of the complexes from the blood into the respiratory tract. As a result, the mechanism of the antiviral effect is transformed and the therapeutic effect is lowered.
BRIEF DISCLOSURE OF THE ESSENCE OF THE INVENTION
The main purpose of the invention was to develop a pharmaceutical aerosol composition of the basis of biologically active polypeptide in the form of an aqueous solution or solid microparticles which, in a lower effective therapeutic dose, would exert an enhanced antiviral and pathogenetic effect in therapy or prophylaxis in man and animals suffering from respiratory tract diseases.
This task is solved by the fact that the pharmaceutical aerosol composition of the invention contains, as the active substance, a proteinase inhibitor of the aprotinino group dissolved in water in amounts of from 1500 to 10,000 KIU/ml of solution.
It is expedient, for better stability of the aerosol and enhancement of its adsorption in the respiratory tracts, to include into the composition a surfactant, preferably Twin-80 or glycerol. The proposed composition is applied predominantly for different parts of the respiratory tract.
The aprotinin consisting of microparticles of aerosol with different humidity is prepared by atomization of an aqueous solution in an air stream or a propellent by means of an atomizer providing the obtainment of a proper size of the particles in relation to the localization si
REFERENCES:
patent: 4153687 (1979-05-01), Schnabel et al.
patent: 4613500 (1986-09-01), Suzuki et al.
patent: 5262157 (1993-11-01), Bernard et al.
Gebhard, W. et al. "Biochemistry of Aprotinin . . . " Proteinase Inhibitors, Chapter 10, (1986) pp. 375-388.
Zhirnov, O.P. "High Protection . . . " Journal of Medical Virology 21, (1987) pp. 161-167.
Hubbard et al. PNAS, USA vol. 86 pp. 680-684 (1989).
R. Gordon Douglas, Jr. "Respiratory Diseases" Antiviral Agents and Viral Diseases of Man, Raven Press, New York, 1979, pp. 385-429.
Remington's Pharmaceutical Sciences, pp. 1694-1712, 1990.
Ovcharenko Alexandr Valentinovich
Zhirnov Oleg Petrovich
Huff Sheela J.
Scheiner Toni R.
Zhirnov Oleg Petrovich
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