Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1994-07-13
1996-04-23
Cintins, Marianne
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
A61K 3118, A61K 3821, A61K 31505
Patent
active
055103871
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/Ru93/00209 filed Aug. 31, 1993.
FIELD OF ART
The present invention relates to medicine and, more specifically, to an antimicrobial and interferon-inducing medicament.
BACKGROUND OF ART
Widely known in the prior art is administration of para-aminobenzenesulfamide (Streptocidum album, Sulfanilamidum), one of the chemotherapeutic preparations of sulfanilamide group. The preparation exerts an antimicrobial effect with relation to streptococcus, meningococcus, gonococcus, pneumococcus, colibacillus and some other bacteria. Said preparation is utilized predominantly in a tablet form. Injection forms of said preparation presuppose their conversion into soluble salts, for example, the formation of soluble compounds through a primary aromatic group. However, this structure is unstable and calls for introducing a stabilizer, i.e. toxic sodium sulfite (M. D. Mashkovsky "Medicinal Drugs", Moscow, "Meditsina", 1984, vol. 2, p. 275-277; G. A. Melentieva, "Pharmaceutical Chemistry", Moscow, "Meditsina", 1986, p. 285-286). In addition, the antimicrobial effect of said preparation is exhibited only in presence of an open aminogroup in a para-position to the sulfanilamide group, so that the degree of its opening and, consequently, its antimicrobial effect well depend on time and on physiological constants of blood. This currently-used preparation in a soluble form (Streptocidum Solubile) features a number of negative properties, such as side effects associated with administration of a toxic stabilizer, irritant effect, low biological availability.
It is common knowledge that para-aminobenzenesulfanilamide can crystallize in the form of three polymorphic modifications designated by .alpha.-, .beta.-, .gamma.-forms (Journal of Pharmaceutical Sciences, v. 58, 59, No. 7, July 1970, p. 972-975; Journal of Pharmaceutical Sciences of Japan, 1942, m.63, No.11, p. 17-19) of which only .alpha.-form is used in practical medicine. The pharmacokinetic properties of the crystalline .gamma.-modification of para-aminobenzenesulfanilamide have not been described. The use of .gamma.-modification as an active principle of the medicament is unknown. Besides, the use of .alpha.-, .beta.- and .gamma.-modifications of para-aminobenzenesulfanilamide in the capacity of interferon inducers is not known either.
It is common knowledge that all inducers of interferon, the most important factor of nonspecific resistance of cells, are divided into two groups, viz., natural (viruses and natural two-spiral nucleic acids) and synthetic (polymers and low-molecular preparations) (F. I. Ershov et al, collected works "Interferon Inducers", Moscow, 1982, p. 7-18).
The natural inducers of interferon are highly antigenic, can be contaminated by other dangerous microorganisms and all of them exert a toxic effect in concentrations requisite for displaying sufficient antiviral activity. The same disadvantages are inherent in the majority of high-molecular synthetic interferon inducers--polycarboxylates and polynucleotides (type poly () and poly (). They are likewise sufficiently toxic while their synthesis is difficult and economically unremunerative.
Clinically promising are also such low-molecular interferon inducers as gossypol analogs, thyloron preparation (2,7-bis-(2-diethylaminoethoxy)-3-fluorenon) and levamisol (-) 2,3,5,6-tetrahydro-6-phenyl-imidaso-(2,1-B)-thiazole hydrochloride) (M. D. Mashkovsky, "Medicinal Drugs", Moscow, "Meditsina", 1986, vol. 2 p. 169-171).
However, all these preparations are noted for high toxicity and numerous side effects, and, what is more, interferon induction shows up after administration of large doses and is effective for a short time only.
DISCLOSURE OF THE INVENTION
The main object of the invention resides in developing a new medicinal drug possessing an antimicrobial and interferon-inducing effect, a high therapeutic efficiency, low toxicity, absence of side effects, and in reducing the time of treatment at diminished doses.
This object of attained by providing a medicinal preparatio
REFERENCES:
patent: 4401663 (1983-08-01), Buckwalter et al.
patent: 5151265 (1992-09-01), Hwang-Felgner et al.
Melent'Eva, G. "Pharmaceutic Chemistry" Moscow, 1968, pp. 285-286.
Mashkovsky, M., "Medical Substances" Handbook on Pharmacotherapy for Medical Practitioners, 1984, pp. 275-277.
Mashkovsky, M., "Medicinal Substances" Handbook on Pharmacotherapy for Medical Practitioners, 1986, pp. 169-171.
Zhdanoy, V., Ed., "Interferon Inducers" USSR Academy of Science, 1982, pp. 7 to 18.
Lin, H., et al., "Polymorphism in Sulfanilamide-dy" Journal of Pharmaceutical Studies vol. 59, No. 7, Jul. 1970, pp. 972 to 975.
Watanabe, A., "The Phenomenon of Polymorphism in Sulfanilamide", 1985.
Leonidov Nikolai B.
Seleznev Nikolai G.
Cintins Marianne
Leonidov Nikolai Borisovich
MacMillan Keith
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