Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-02-22
1996-05-21
Kumar, Shailendra
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514307, A61K 3144, A61K 3147
Patent
active
055190286
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
This invention relates to the antiviral usage of flavopereirine. More specifically, it relates to a pharmaceutical preparation whose sole active ingredient is flavopereirine, and to the use of this preparation for the treatment of viral infections in human--in particular, infections such as those provoked by the Human Immunodeficiency Virus (HIV).
Flavopereirine is an alkaloid of the beta-carboline class. It is also traditionally referred to as "H or PB 100 composition," and shows UV emission fluorescence at 250-254 and 306 nm.
Flavopereirine may be obtained from the peel of the Pao Pereira Geissospermum vellosii-Baillon Apocynaceae (see H. Rapaport et al., J. Amer. Chem. Soc. 80:1601-1608 (1958) and Beljanski et al., request for first certificate of addition #79 05853 to French patent application #78 07155 and EP-A-0 059 817.).
It is known that flavopereirine, administered intracutaneously at a dosage of 200-600 .mu.g or a dosage of 2.5-500 mg/day, preferably 30 mg/day, prevents the appearance and development of vital papules in the case of viruses of the Shope fibrome type and of vaccine.
It is also known that flavopereirine appears to act in vivo against influenza (RNA virus), and that it may moreover inhibit the multiplication of the tobacco mosaic virus (TMV) after brief contact with this virus.
European Patent Application EP-A-0 059 817 reveals that flavopereirine is active against the influenza virus; however, the half-life of a quaternary beta-carboline of this type is too short for efficient use in humans in a galenic form other than time-release capsules.
French Patent Application No. 88 15845 describes a system for improving immune defense in humans (against RNA viruses--AIDS in particular--and DNA viruses). According to this document, the inhibition of the multiplication of the viruses in question is possible only by a combination of four different substances, of which flavopereirine is only one. The pharmaceutical preparation revealed in the document must include at least one representative of each of these four categories of active substances. The flavopereirine included in this combination is administered at a dosage of 0.25 g/day, preferably orally.
SUMMARY OF THE INVENTION
It has now unexpectedly been discovered that flavopereirine taken alone may act as an effective active agent in the struggle against HIV viruses in mammals, including humans. More specifically, it has been found that flavopereirine is an active agent which on its own, whether in vitro or in vivo exerts a selective inhibitive action on viral HIV infection, particularly in patients infected by HIV-1. Thus, in accordance with the present invention there is provided a method for the treatment of human immunodeficiency virus comprising administering to a human patient infected with human immunodeficiency virus an effective antiviral amount of a composition consisting of flavopereirine or a pharmaceutically acceptable salt or derivative thereof and a pharmaceutically acceptable carrier. The flavopereirine, or one of its salts or other acceptable pharmaceutical derivatives, is preferably administered in solid form containing approximately 250-500 mg of flavopereirine per dose.
It is also an object of the present invention to provide a method of using a pharmaceutical preparation based on flavopereirine in order to provide an antiviral treatment for HIV.
A further aspect of the present invention is an article of manufacture comprising a packaging material and a pharmaceutical agent contained within said packaging material, wherein said pharmaceutical agent contains flavopereirine as the sole active ingredient, and wherein said packaging material comprises a label which indicates that the pharmaceutical agent can be used for treatment of human immunodeficiency virus.
BRIEF DESCRIPTION OF THE DRAWINGS
FIG. 1 is a graphic representation of the comparative counts of cells/ml as a function of the number of hours following infection, the addition of flavopereirine (labeled "H") having been made 12 ho
REFERENCES:
patent: 5011853 (1991-04-01), Olney
Beljanski et al., "Selective Inhibiton of in vitro Synthesis of Cancer DNA by Alkaloids of the .beta.-Carboline Class", Exp. Cell Biol. 50: 79-87 (1982).
Rapaport et al., "Alkaloids of Geissospermum vellosii", J. Amer. Chem. Soc. 80: 1601-1604 (1958).
Hughes et al. "Flavopereirine, an Alkaloid from Geissospermum vellossii", J. Amer. Chem. Soc. 80: 1604-1609 (1958).
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