Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1995-12-18
2000-02-01
Travers, Russell
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514457, 514474, 514458, 514358, 514763, A01N 4360, A01N 4308, A01N 4316, A01N 2700
Patent
active
060203331
DESCRIPTION:
BRIEF SUMMARY
The use of condoms intended for the prevention of sexually-transmissible diseases and namely the diseases due to HSV2 and HIV viruses, as well as the genito-anal infections due to papillomavirus does not appear to obey to the prophylactic sanitary recommendations. This restriction in the use in connection with socio-economic, technical or sexual reasons, lead to propose some other solutions to limit the venereal propagation and count. The use of salves, vaginal suppositories and suppositories made of biological and not toxic anti-viral molecules seems to supply with a response ot this need. Such an alternative appears to be more especially as advantageous, the used molecules may further show anti-inflammatory, anti-allergic, anti-bacterial, anti-fungal, immonostimulating and healing properties. Some tests with chemical synthetic molecules with anti-viral activity have been performed. So have been proposed sponges based on nonoxynol-9 with the aim to be both contraceptive and virulicide. These tests are far to be conclusive from a point of view of efficacy and moreover the products to be used produced micro-lesions of the vaginal wall. Once again experimentation carries the proof of the existing gap between "in vitro" efficacy then "in vivo" efficacy and tolerance. This invention has thus as a subject matter a composition based on biological molecules having shown an "in vitro" anti-viral activity but being totally non toxic and even displaying local curative properties due to recovery of the cell respiratory chain, the equilibrium of oxydo reduction and the healing of the mucosal microlesions from carential origin.
Consequently, this invention has as a subject matter novel pharmaceutical compositions having anti-viral action intended for the local protection of the genital and rectal mucosae, wherein they contain as an active ingredient, riboflavin and/or one of an acid addition salt thereof with a mineral or organic acid and/or FAD.
The active ingredient may be further added with Niacine and/or NAD and/or NADP. They may be also added vitaminic factors, such as carotenoids, flavonoids, acetylcoenzyme A, vitamins A, E, C, B6, B8 and/or F.
It may be also added to the compositions filling agents which increase adhesiveness of the preparations to the mucosae such as insoluble salts of baryum, titanium derivatives, earth alkaline silicates, mineral or organic salts of bismuth, insoluble salts of zinc, derivatives of rare earths, derivatives of zirconium.
It may also be possible to incorporate to the pharmaceutical compositions according to this invention, vegetal extracts containing flavonoids or anthrocyanosides.
The preferred pharmaceutical compositions are the creams, the gels, the milks, the viscous emulsions, the suppositories, the vaginal suppositories, the capsules, the vaginal tablets and the like.
The initial effect relates at first in preventing the viral sexually transmissible diseases (AIDS, genital herpes, papillomavirus). However, if the same mixture both may be curative and offer complementary properties, it is a matter of undeniable advantage. It will substantially be antibacterial, antifungal, antiparasitic, anti-allergic and anti-inflammatory actions, trophic effects, healing effects and finally vasculotropic effects.
Riboflavin and FAD (or FADH2) may be used alone. However, complementary and action synergy brought by Niacin and its active forms, acetylcoenzyme A, Vitamins A, E, C, biotin, flavonoids, carotenes are interesting to take into consideration. The addition of pyridoxal-5-phosphate and of N5-methyl tetrahydrofolate may be useful.
Such a composition having anti-oxydising polarity is intended to be applied or introduced at the level of mucosae, depending on the knowledge of the pharmacokinetics and of the galenical pharmacy.
The preparations intended to the local application will be offer in the form of ointments, gels, creams, foams or any other preparations issued from the recent galenical pharmacy. The preparations intended for endo-vaginal or endo-rectal insertion are of about the
REFERENCES:
patent: 5366440 (1994-11-01), Fossel
Isaacs et al 112 CA:112053g 1990.
Harukeh et al 113 CA:184287e 1990.
Child et al 108 CA 109452y 1988.
Totani et al 116 CA 99299c 1992.
Merchk Index 10.sup.th Ed 1985 # 5457 & 8338.
Jamison et al 110 CA: 209216j 1989.
Roedenen et al PNAS vol. 87 pp. 4884-4888 1990.
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