EP0243352A1 - Verfahren zur ermässigung der wahrscheinlichkeit einer infektion durch aids-virus(htlv-iii/lav/arv) - Google Patents

Verfahren zur ermässigung der wahrscheinlichkeit einer infektion durch aids-virus(htlv-iii/lav/arv)

Info

Publication number
EP0243352A1
EP0243352A1 EP19850905565 EP85905565A EP0243352A1 EP 0243352 A1 EP0243352 A1 EP 0243352A1 EP 19850905565 EP19850905565 EP 19850905565 EP 85905565 A EP85905565 A EP 85905565A EP 0243352 A1 EP0243352 A1 EP 0243352A1
Authority
EP
European Patent Office
Prior art keywords
anions
zinc
compounds
infection
ipg
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
EP19850905565
Other languages
English (en)
French (fr)
Inventor
William Sergio
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of EP0243352A1 publication Critical patent/EP0243352A1/de
Pending legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/28Compounds containing heavy metals
    • A61K31/315Zinc compounds

Definitions

  • AIDS has become a serious problem in both homosexual and heterosexual groups around the world.
  • the disease is life-threatening ⁇ disabling* and may well be the greatest threat faced by centuries. Since many persons at high risk or who are already infected with the virus continue to engage in sexual activity, which is a known factor in the spread of this disease, there can be no question as to the need for a safe, simple, inexpensive, effective and available treatment to minimize the risk or probability of infection during periods of such physical contact or exposure.
  • anions of charge greater than one can inhibit replication of many of the antigentically different viruses including the suspected infectious agent of AIDS, namely HTLV-III/LAV/ARV.
  • anion shall refer to anions of charge greater than one.
  • Metal ions are required in virtually every phase of genetic information ransfer, and they are essential components of biochemical processes involving DNA and RNA. However, under the correct conditions metal ions can have deleterious effects such as the distortation and/or inactivation of enzynes such as reverse transcriptases and the degradation of polyribonucleotides, is not frequently considered by physicians and researchers when seeking a method of reducing the probability of infection by a viral agent by lowing the viral titer in external mucosa of the body.
  • RNA retroviruses such as HTLV-III/LAV/ARV both in vitro and in vivo.
  • concentration of anions required to be antiviral would require at least 10(-4)M or greater which is 10 times or more than the ion concentration of human serum of any single anions normally present.
  • inhibitory effects on different viruses by different anions are reversible and provide no lasting effect once the anions are removed from the medium. In the case of many viruses, when anion sources are removed they will resume their replication and again become fully ineffective.
  • anion sources to slow and/or stop viral replication can be used effectively in the case of the AIDS virus (HTLV-III/LAV/ARV) to reduce the risk or probability of viral infection PRIOR to the virus entering the body by limiting viral titers in external mucosa.
  • the anion source HPA-23 as been shown to effectively block the reverse transcriptase required by the AIDS viruses (HTLV-III/LAV/ARV). In this way, the AIDS virus (HTLV-III/LAV/ARV) seems unique because of its rapid rate of replication and mutation it is more and unusually susceptible to the actions of compounds that generate anions.
  • Some compounds that generate anions may play a fundamental role in the human body as the body's natural antiviral agent. This is evidenced by the fact that zinc is concentrated in mast cells. This means that zinc may be given in higher quantities and for much longer periods of time in the body.
  • the main function of mast cells may be to deliver zinc anions right to the site of a viral infection.
  • the mast cell is known to contain large amounts of histamine and to be involved in allergic responses. Its release of this histamine is responsible for the familar symptoms of swelling, redness, and runny noses associated with allergies. However, it is my conjecture that the mast cell serves a well-defined function in the immune system of being the vehicle that delivers zinc anions directly to the site of a viral attack.
  • Mast cells through an unknown mechanism, are drawn to the site of a viral infection. These cells contain large stores of zinc ions which are released at the site of the virus attack. While the zinc remains in the form of anions in the neighborhood of the mast cell, the mast cell is chemically inhibited from releasing its histamine. After the zinc anions have reacted with the virus and viral components, the now lowered concentration of zinc anions in the vicinity of the mast cells no longer inhibits the release of histamine. When this concentration of zinc ions gets sufficiently low in the vicinity of the mast cell, the mast cell can release its histamine. The released histamine dilates small blood vessels, thus allowing a greater supply of blood and more cells into the area of viral infection.
  • the concentration of zinc in human plasma is about 10(-5)M and this concentration of zinc anions markedly inhibits in vitro histamine release from human basophils like mast cells. Inhibition begins at even lower levels and is freely reversible. Human basophils, like mast cells, contain high concentrations of zinc and zinc is released with histamine after antigen challenge. High concentrations of zinc anions inhibit histamine release and significant amounts of zinc anions are released after antigen challenge.
  • anions can inhibit replication of many viruses, including the AIDS virus HTLV-III/LAV/ARV, one may theorize that a pharmaceutically safe dosage of compounds that generate such anions will only produce anion concentrations that can reach antiviral concentrations if the method of application is such that it maintains a sufficiently high level of anions in the locus of viral infection to prevent continued viral replication. It has been demonstrated that the AIDS virus (HTLV-III/LAV/ARV) can infect both T-cells and neurons.
  • IPG is defined as a compound or complex capable of producing anions, of charge greater than one, that if applied to the body by any method, produces levels of anions in the external mucosa and surface regions of the body that are antiviral and reduce the risk or probability of infection from the ineffective agent of AIDS.
  • ZPG-1 is defined as compounds or complexes that contain zinc and generate zinc anions or provide a source of anions.
  • This invention relates to a new method for reducing the risk or probability of infection from the AIDS VIRUS (HTLV-III/LAV/ARV) through the use of compounds applied in a manner and at a frequency so as to cause a sustained, abnormal concentration of anions in external tissues during contact with the source of this virus and until it is removed.
  • AIDS VIRUS HTLV-III/LAV/ARV
  • Several compounds that effectively generate anions in antiviral amounts when applied topically to the oral, anal, or vaginal mucosa are listed.
  • the objective of this invention is to correct the lack of a prior art in the reduction of the risk or probability of infection from the AIDS virus.
  • the invention disclosed and is a method to reduce the risk or probability of infection with the infectious agent that causes AIDS.
  • Such method involves administration of pharmaceutically acceptable IPG compounds that generate anions TOPICALLY when applied to oral, pharyngeal, nasal, anal, and/or vaginal mucosal membranes by a manner that raises the concentration of anions in virally infected areas. Those concentrations are maintained for a period of time during contact with a possible source of infection.
  • Means of application include, but are not limited to the following direct, indirect, carrier, and special means or any combination of means.
  • IPG compounds Direct application of such IPG compounds may be through the use of throat lozenges or troches, or through the use of anal or vaginal suppositories or douches, anal or vaginal napkins, creams or ointments or liquids, and through the use of mouth washes or gargles, nasal sprays, nasal drops, nasal oinments,nasal washes,nasal injections,packings, or indirectly through the use of ,or through the use of inhalants or ointments applied to the nasal nares, or any combination of these and similar methods of application.
  • Carriers such as dimethyl sulfoxide and other special methods such as oral ingestion or parental introduction of IPG compounds where such treatment allows elevation of anions sufficiently and topically topically in areas outside of the body that are exposed to the AIDS virus.
  • any means of administration including oral ingestion or parental administration, may be used as needed.
  • the forms in which the IPG compounds may be administered include but are not limited to lozenges, troches, candies, injectants, chewing gums, tablets, powders, sprays, liquids, ointments, and aerosols.
  • IPG compounds examples include the gluconate, ascorbate, citrate, oxide, acetate, picolinate, transferrin, orotate and aspartate salts of zinc;and,in particular,the phosphonoformate salt or complex of zinc, the palmitate salt, and complexes of zinc tungstanate are exceptionally promising from my own early calculations . and, HeteroPolyAnion compounds known as HPA such as HPA-23.
  • IPG compounds that are lipid soluble are particularly important in that they can penetrate the lipid layer surrounding the neuron in the mucosal areas and provide resistance to infection by the AIDS virus (HTLV-III/LAV/ARV). This is particularly important since it is hypothesized that this virus infects the nervous system through parasynpathetic neurons. The disease becomes completely manifest only after the infection travels up to the brain stem, and then eventually reaches down to the thynus, where T cells become infected by virus budding from neurons at critical times in their cell cycle, or at ⁇ arly 100% incidence, or both.
  • AIDS virus HTLV-III/LAV/ARV
  • lozenges or anal or vaginal suppositories or other appropriate vehicle that contain combinations of different IPG compounds with different abilities to generate anions in aqueous and lipid phases as well as the use of salts or complexes where the cation portion exhibits unique antiviral activity to the AIDS virus (HTLV-III/LAV/ARV).
  • such a combination of IPG compounds might be zinc gluconate, zinc palmitate, zinc phosphonoformate, and zinc tungstanate.
  • the gluconate forms anions in aqueous phases easily.
  • the palimitate forms anions in lipid phases easilyand the phosphonoformate and tungstanate complexes have other antiviral properties in addition to their ability to generate zinc anions in the external mucosa.
  • the zinc anions are complexed with tungstanate and phosphonoformate moieties which have their own antiviral actions against the AIDS virus (HTLV-III/LAV/ARV) and other viruses in addition to their ability to generate zinc anions from their complexes with zinc.
  • AIDS virus HTLV-III/LAV/ARV

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
EP19850905565 1985-10-21 1985-10-24 Verfahren zur ermässigung der wahrscheinlichkeit einer infektion durch aids-virus(htlv-iii/lav/arv) Pending EP0243352A1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US78932485A 1985-10-21 1985-10-21
US789324 1985-10-21

Publications (1)

Publication Number Publication Date
EP0243352A1 true EP0243352A1 (de) 1987-11-04

Family

ID=25147296

Family Applications (1)

Application Number Title Priority Date Filing Date
EP19850905565 Pending EP0243352A1 (de) 1985-10-21 1985-10-24 Verfahren zur ermässigung der wahrscheinlichkeit einer infektion durch aids-virus(htlv-iii/lav/arv)

Country Status (3)

Country Link
EP (1) EP0243352A1 (de)
AU (1) AU5014285A (de)
WO (1) WO1987002246A1 (de)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8906190D0 (en) * 1989-03-17 1989-05-04 Johnson Matthey Plc Improvements in chemical compounds
US5624675A (en) * 1989-06-06 1997-04-29 Kelly; Patrick D. Genital lubricants containing zinc salts to reduce risk of HIV infection
US5599551A (en) * 1989-06-06 1997-02-04 Kelly; Patrick D. Genital lubricants containing zinc as an anti-viral agent
US5785054A (en) * 1989-06-06 1998-07-28 Kelly; Patrick D. Genital lubricant with zinc salt, labelled as anti-viral agent
EP0402078A3 (de) * 1989-06-06 1991-07-31 Patrick Daniel Kelly Sexuelles Gleitmittel mit Zink als antiviralem Wirkstoff
US5208031A (en) * 1989-06-06 1993-05-04 Kelly Patrick D Sexual lubricants containing zinc as an anti-viral agent
US5545673A (en) * 1989-06-06 1996-08-13 Kelly; Patrick D. Method for reducing risk of infection by sexually transmitted viruses
US5482053A (en) * 1989-06-06 1996-01-09 Kelly; Patrick D. Condom lubricants containing zinc as an anti-viral agent
DE4302053C1 (de) * 1993-01-26 1994-06-30 Gunther Dr Kuemel Pharmazeutische Zusammensetzung, die gegenüber Infektionen mit HIV-Viren prophylaktisch wirkt

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2245374B1 (de) * 1973-07-27 1977-02-25 Anvar
SE7607496L (sv) * 1976-07-01 1978-01-02 Astra Laekemedel Ab Sett for bekempning av virusinfektioner
LU77562A1 (de) * 1977-06-17 1979-03-26 Ciba Geigy Ag Verfahren zur herstellung von neuen pharmazeutischen praeparaten

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO8702246A1 *

Also Published As

Publication number Publication date
WO1987002246A1 (en) 1987-04-23
AU5014285A (en) 1987-05-05

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