EP0243352A1 - Method for reducing the risk or probability of infection from the aids virus (htlv-iii/lav/arv) - Google Patents
Method for reducing the risk or probability of infection from the 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
Links
- 208000015181 infectious disease Diseases 0.000 title claims abstract description 21
- 238000000034 method Methods 0.000 title claims abstract description 16
- 241000700605 Viruses Species 0.000 title abstract description 24
- 150000001450 anions Chemical class 0.000 claims abstract description 41
- 241000725303 Human immunodeficiency virus Species 0.000 claims abstract description 18
- 150000002632 lipids Chemical class 0.000 claims abstract description 8
- 239000011701 zinc Substances 0.000 claims description 33
- 229910052725 zinc Inorganic materials 0.000 claims description 33
- -1 IPG compound Chemical class 0.000 claims description 20
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 claims description 19
- 230000000840 anti-viral effect Effects 0.000 claims description 15
- 150000001875 compounds Chemical class 0.000 claims description 14
- 210000004877 mucosa Anatomy 0.000 claims description 10
- 239000007937 lozenge Substances 0.000 claims description 6
- ZJAOAACCNHFJAH-UHFFFAOYSA-N phosphonoformic acid Chemical compound OC(=O)P(O)(O)=O ZJAOAACCNHFJAH-UHFFFAOYSA-N 0.000 claims description 6
- 239000002674 ointment Substances 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 230000001568 sexual effect Effects 0.000 claims description 4
- 239000006216 vaginal suppository Substances 0.000 claims description 4
- RGHNJXZEOKUKBD-SQOUGZDYSA-M D-gluconate Chemical class OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O RGHNJXZEOKUKBD-SQOUGZDYSA-M 0.000 claims description 2
- WHMDKBIGKVEYHS-IYEMJOQQSA-L Zinc gluconate Chemical compound [Zn+2].OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O WHMDKBIGKVEYHS-IYEMJOQQSA-L 0.000 claims description 2
- 210000001124 body fluid Anatomy 0.000 claims description 2
- 239000010839 body fluid Substances 0.000 claims description 2
- 239000002324 mouth wash Substances 0.000 claims description 2
- 150000002942 palmitic acid derivatives Chemical class 0.000 claims description 2
- 229960000306 zinc gluconate Drugs 0.000 claims description 2
- 235000011478 zinc gluconate Nutrition 0.000 claims description 2
- 239000011670 zinc gluconate Substances 0.000 claims description 2
- 229940012185 zinc palmitate Drugs 0.000 claims description 2
- GJAPSKMAVXDBIU-UHFFFAOYSA-L zinc;hexadecanoate Chemical compound [Zn+2].CCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCC([O-])=O GJAPSKMAVXDBIU-UHFFFAOYSA-L 0.000 claims description 2
- 239000000126 substance Substances 0.000 claims 1
- 239000000829 suppository Substances 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- 208000030507 AIDS Diseases 0.000 abstract description 11
- 208000036142 Viral infection Diseases 0.000 abstract description 6
- 230000009385 viral infection Effects 0.000 abstract description 6
- 230000002159 abnormal effect Effects 0.000 abstract description 2
- 230000002459 sustained effect Effects 0.000 abstract description 2
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 description 20
- 210000003630 histaminocyte Anatomy 0.000 description 13
- 229960001340 histamine Drugs 0.000 description 10
- 210000002569 neuron Anatomy 0.000 description 6
- 238000000338 in vitro Methods 0.000 description 5
- 230000010076 replication Effects 0.000 description 5
- 230000003612 virological effect Effects 0.000 description 4
- 102100034343 Integrase Human genes 0.000 description 3
- 108010092799 RNA-directed DNA polymerase Proteins 0.000 description 3
- VFBJEDFCUUCMBQ-UHFFFAOYSA-O azanium;sodium;antimony(3+);oxygen(2-);tungsten Chemical compound [NH4+].[O-2].[Na+].[Sb+3].[W] VFBJEDFCUUCMBQ-UHFFFAOYSA-O 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 239000012678 infectious agent Substances 0.000 description 3
- 239000012071 phase Substances 0.000 description 3
- 230000029812 viral genome replication Effects 0.000 description 3
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 2
- 210000001744 T-lymphocyte Anatomy 0.000 description 2
- PTFCDOFLOPIGGS-UHFFFAOYSA-N Zinc dication Chemical compound [Zn+2] PTFCDOFLOPIGGS-UHFFFAOYSA-N 0.000 description 2
- 230000009471 action Effects 0.000 description 2
- 239000000427 antigen Substances 0.000 description 2
- 102000036639 antigens Human genes 0.000 description 2
- 108091007433 antigens Proteins 0.000 description 2
- 239000003443 antiviral agent Substances 0.000 description 2
- 230000004888 barrier function Effects 0.000 description 2
- 210000003651 basophil Anatomy 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 description 2
- 230000037406 food intake Effects 0.000 description 2
- 230000000652 homosexual effect Effects 0.000 description 2
- 238000001727 in vivo Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 230000007246 mechanism Effects 0.000 description 2
- 229910021645 metal ion Inorganic materials 0.000 description 2
- 230000002441 reversible effect Effects 0.000 description 2
- 210000001519 tissue Anatomy 0.000 description 2
- 238000011282 treatment Methods 0.000 description 2
- 210000000605 viral structure Anatomy 0.000 description 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
- 206010015150 Erythema Diseases 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical class OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 1
- 208000036071 Rhinorrhea Diseases 0.000 description 1
- 206010039101 Rhinorrhoea Diseases 0.000 description 1
- 206010042674 Swelling Diseases 0.000 description 1
- 102000004338 Transferrin Human genes 0.000 description 1
- 108090000901 Transferrin Proteins 0.000 description 1
- 239000000443 aerosol Substances 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 239000008346 aqueous phase Substances 0.000 description 1
- 229940072107 ascorbate Drugs 0.000 description 1
- 235000010323 ascorbic acid Nutrition 0.000 description 1
- 239000011668 ascorbic acid Substances 0.000 description 1
- JVUIPFRSLYDCCX-UHFFFAOYSA-O azanium;antimony(3+);oxygen(2-);tungsten Chemical compound [NH4+].[O-2].[O-2].[O-2].[O-2].[O-2].[Sb+3].[W] JVUIPFRSLYDCCX-UHFFFAOYSA-O 0.000 description 1
- 230000003851 biochemical process Effects 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 210000000133 brain stem Anatomy 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 150000001768 cations Chemical class 0.000 description 1
- 230000034303 cell budding Effects 0.000 description 1
- 230000022131 cell cycle Effects 0.000 description 1
- 235000015218 chewing gum Nutrition 0.000 description 1
- 229940001468 citrate Drugs 0.000 description 1
- 210000003555 cloaca Anatomy 0.000 description 1
- 229960003920 cocaine Drugs 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- 230000002939 deleterious effect Effects 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000002068 genetic effect Effects 0.000 description 1
- 229940050410 gluconate Drugs 0.000 description 1
- 230000002650 habitual effect Effects 0.000 description 1
- 230000000423 heterosexual effect Effects 0.000 description 1
- 210000000987 immune system Anatomy 0.000 description 1
- 230000002779 inactivation Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- 230000002045 lasting effect Effects 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 230000035772 mutation Effects 0.000 description 1
- 239000007923 nasal drop Substances 0.000 description 1
- 229940100662 nasal drops Drugs 0.000 description 1
- 239000007922 nasal spray Substances 0.000 description 1
- 210000000653 nervous system Anatomy 0.000 description 1
- 210000000118 neural pathway Anatomy 0.000 description 1
- 230000010004 neural pathway Effects 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- PXQPEWDEAKTCGB-UHFFFAOYSA-N orotic acid Chemical compound OC(=O)C1=CC(=O)NC(=O)N1 PXQPEWDEAKTCGB-UHFFFAOYSA-N 0.000 description 1
- 238000012856 packing Methods 0.000 description 1
- 210000003254 palate Anatomy 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- SIOXPEMLGUPBBT-UHFFFAOYSA-M picolinate Chemical compound [O-]C(=O)C1=CC=CC=N1 SIOXPEMLGUPBBT-UHFFFAOYSA-M 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 239000012581 transferrin Substances 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- 241001430294 unidentified retrovirus Species 0.000 description 1
- 150000003752 zinc compounds Chemical class 0.000 description 1
- JITJDVYWXGOEMC-UHFFFAOYSA-L zinc;phosphonoformate Chemical compound [Zn+2].OP(O)(=O)C([O-])=O.OP(O)(=O)C([O-])=O JITJDVYWXGOEMC-UHFFFAOYSA-L 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/28—Compounds containing heavy metals
- A61K31/315—Zinc 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)
Abstract
Moyen pour réduire la probabilité de l'infection virale par le virus du sida au site de l'infection à l'extérieur du corps et avant l'infection par le sida. Egalement, procédé pour réduire le risque ou la probabilité d'infection par le virus du sida (HTLV-III/LAV/ARV) par l'utilisation de composés IPG qui offrent une source sûre et efficace d'anions qui sont appliqués d'une manière et à une fréquence telles qu'une concentration anormale et soutenue d'anions s'installe dans les tissus infectés par le virus, dans les phases aqueuse ou lipide ou les deux phases au moment de l'exposition à ce virus.Means to reduce the likelihood of viral infection with the AIDS virus at the site of infection outside the body and before infection with AIDS. Also, a method of reducing the risk or likelihood of infection with the AIDS virus (HTLV-III / LAV / ARV) by the use of IPG compounds which provide a safe and effective source of anions which are applied in a in such a way and at such a frequency that an abnormal and sustained concentration of anions settles in the tissues infected by the virus, in the aqueous or lipid phases or both phases at the time of exposure to this virus.
Description
/•***• METHOD FOR REDUCING THE RISK OR PROBABILITY OF INFECTION FROM THE AIDS VIRUS (HTLV-III/LAV/ARV)
BACKGROUND
The art of preventing infection or prophylaxis or simply reducing the risk or probability of infection from the infectious agent of Acquired Immune Deficiency Syndrome (AIDS) during sexual intercourse, fellatio, cunningulus, anal intromission, and sexual contact and exchange in any manner of body fluids of any kind has been lacking.
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 mankind. 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.
Heretofore, prophylactic measures were non existent.
PRIOR ART It has been established in vitro that 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. Hereinafter, the term "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.
Anions of numerous elements and complexes inhibit the reverse transcriptase of the AIDS virus required fr viral replication.
In particular, zinc anions and HeteroPolyAnions, such as HPA-23 (5-tungsto-2-antimoniate), have been found to be antiviral to RNA retroviruses such as HTLV-III/LAV/ARV both in vitro and in vivo. The 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. But other in vitro studies have demonstrated that 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.
The use of compounds that generate or provide an anion source are of limited value, in general, because they do NOT destroy virus particles, but prevent replication of the virus ONLY while the anion source is in contact with the virus. In most cases, toxicity of such compounds prevents long-term or lifetime use of such compounds. However, the limited action of 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, i.e. some zinc compounds, 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.
In studying zinc, I was amazed by the fact that NO OTHER antiviral agent, except zinc, was effective against such a broad group of viruses while exerting its antiviral actions through so many different mechanisms. In medical school, I was fascinated by the puzzle of why the mast cells contained such large quantities of zinc as well as histamine and guessed that zinc serves as the body's own source of antiviral anions.
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.
Because it has been established in vitro and in vivo that 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.
For the purpose of convience, let me define two terms here. First, the term "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. Second, the term "ZPG-1," is defined as compounds or complexes that contain zinc and generate zinc anions or provide a source of anions.
SUMMARY OF THE INVENTION
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. Several compounds that effectively generate anions in antiviral amounts when applied topically to the oral, anal, or vaginal mucosa are listed.
Accordingly, 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.
DETAILED DESCRIPTION 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. 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.
So long as the concentration of anions is raised OUTSIDE the body in mucosal areas or in the surface neurons of the mucosa that may be exposed to the AIDS virus, then 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.
Examples of pharmaceutically acceptable IPG compounds that may be used in sufficiently low and safe dosages 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 ηarly 100% incidence, or both.
Repeated exposure to this virus may be necessary for infection or manifestation of the AIDS.
Homosexuals and habitual drug abusers, both have strong likehood of minor trauma at the time of exposure, the former in the cloaca, which may be torn, the latter at the site of injection or in the nasopharyngeal passages, which are likely to be raw if cocaine is used. Hemophiliacs are probably more sensitive ti this virus since it is known that they have small unhealed lesions in parasynpathetically supplied organs. Children have more delicate palate and nasal tissues than adults which probably accounts, in part, for their greater suspectibility to the AIDS virus (HTLV-III/LAV/ARV). With regard to
the neural pathway of infection, compounds such as zinc pal itate which is lipid soluble can penetrate and reside in mucosal neurons to add a further barrier of protection. In particular, zinc anions are able to easily penetrate lipid barriers.
Also included are 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).
As an example, 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. In the case of the phosphonoformate and the tungstanate, 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.
There are no known contraindication to this method if suitable IPG compounds are selected.
Claims
1. The novel method of reducing the risk or probability of infection from the AIDS virus (HTLV-III/LAV/ARV) by administering certain compounds that can generate antiviral concentrations of anions when appied topically to the external mucosa of the body such as the oral, anal, or vaginal mucosa comprising:
applying, in the form of lozenges or troches, or through the use of anal or vaginal suppositories or through mouth washes or garles, or through the use of inhalants or ointments applied to the nasal nares, or through the use of other such means IPG compounds that generate anions or their equivalent electrochemicall to the oral, anal, vaginal, or any external mucosa of a human desiring a means of reducing the risk or probability of infection from the AIDS virus HTLV-III/LAV/ARV during sexual contact or contact in which exchange of body fluids may take place; permitting anions to remain in contact with the mucosa for a period of time necessary for lozenges or suppositories or other appropriate carrier to dissolve and/or produce anions in sufficient quantities; and applying additional dosages of IPG compounds until exposure to the source of possible AIDS virus is ended.
2. The method according to claim 1 wherein IPG compounds or complexes each contain appropriate pharmacologically suitable dosages of IPG that deliver antiviral concentrations of anions that reduce the probability of infection with the AIDS virus (HTLV-III/LAV/ARV) when applied once or at repeated intervals either prior, during, or after physical contact between two or more persons using such compounds in the manner prescribed.
3. The method according to claim 1 of using an IPG compound, such as zinc, combined as a salt or complex with another chemical that has antiviral properties. For example, zinc combined as a salt or complex with either or both the phosphonoformate or the tungstanate in order to obtain the combined antiviral effects of the zinc anions and the other antiviral properties of the phosphonoformate and tungstanate moieties.
4. The method according to claim 1 wherein several salts or complexes of IPG compounds are used together. For example, zinc gluconate and zinc palmitate combined in the same lozenge, or anal, or vaginal suppositories or other appropriate vehicle. The gluconate salt is used for its ability to generate anions in water; the palmitate salt for its ability to generate anions in lipids.
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 (en) | 1987-11-04 |
Family
ID=25147296
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP19850905565 Pending EP0243352A1 (en) | 1985-10-21 | 1985-10-24 | Method for reducing the risk or probability of infection from the aids virus (htlv-iii/lav/arv) |
Country Status (3)
| Country | Link |
|---|---|
| EP (1) | EP0243352A1 (en) |
| AU (1) | AU5014285A (en) |
| WO (1) | WO1987002246A1 (en) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8906190D0 (en) * | 1989-03-17 | 1989-05-04 | Johnson Matthey Plc | Improvements in chemical compounds |
| US5545673A (en) * | 1989-06-06 | 1996-08-13 | Kelly; Patrick D. | Method for reducing risk of infection by sexually transmitted viruses |
| US5785054A (en) * | 1989-06-06 | 1998-07-28 | Kelly; Patrick D. | Genital lubricant with zinc salt, labelled as anti-viral agent |
| EP0402078A3 (en) * | 1989-06-06 | 1991-07-31 | Patrick Daniel Kelly | Sexual lubricants containing zinc as an anti-viral agent |
| US5482053A (en) * | 1989-06-06 | 1996-01-09 | Kelly; Patrick D. | Condom lubricants containing zinc as an anti-viral agent |
| US5599551A (en) * | 1989-06-06 | 1997-02-04 | Kelly; Patrick D. | Genital lubricants containing zinc as an anti-viral agent |
| US5208031A (en) * | 1989-06-06 | 1993-05-04 | Kelly Patrick D | Sexual lubricants containing zinc as an anti-viral agent |
| US5624675A (en) * | 1989-06-06 | 1997-04-29 | Kelly; Patrick D. | Genital lubricants containing zinc salts to reduce risk of HIV infection |
| DE4302053C1 (en) * | 1993-01-26 | 1994-06-30 | Gunther Dr Kuemel | Synergistic compsn. for preventing HIV infection |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2245374B1 (en) * | 1973-07-27 | 1977-02-25 | Anvar | |
| SE7607496L (en) * | 1976-07-01 | 1978-01-02 | Astra Laekemedel Ab | METHOD FOR FIGHTING VIRUS INFECTIONS |
| LU77562A1 (en) * | 1977-06-17 | 1979-03-26 | Ciba Geigy Ag | METHOD FOR PRODUCING NEW PHARMACEUTICAL PREPARATIONS |
-
1985
- 1985-10-24 EP EP19850905565 patent/EP0243352A1/en active Pending
- 1985-10-24 WO PCT/US1985/002067 patent/WO1987002246A1/en unknown
- 1985-10-24 AU AU50142/85A patent/AU5014285A/en not_active Abandoned
Non-Patent Citations (1)
| 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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