Note : Les descriptions sont présentées dans la langue officielle dans laquelle elles ont été soumises.
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A THERAPEUTIC COMPOSITION
FOR THE TREATMENT OF HIV-1 AND HIV-2
Applicant claims the benefit of following prior filed co-pending U.S. Patent
Application, Serial No. 10/353,483, filed 29 January X003.
BACKGROUND OF THE INVENTION
A pharmaceutical mixture for blocking the HIV-1 and/or HIV-2 virus
1 o replication in the CI~4+ cells of the human immune system in all stages of
that
viral infection, and in AIDS, also the method of production of the
pharmaceutical
mixture for blocking the HIV-1 and HIV-2 virus replication in the CI~4~+ cells
of
the human immune system in all stages of that viral infection, and in AIDS.
Hereinafter it should be understood that the terms "HIV treatment" and
15 "treatment of HIV in a patient in need of such treatment" mean treating a
patient
with HIV-1 and/or HIV-2. Additionally, the teen "blocking HIV virus
replication" means blocking HIV-1 andfor HIV-2 virus replication. Further the
term "HIV virus" refers to the HIV-1 andlor HIV-2 virus. Still further, the
term
"HIV infection" refers to HIV-1 and/or HIV-2 infection.
2 o The subject of the invention is a pharmaceutical mixture for blocking the
HIV-1 and HIV-2 virus replication in the CI~4+ cells of the human immune
system
in all stages of that viral infection, and in AIDS, also the method of
production of
the pharmaceutical mixture for blocking the HIV-1 and HIV-2 virus replication
in
the CD4+ cclls of the human immune system in all stages of that viral
infection,
z s and in All7S.
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The invented mixture has a particular application in treatment of the
Acquired Immunodeficiency Syndrome, or AIDS.
Synopsis of the Description
The subj ect of the invention is a pharmaceutical mixture for blocking the
HIV-1 and HIV-2 virus replication in the GD4+ cells of the human immune system
in that viral infection, and in All~S contains previously known carriers
and/or
auxiliary substances, as well as active substances, and it is characterized by
the
presence of at least 10 chemical substances as active substances, among them,
allocryptopine, present in the amount from 1.0 mg to 10.0 mg; nimodipine,
present
to in the amount from 20.0 mg to 100.0 mg; potassium iodide, present in the
amount
from 120.0 mg to 560.0 mg; potassium iodate, present in the amount from 30.0
mg
to 140.0 mg; inulina, present in the amount from 125.0 mg to 375.0 mg; silver,
present in the amount from 0.10 mg to 0.50 mg; zinc, present in the amount
from
10.0 mg to 20.0 mg; chromium, present in the amount from 0.05 mg to 0.20 mg;
orotic acid, present in the amount from 150.0 mg to 500.0 mg; desferrin,
present in
the amount from 100.0 mg to 300.0 mg
Summary
A pharmaceutical mixture and a method of its production of a therapeutic
2o composition for blocking the HIV-1 and HIV-2 virus replication in the
CI~4~+ cells
of the human immune system in all stages of that viral infection, and in
.~IL2S for
the treatment of HIV in a patient in need of such treatment, the therapeutic
composition comprising of pharmaceutically effective amounts of
allocryptopine,
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nimodipine, potassium iodide, potassium iodate, inuline, silver, zinc,
chromium,
orotic acid and desferrin. In one embodiment of the invention, the
pharmaceutical
mixture and method further comprises pharmaceutically effective amounts of
taraxasterol and B-sitosterol.
Detailed Description of the Invention
The invention pertains also to the method of production of the
pharmaceutical mixture for blocking the HIV-1 and HIV-2 virus replication in
the
C1~4+ cells of the human immune system in all stages of that viral infection,
and in
to AIDS, characterized by mixing, in the room temperature, of allocryptopine,
in the
amount from 1.0 mg to 10.0 mg; nimodipine, in the amount from 20.0 mg to 100.0
mg; potassium iodide, in the amount from 120.0 mg to 560.0 mg; potassium
iodate,
in the amount from. 30.0 mg to 140.0 mg; inuline, in the amount from 125.0 mg
to
375.0 mg; silver, in the amount from 0.10 mg to 0.50 mg; zinc, in the amount
from
is 10.0 mg to 20.0 mg; chromium, in the amount from 0.05 mg to 0.20 mg; orotic
acid, in the amount from 150.0 mg to 500.0 mg; desferrin, in the amount from
100.0 mg to 300.0 mg, until a mix approximating uniform substance is produced,
subsequently pressed into tablets, and can also have a form of coated tablets,
or can
be shaped into a wafer, a suppository, effervescent powder, gel, or colloid
solution;
2 0 or made into suspension, syrup, salt soluble in body fluids, or liquid for
intramuscular or I~ injections, also in ampules.
In the existing publications pertaining to treatment regimens for patients
with a diagnosed HIV infection, or with the Acquired Imrnunodeficiency
Syndrome
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(AIDS), there has been no description of any medications/ pharmaceutical
preparations for blocking the HIV-1 and HIV-2 virus replication in the CD4+
cells
of the human immune system based on the reasoning adopted here.
The premiss underlying the invention discussed here is the reasoning that
the basis for the HIV- I and HIV-2 virus replication in the CD4+ cells of the
human
immune system is the exeitono-excimeric correlation between the HIV- I and HIV-
2 viruses and the CD4 cell of the human immune system.
The effect of the adoption of that reasoning is as follows: the initiation of
the therapy aimed at treatment of the HIV-1 and HIV-2 viral infections, and
AIDS,
to is reduced to delivering substances completely blocking the mechanism
causing the
HIV-1 and HIV-2 replication to the patient's body.
The following substances proved to be helpful in that task: allocryptopine,
an alkaloid found in the Chelidonium maius plant, nimodipine, potassium
iodide,
potassium iodate, inuline, silver, zinc, chromium, orotic acid and desferrin.
Other
15 substances found to be helpful in this task were taraxasterol and B-
sitosterol.
It is known that: allocryptopine is a nucleotide phosphodiesterase blocker,
nimodipine is a calcium channel blocker, potassium iodide when combined with
potassium iodate in the acidic environment, produces iodic free radicals,
inuline is
a polysaccharide which is not decomposed in the body9 silver, zinc, and
chromium
~ o are elements playing a role in the enzymatic processes, - desferrin
chelates ferric
ions, - ~r~tic acid a the precursor of the nucleotide compounds.
However, the substances listed above have never appeared nor been applied
together, and in particular they have not been used together in the
therapeutic
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application such as those described in this invention.
The goal of the invention is supplying the pharmaceutical mixture for
blocking the HIV-1 and HIV-2 virus replication in the CD4+ cells of the human
immune system.
The invention provides that the pharmaceutical mixture for blocking the
HIV-1 and HIV2 virus replication in the CD4+ cells of the human immune system
in all stages of that viral infection, and in AIDS, contains previously known
carriers
and/or auxiliary substances, as well as active substances, and it is
characterized by
the presence of at least 10 chemical substances as active substances, among
them:
to - allocryptopine is present in the amount from 1.0 mg to 10.0 mg,
- nimodipine is present in the amount from 20.0 mg to 100.0 mg,
- potassium iodide is present in the amount from 120.0 mg to 560.0 mg,
- potassium iodate is present in the amount from 30.0 mg to 140.0 mg,
- inuline is present in the amount from 125.0 mg to 375.0 mg,
15 - silver is present in the amount from 0.10 mg to 0.50 mg,
- zinc is present in the amount from 10.0 mg to 20.0 mg, -
- chromium is present in the amount from 0.05 mg to 0.20 mg,
- orotic acid is present in the amount from 150.0 mg to 500.0 mg,
-desferrin is present in the amount from 100.0 mg to 300.0 mg
ao
It is beneficial v~hen:
- allocryptopine content is 10.0 mg,
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- and nimodipine content is 100.0 mg,
- and potassium iodide content is 560.0 mg,
- and potassium iodate content is 140.0 mg,
- and inuline content is 375.0 mg,
- and silver content is 0.50 mg,
- and zinc content is 20.0 mg,
- and chromium content is 0.20 mg,
and orotic acid content is 500.0 mg,
- and desferrin content is 300.0 mg.
It is beneficial when:
- allocryptopine content is 4.50 mg,
- and nimodipine content is 60.0 mg,
- and potassium iodide content is 340.0 mg,
i5 - and potassium iodate content is X5.0 mg,
- and inuline content is 250.0 mg,
- and silver content is 0.30 mg,
- and zinc content is 15.0 mg,
- and chromium content is 0.125 mg,
- and orotic acid content is 325.0 mg,
- and desferrin content is 200.0 mg.
It is beneficial when:
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- allocryptopine content is 4.50 mg,
- and nimodipine content is 60.0 mg,
- and potassium iodide content is 340.0 mg,
- and potassium iodate content is 85.0 mg,
- and inuline content is 250.0 mg,
- and silver content is 0.30 mg,
- and zinc content is 15.0 mg,
- and chromium content is 0.125 mg,
- and orotic acid content is 325.0 mg,
to - and desferrin content is 200.0 mg,
- and taraxasterol content is 350 mg,
- and B-sitosterol content is 400 mg,
It is beneficial when:
- allocryptopine content is 1.0 mg,
- and nimodipine content is 20.0 mg,
- and potassium iodide content is 120.0 mg,
- and potassium iodate content is 30.0 mg,
- and inulinc content is 125.0 mg,
~ o - and silver content is 0.10 mg,
- arid zinc content is 10.0 mg,
- and chromium content is 0.05 mg,
- and orotic acid content is 250.0 mg,
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- and desferrin content is 100.0 mg,
- and taraxasterol content is 250 mg,
- and B-sitosterol content is 300 mg
It is beneficial when:
- allocryptopine content is 1.0 mg,
- and nimodipine content is 20.0 mg,
- and potassium iodide content is 120.0 mg,
- and potassium iodate content is 30.0 mg,
to - and muline content is 125.0 mg,
- and silver content is 0.10 mg,
- and zinc content is 10.0 mg,
- and chromium content is 0.05 mg,
- and orotic acid content is 250.0 mg,
- and desferrin content is 100.0 mg.
It is beneficial when the weight ratio of allocryptopine to nimodipine to
potassium iodide to potassium iodate to inuline to silver to zinc to chromium
to
orotic acid to desferrin is generally maintained as
1:20:120:30:125:0.1:10:0.05:250:100.
~ o It is beneficial when the mixture of the ingredients has a form of a
tablet, or
coated tablet, or wafer, oi° suppository, or effervescent
powder°, or gel, or colloid
solution.
It is beneficial when the mixture of the ingredients has a form of
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suspension, or syrup, or salt soluble in body fluids, or liquids for
intramuscular or
IV injections.
The production of the pharmaceutical mixture for blocking the HIV-1 and
HIV-2 virus replication in the CD4+ cells of the human immune system in all
stages of that viral infection, and in AIDS, is characterized by mixing, in
the room
temperature, the following ingredients: - - allocryptopine in the amount from
1.0
~, mg to 10.0 mg,
- nimodipme in the amount from 20.0 mg to 100.0 mg,
- potassium iodide in the amount from 120.0 mg to 560.0 mg,
so - potassium iodatc in the amount from 30.0 mg to 140.0 mg,
- incline in the amount from 125.0 mg to 375.0 mg,
- silver in the amount from 0.10 mg to 0.50 mg,
- zinc in the amount from 10.0 mg to 20.0 mg,
- chromium in the amount from 0.05 mg to 0.20 mg,
- orotic acid in the amount from 150.0 mg to 500.0 mg,
-desferrin in the amount from 100.0 mg to 300.0 mg, until homogeneous mixture
is
created.
It is beneficial when:
2 0 - alloc~yptopine content is 10.0 mg,
- and nimodipinc content is 100.0 mg,
- and potassium iodide content is 560.0 mg,
- and potassium iodate content is 140.0 mg,
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- and inuline content is 375.0 mg,
- and silver content is 0.50 mg,
- and zinc content is 20.0 mg,
- and chromium content is 0.20 mg,
- and orotic acid content is 500.0 mg,
- and desferrin content is 300.0 mg.
It is beneficial when:
- allocryptopine content is 4.50 mg,
- and nimodipine content is 60.0 mg,
to - and potassium iodide content is 340.0 mg,
- and potassium iodate content is 85.0 mg,
- and inuline content is 250.0 mg,
- and silver content is 0.30 mg,
- and zinc content is 15.0 mg,
- and chromium content is 0.125 mg,
- and orotic acid content is 325.0 mg,
- and desferrin content is 200.0 mg.
It is beneficial when:
- allocryptopine content is 1.0 mg,
z o - and nimodipine content is 20.0 zng,
- and potassium iodide content is 120.0 mg,
- and potassium iodate content is 30.0 mg,
- and inuline content is 125.0 mg,
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- and silver content is 0.10 mg,
- and zinc content is 10.0 mg,
- and chromium content is 0.05 mg,
- and orotic acid content is 250.0 mg,
- and desferrin content is 100.0 mg.
It is beneficial when the weight ratio of allocryptopine to nimodipme to
potassium iodide to potassium iodate to inuline to silver to zinc to chromium
to
orotic acid to desferrin is generally maintain as
1:20:120:30:125:0.1:10:0.05:250:100.
to The pharmaceutical mixture and method of making it may further comprise
pharmaceutically effective amounts of taraxasterol and B-sitosterol. It is
beneficial
when the pharmaceutical mixture and method of making it is characterized by
mixing, in the room temperature, of allocryptopine, in the amount from 1.0 mg
to
10.0 mg; nimodipine, in the amount from 20.0 mg to 100.0 mg; potassium iodide,
in the amount from 120.0 mg to 560.0 mg; potassium iodate, in the amount from
30.0 mg to 140.0 mg; inuline, in the amount from 125.0 mg to 375.0 mg; silver,
in
the amount from 0.10 mg to 0.50 mg; zinc, in the amount from 10.0 mg to 20.0
mg; chromium, in the amount from 0.05 mg to 0.20 mg; orotic acid, in the
amount
from 150.0 mg to 500.0 mg; desferrin, in the amount from 100.0 mg to 300.0 mg;
2o taraxasterol, in the amount from 250-400 mg, and 13-sitosterol in the
amount from
300-500 mg until a mix approximating uniform substance is produced,
subsequently pressed into tablets9 and can also have a form of coated tablets,
or can
be shaped into a wafer, a suppository, effervescent powder, gel, or colloid
solution;
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or made into suspension, syrup, salt soluble in body fluids, or liquid for
intramuscular or IV injections, also in ampules.
It is beneficial when the weight ratio of allocryptopine to nimodipine to
potassium iodide to potassium iodate to inuline to silver to zinc to chromium
to
orotic acid to desferrin to taraxasterol to B-sitosterol is generally maintain
as
1:20:120:30:125:0.1:10:0.05:250:100:400:500.
It is also beneficial when the weight ratio of allocryptopine to nimodipine to
potassium iodide to potassium iodate to inuline to silver to zinc to chromium
to
orotic acid to desferrin to taraxasterol to B-sitosterol is generally maintain
as
l0 1:20:120:30:125:0.1:10:0.05:250:100:350:400.
It is beneficial when the mixture of the ingredients has a form of a tablet,
or
coated tablet, or wafer, or suppository, or effervescent powder, or gel, or a
colloid
solution.
It is beneficial when the mixture of the ingredients has a form of
15 suspension, or syrup, or salt soluble in body fluids, or liquids for
intramuscular or
IV injections.
The beneficial effect of the pharmaceutical mixture in the invention is
blocking the mechanism of attaching the gp 160 protein of the HIV virus
capsule to
the receptors of the CI24+ cells of the human immune system, as well as
blocking
2o the intracellular processes related to the HIV-1 and HIV-2 virus
replication.
E~~aaxaple l~To. 1. Content of the pharmaceutical mixture:
- allocryptopine in the amount of 10.0 mg,
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- nimodipine in the amount of 100.0 mg,
- potassium iodide in the amount of 560.0 mg,
- potassium iodate in the amount of 140.0 mg,
- inuline in the amount of 375.0 mg,
- silver in the amount of 0.50 mg,
- zinc in the amount of 20.0 mg,
- chromium in the amount of 0.20 mg,
- orotic acid in the amount of 500.0 mg,
- desferrin in the amount of 300.0 mg.
to Production of the pharmaceutical mixture:
Mix together in the room temperature: 10.0 mg of allocryptopine, 100.0 mg
of nimodipine, 560.0 mg of potassium iodide, 140:0 mg of potassium iodate,
375.0
mg of inuline, 0.50 mg of silver, 20.0 mg of zinc, 0.20 mg of chromium, 500.0
mg
of orotic acid, and 300.0 mg of desferrin.
After adding all ingredients, mix them all together for about 10-20 minutes
until a uniform substance is produced. The mix can then be pressed into
tablets,
and can also have a form of coated tablets, or can be shaped into a wafer, a
suppository, effervescent powder, gel, or colloid solution.
2 0 ~:~a~mpl~ I'~T~. 2. Content of the pharmaceutical mixture:
- allocryptopine in the amount of 1.0 mg,
- nimodipine in the amount of 20.0 mg,
- potassium iodide in the amount of 120.0 mg,
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- potassium iodate in the amount of 30.0 mg,
- mulme in the amount of 125.0 mg,
- silver in the amount of 0.10 mg,
- zinc in the amount of 10.0 mg,
- chromium in the amount of 0.05 mg,
- orotic acid in the amount of 150.0 mg,
- desferrin in the amount of 100.0 mg.
Production of the pharmaceutical mixture:
IvIix together in the room temperature: 1.0 mg of allocryptopine, 20.0 mg of
1 o nimodipinc, 120.0 mg of potassium iodide, 30.0 mg of potassium iodatc,
125.0 mg
of inuline, 0. I O mg of silver, 10.0 mg of zinc, 0.05 mg of chromium, 150.0
mg of
orotic acid, and 100.0 mg of desferrin.
After adding all ingredients, mix them all together for about 10-20 minutes
until a uniform substance is produced.
The product can then be made into suspension, syrup, salt soluble in body
fluids, or liquid fox intramuscular or TV injections, also in ampules.
Exaruple IV~. 3. Content of the pharmaceutical mixture:
- allocryptopine in the amount of 10.0 mg,
2 0 - nimodipine in the amount of 100.0 mg,
- potassium iodide in the amount of 560.0 mg,
- potassium iodate in the amount of 140.0 mg,
- inulinc in the amount of 375.0 mg,
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- silver in the amount of 0.50 mg,
- zinc in the amount of 20.0 mg,
- chromium in the amount of 0.20 mg,
- orotic acid in the amount of 500.0 mg,
- desferrin in the amount of 300.0 mg,
- taraxasterol in the amount of 400 mg,
- B-sitosterol in the amount of 500 mg.
production of the pharmaceutical mixture:
Mix together in the room temperature: I0.0 mg of allocryptopine, 100.0 mg
so of nimodipine, 560.0 mg of potassium iodide, 140.0 mg of potassium iodate,
375.0
mg of inuline, 0.50 mg of silver, 20.0 mg of zinc, 0.20 mg of chromium, 500.0
mg
of orotic acid, 300.0 mg of desferrin, 400 mg of taraxasterol, and 500mg. of B-
sitosterol.
After adding all ingredients, mix them all together for about 10-20 minutes
until a uniform substance is produced. The mix can then be pressed into
tablets,
and can also have a form of coated tablets, or can be shaped into a wafer, a
suppository, effervescent powder, gel, or colloid solution.
E~saxrapl~ N~. 4. Content of the pharmaceutical mixture:
- allocryptopine in the amount of 1.0 mg,
- nimodipine in the amount of 20.0 mg,
- potassium iodide in the amount of 120.0 mg,
- potassium iodate in the amount of 30.0 mg,
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- mulme in the amount of 125.0 mg,
- silver in the amount of 0.10 mg,
- zinc in the amount of 10.0 mg,
- chromium in the amount of O.OS mg,
- orotic acid in the amount of 150.0 mg,
- desferrin in the amount of 100.0 mg,
- taraxasterol in the amount of 2S0 mg,
- B-sitosterol in the amount of 300 mg.
1 o Production of the pharmaceutical mixture:
Mix together in the room temperature: 1.0 mg of allocryptopine, 20.0 mg of
nimodipine, 120.0 mg of potassium iodide, 30.0 mg of potassium iodate, 125.0
mg
of inuline, 0.10 mg of silver, 10.0 mg of zinc, O.OS mg of chromium, I 50.0 mg
of
orotic acid, 100.0 mg of desferrin, 250 mg of taraxasterol, and 300mg. of B-
i5 sitosterol.
After adding all ingredients, mix them all together for about 10-20 minutes
until a uniform substance is produced.
The product can then be made into suspension, syrup, salt soluble in body
fluids, or liquid for intramuscular or IV injections, also in ampules.
~ o It should be understood that the term 'Gpharmaceutically effective amount"
means an effective amount of the pharmaceutical mixture of the present
invention
(comprising a mixture of allocryptopine, nimodipine, potassium iodide,
potassium
iodate, inuline, silver, zinc, chromium, orotic acid and desferrin). Actual
dosage
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levels of the pharmaceutical composition of this invention can be varied so as
to
achieve the desired therapeutic response for a particular patient,
compositions and
mode of administration. The selected dosage level will depend upon the
activity of
the particular compound, the route of administration, the severity of the
condition
being treated and the condition and prior medical history of the patient being
treated. However, it is within the skill of the art to start doses of the
compound at
levels lower than required to achieve the desired therapeutic effect and to
gradually
increase the dosage until the desired effect is achieved.
