ZA200505977B - A therapeutic compsotion for the treatment of HIV-1 and HIV-2 - Google Patents
A therapeutic compsotion for the treatment of HIV-1 and HIV-2 Download PDFInfo
- Publication number
- ZA200505977B ZA200505977B ZA200505977A ZA200505977A ZA200505977B ZA 200505977 B ZA200505977 B ZA 200505977B ZA 200505977 A ZA200505977 A ZA 200505977A ZA 200505977 A ZA200505977 A ZA 200505977A ZA 200505977 B ZA200505977 B ZA 200505977B
- Authority
- ZA
- South Africa
- Prior art keywords
- amount
- present
- allocryptopine
- nimodipine
- desferrin
- Prior art date
Links
- 241000713772 Human immunodeficiency virus 1 Species 0.000 title claims description 20
- 241000713340 Human immunodeficiency virus 2 Species 0.000 title claims description 19
- 230000001225 therapeutic effect Effects 0.000 title claims description 19
- 238000011282 treatment Methods 0.000 title claims description 15
- 208000031886 HIV Infections Diseases 0.000 title claims description 10
- NLKNQRATVPKPDG-UHFFFAOYSA-M potassium iodide Chemical compound [K+].[I-] NLKNQRATVPKPDG-UHFFFAOYSA-M 0.000 claims description 93
- PXQPEWDEAKTCGB-UHFFFAOYSA-N orotic acid Chemical compound OC(=O)C1=CC(=O)NC(=O)N1 PXQPEWDEAKTCGB-UHFFFAOYSA-N 0.000 claims description 62
- 239000000203 mixture Substances 0.000 claims description 44
- NGFLTEGALWMQIJ-UHFFFAOYSA-N allocryptopine Natural products COc1ccc2CC(=O)c3cc4OCOc4cc3CN(C)CCc2c1OC NGFLTEGALWMQIJ-UHFFFAOYSA-N 0.000 claims description 32
- HUIJAZQRYSCNED-UHFFFAOYSA-N alpha-allo-cryptopine Natural products C1CN(C)CC2=C(OC)C(OC)=CC=C2CC(=O)C2=CC(OC)=C(OC)C=C21 HUIJAZQRYSCNED-UHFFFAOYSA-N 0.000 claims description 32
- 229910052804 chromium Inorganic materials 0.000 claims description 32
- 239000011651 chromium Substances 0.000 claims description 32
- 229960000715 nimodipine Drugs 0.000 claims description 32
- 229960005010 orotic acid Drugs 0.000 claims description 32
- 239000011701 zinc Substances 0.000 claims description 32
- 229910052725 zinc Inorganic materials 0.000 claims description 32
- UIAGMCDKSXEBJQ-IBGZPJMESA-N 3-o-(2-methoxyethyl) 5-o-propan-2-yl (4s)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate Chemical compound COCCOC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)C)[C@H]1C1=CC=CC([N+]([O-])=O)=C1 UIAGMCDKSXEBJQ-IBGZPJMESA-N 0.000 claims description 31
- VYZAMTAEIAYCRO-UHFFFAOYSA-N Chromium Chemical compound [Cr] VYZAMTAEIAYCRO-UHFFFAOYSA-N 0.000 claims description 31
- UXOXDDUEWZOAIW-UHFFFAOYSA-N Inuline Natural products CCN1CC2(CC(=O)Oc3ccccc3N)CCC(OC)C45C6CC7C(CC(O)(C6C7OC)C(O)(C(OC)C24)C15)OC UXOXDDUEWZOAIW-UHFFFAOYSA-N 0.000 claims description 31
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 claims description 31
- VNRZCPPHNPEBFC-UHFFFAOYSA-N anthranoyllycoctonine Natural products CCN1CC2(COC(=O)c3ccccc3N)CCC(OC)C45C2C(OC)C(O)(C14)C6(O)CC(OC)C7CC5(O)C6C7OC VNRZCPPHNPEBFC-UHFFFAOYSA-N 0.000 claims description 31
- 239000001230 potassium iodate Substances 0.000 claims description 31
- 229940093930 potassium iodate Drugs 0.000 claims description 31
- 235000006666 potassium iodate Nutrition 0.000 claims description 31
- 229910052709 silver Inorganic materials 0.000 claims description 31
- 239000004332 silver Substances 0.000 claims description 31
- NNDHDYDFEDRMGH-CAEIVAEBSA-N Anthranoyllycoctonine Chemical compound C([C@]12CN(C3[C@@]4(O)[C@]5(O)[C@H]6[C@@H](OC)[C@@H]([C@H](C5)OC)C[C@H]6[C@@]3([C@@H]1[C@@H]4OC)[C@@H](OC)CC2)CC)OC(=O)C1=CC=CC=C1N NNDHDYDFEDRMGH-CAEIVAEBSA-N 0.000 claims description 30
- BQCADISMDOOEFD-UHFFFAOYSA-N Silver Chemical compound [Ag] BQCADISMDOOEFD-UHFFFAOYSA-N 0.000 claims description 30
- JLKDVMWYMMLWTI-UHFFFAOYSA-M potassium iodate Chemical compound [K+].[O-]I(=O)=O JLKDVMWYMMLWTI-UHFFFAOYSA-M 0.000 claims description 30
- UBQYURCVBFRUQT-UHFFFAOYSA-N N-benzoyl-Ferrioxamine B Chemical compound CC(=O)N(O)CCCCCNC(=O)CCC(=O)N(O)CCCCCNC(=O)CCC(=O)N(O)CCCCCN UBQYURCVBFRUQT-UHFFFAOYSA-N 0.000 claims description 29
- HYBRYAPKQCZIAE-UHFFFAOYSA-N allocryptopine Chemical compound C1=C2CCN(C)CC3=C(OC)C(OC)=CC=C3CC(=O)C2=CC2=C1OCO2 HYBRYAPKQCZIAE-UHFFFAOYSA-N 0.000 claims description 27
- 238000000034 method Methods 0.000 claims description 27
- 230000000903 blocking effect Effects 0.000 claims description 17
- 230000029812 viral genome replication Effects 0.000 claims description 17
- XWMMEBCFHUKHEX-MRTCRTFGSA-N (+)-Taraxasterol Chemical compound C([C@@]12C)C[C@H](O)C(C)(C)[C@@H]1CC[C@]1(C)[C@@H]2CC[C@H]2[C@@H]3[C@H](C)C(=C)CC[C@]3(C)CC[C@]21C XWMMEBCFHUKHEX-MRTCRTFGSA-N 0.000 claims description 12
- QMKPCZNFLUQTJZ-UHFFFAOYSA-N (4aR)-10c-Hydroxy-1t.2c.4ar.6at.6bc.9.9.12ac-octamethyl-(8atH.12btH.14acH.14btH)-docosahydro-picen Natural products CC1CCC2(C)CCC3(C)C(CCC4C5(C)CCC(O)C(C)(C)C5CCC34C)C2C1C QMKPCZNFLUQTJZ-UHFFFAOYSA-N 0.000 claims description 12
- NGFFRJBGMSPDMS-UHFFFAOYSA-N psi-Taraxasterol Natural products CC12CCC(O)C(C)(C)C1CCC1(C)C2CCC2C3C(C)C(C)=CCC3(C)CCC21C NGFFRJBGMSPDMS-UHFFFAOYSA-N 0.000 claims description 12
- HUTYZQWCTWWXND-NCTFTGAASA-N taraxasterol Natural products C[C@H]1[C@H]2C3=CC[C@@H]4[C@@]5(C)CC[C@H](O)C(C)(C)[C@@H]5CC[C@@]4(C)[C@]3(C)C[C@H](O)[C@@]2(C)CCC1=C HUTYZQWCTWWXND-NCTFTGAASA-N 0.000 claims description 12
- KZJWDPNRJALLNS-VJSFXXLFSA-N sitosterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CC[C@@H](CC)C(C)C)[C@@]1(C)CC2 KZJWDPNRJALLNS-VJSFXXLFSA-N 0.000 claims description 11
- 241000725303 Human immunodeficiency virus Species 0.000 claims description 10
- 229960004839 potassium iodide Drugs 0.000 claims description 8
- 239000000084 colloidal system Substances 0.000 claims description 4
- 239000007911 effervescent powder Substances 0.000 claims description 4
- 239000000499 gel Substances 0.000 claims description 4
- 239000000829 suppository Substances 0.000 claims description 4
- 208000037357 HIV infectious disease Diseases 0.000 claims description 3
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims description 3
- 239000000725 suspension Substances 0.000 claims description 2
- 238000010253 intravenous injection Methods 0.000 claims 2
- KZJWDPNRJALLNS-VPUBHVLGSA-N (-)-beta-Sitosterol Natural products O[C@@H]1CC=2[C@@](C)([C@@H]3[C@H]([C@H]4[C@@](C)([C@H]([C@H](CC[C@@H](C(C)C)CC)C)CC4)CC3)CC=2)CC1 KZJWDPNRJALLNS-VPUBHVLGSA-N 0.000 claims 1
- CSVWWLUMXNHWSU-UHFFFAOYSA-N (22E)-(24xi)-24-ethyl-5alpha-cholest-22-en-3beta-ol Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(C)C=CC(CC)C(C)C)C1(C)CC2 CSVWWLUMXNHWSU-UHFFFAOYSA-N 0.000 claims 1
- KLEXDBGYSOIREE-UHFFFAOYSA-N 24xi-n-propylcholesterol Natural products C1C=C2CC(O)CCC2(C)C2C1C1CCC(C(C)CCC(CCC)C(C)C)C1(C)CC2 KLEXDBGYSOIREE-UHFFFAOYSA-N 0.000 claims 1
- LPZCCMIISIBREI-MTFRKTCUSA-N Citrostadienol Natural products CC=C(CC[C@@H](C)[C@H]1CC[C@H]2C3=CC[C@H]4[C@H](C)[C@@H](O)CC[C@]4(C)[C@H]3CC[C@]12C)C(C)C LPZCCMIISIBREI-MTFRKTCUSA-N 0.000 claims 1
- ARVGMISWLZPBCH-UHFFFAOYSA-N Dehydro-beta-sitosterol Natural products C1C(O)CCC2(C)C(CCC3(C(C(C)CCC(CC)C(C)C)CCC33)C)C3=CC=C21 ARVGMISWLZPBCH-UHFFFAOYSA-N 0.000 claims 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims 1
- MJVXAPPOFPTTCA-UHFFFAOYSA-N beta-Sistosterol Natural products CCC(CCC(C)C1CCC2C3CC=C4C(C)C(O)CCC4(C)C3CCC12C)C(C)C MJVXAPPOFPTTCA-UHFFFAOYSA-N 0.000 claims 1
- LGJMUZUPVCAVPU-UHFFFAOYSA-N beta-Sitostanol Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(C)CCC(CC)C(C)C)C1(C)CC2 LGJMUZUPVCAVPU-UHFFFAOYSA-N 0.000 claims 1
- NJKOMDUNNDKEAI-UHFFFAOYSA-N beta-sitosterol Natural products CCC(CCC(C)C1CCC2(C)C3CC=C4CC(O)CCC4C3CCC12C)C(C)C NJKOMDUNNDKEAI-UHFFFAOYSA-N 0.000 claims 1
- 229910052700 potassium Inorganic materials 0.000 claims 1
- 239000011591 potassium Substances 0.000 claims 1
- 229950005143 sitosterol Drugs 0.000 claims 1
- NLQLSVXGSXCXFE-UHFFFAOYSA-N sitosterol Natural products CC=C(/CCC(C)C1CC2C3=CCC4C(C)C(O)CCC4(C)C3CCC2(C)C1)C(C)C NLQLSVXGSXCXFE-UHFFFAOYSA-N 0.000 claims 1
- 235000015500 sitosterol Nutrition 0.000 claims 1
- 208000030507 AIDS Diseases 0.000 description 13
- 210000000987 immune system Anatomy 0.000 description 12
- 208000036142 Viral infection Diseases 0.000 description 9
- 239000000126 substance Substances 0.000 description 9
- 230000009385 viral infection Effects 0.000 description 9
- 239000013543 active substance Substances 0.000 description 4
- 230000009286 beneficial effect Effects 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 4
- 239000000969 carrier Substances 0.000 description 2
- 125000003729 nucleotide group Chemical group 0.000 description 2
- 229940127291 Calcium channel antagonist Drugs 0.000 description 1
- 241001017738 Chelidonium <beetle> Species 0.000 description 1
- VTLYFUHAOXGGBS-UHFFFAOYSA-N Fe3+ Chemical compound [Fe+3] VTLYFUHAOXGGBS-UHFFFAOYSA-N 0.000 description 1
- 102000004861 Phosphoric Diester Hydrolases Human genes 0.000 description 1
- 108090001050 Phosphoric Diester Hydrolases Proteins 0.000 description 1
- 241000700605 Viruses Species 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 229930013930 alkaloid Natural products 0.000 description 1
- 150000003797 alkaloid derivatives Chemical class 0.000 description 1
- 239000003708 ampul Substances 0.000 description 1
- 210000001124 body fluid Anatomy 0.000 description 1
- 239000010839 body fluid Substances 0.000 description 1
- 239000000480 calcium channel blocker Substances 0.000 description 1
- 210000004970 cd4 cell Anatomy 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000002255 enzymatic effect Effects 0.000 description 1
- 229910001447 ferric ion Inorganic materials 0.000 description 1
- 150000004676 glycans Chemical class 0.000 description 1
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000000977 initiatory effect Effects 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 238000002483 medication Methods 0.000 description 1
- 239000002773 nucleotide Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 230000010076 replication Effects 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 238000011269 treatment regimen Methods 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/24—Heavy metals; Compounds thereof
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
-
- 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
- A61K31/33—Heterocyclic compounds
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/14—Alkali metal chlorides; Alkaline earth metal chlorides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/16—Fluorine compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/18—Iodine; Compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/24—Heavy metals; Compounds thereof
- A61K33/30—Zinc; Compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/24—Heavy metals; Compounds thereof
- A61K33/38—Silver; Compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Inorganic Chemistry (AREA)
- Molecular Biology (AREA)
- Virology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Description
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 2003.
A pharmaceutical mixture for blocking the HIV-1 and/or HIV-2 virus replication in the CD4+ 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+ 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 “treatment of HIV in a patient in need of such treatment” mean treating a patient with HIV-1 and/or HIV-2. Additionally, the term “blocking HIV virus replication” means blocking HIV-1 and/or HIV-2 virus replication. Further the term “HIV virus” refers to the HIV-1 and/or HIV-2 virus. Still further, the term “H]V infection” refers to HIV-1 and/or HIV-2 infection.
The subject of the invention is a 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, also the method of 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, 2 25 and in AIDS.
The invented mixture has a particular application in treatment of the
Acquired Immunodeficiency Syndrome, or AIDS. : Synopsis of the Description
The subject of the invention is a pharmaceutical mixture for blocking the
HIV-1 and HIV-2 virus replication in the CD4+ cells of the human immune system in 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, allocryptopine, present in the amount from 1.0 mg to 10.0 mg; nimodipine, present 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
A pharmaceutical mixture and a method of its production of a therapeutic composition 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 for the treatment of HIV in a patient in need of such treatment, the therapeutic composition comprising of pharmaceutically effective amounts of allocryptopine,
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.
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
CD4+ cells of the human immune system in all stages of that viral infection, and in
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 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; or made into suspension, syrup, salt soluble in body fluids, or liquid for intramuscular or IV injections, also in ampules. . In the existing publications pertaining to treatment regimens for patients with a diagnosed HIV infection, or with the Acquired Immunodeficiency Syndrome
(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, 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 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 body; silver, zinc, and chromium are elements playing a role in the enzymatic processes, - desferrin chelates ferric ions, - orotic 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 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 HIV? 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: - 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, - patassium 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, - 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 . It is beneficial when: - allocryptopine content is 10.0 mg,
- 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, - 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:
-7 = - 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, - 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 inuline 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,
Claims (31)
1. A therapeutic composition for the treatment of HIV in a patient in - need of such treatment, the therapeutic composition comprising of pharmaceutically effective amounts of allocryptopine, nimodipine, potassium iodide, potassium iodate, inuline, silver, zinc, chromium, orotic acid and desferrin.
2. The therapeutic composition of claim 1, wherein the allocryptopine is present in the amount from about 1.0 mg to about 10.0 mg, nimodipine is present in the amount from about 20.0 mg to about 100.0 mg, potassium iodide is present in the amount from about 120.0 mg to about 560.0 mg, potassium iodate is present in the amount from about 30.0 mg to about 140.0 mg, inuline is present in the amount from about 125.0 mg to about 375.0 mg, silver is present in the amount from about 0.10 mg to about 0.50 mg, zinc, present in the amount from 10.0 mg to about 20.0 mg, chromium is present in the amount from about 0.05 mg to about
0.20 mg, orotic acid is present in the amount from about 150.0 mg to about 500.0 mg, and the desferrin is present in the amount from about 100.0 mg to about 300.0 mg.
3. The therapeutic composition of claim 1, wherein the allocryptopine is present in the amount of about 10.0 mg, the nimodipine is present in the amount of about 100.0 mg, the potassium iodide is present in the amount of about 560.0 mg, the potassium iodate is present in the amount of about 140.0 mg, the inuline is present in the amount of about 375.0 mg, the silver is present in the amount of about 0.50 mg, the zinc is present in the amount of about 20.0 mg, the chromium is present in the amount of about 0.20 mg, the orotic acid is present in the amount of about 500.0 mg, and the desferrin is present in the amount of about 300.0 mg.
4. The therapeutic composition of claim I, wherein the allocryptopine is present in the amount of about 4.5 mg, the nimodipine is present in the amount of about 60.0 mg, the potassium iodide is present in the amount of about 340.0 mg, the potassium iodate is present in the amount of about 85.0 mg, the inuline is present in the amount of about 250.0 mg, the silver is present in the amount of about 0.30 mg, the zinc is present in the amount of about 15.0 mg, the chromium is present in the amount of about 0.125 mg, the orotic acid is present in the amount of about 325.0 mg, and the desferrin is present in the amount of about 200.0 mg.
5. The therapeutic composition of claim 1, wherein the allocryptopine is present in the amount of about 1.0 mg, the nimodipine is present in the amount of about 20.0 mg, the potassium iodide is present in the amount of about 120.0 mg, the potassium iodate is present in the amount of about 30.0 mg, the inuline is present in the amount of about 125.0 mg, the silver is present in the amount of about 0.10 mg, the zinc is present in the amount of about 10.0 mg, the chromium is present in the amount of about 0.05 mg, the orotic acid is present in the amount of - about 250.0 mg, and the desferrin is present in the amount of about 100.0 mg.
6. The therapeutic composition of claim 1 further comprises a 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 of about . 1:20:120:30:125:0.1:10:0.05:250:100, respectively.
7. The therapeutic composition of claim 1, wherein said composition is in a form suitable for administering to a patient, wherein the form is selected from the group consisting of a tablet, coated tablet, wafer, suppository, effervescent powder, gel, and a colloid suspension.
8. A therapeutic composition for the treatment of HIV in a patient in need of such treatment, the therapeutic composition comprising of pharmaceutically effective amounts of allocryptopine, nimodipine, potassium iodide, potassium iodate, inuline, silver, zinc, chromium, orotic acid, desferrin, taraxasterol and B-sitosterol.
9. The therapeutic composition of claim 8, wherein the allocryptopine is present in the amount from about 1.0 mg to about 10.0 mg, nimodipine is present in the amount from about 20.0 mg to about 100.0 mg, potassium iodide is present in the amount from about 120.0 mg to about 560.0 mg, potassium iodate is present in the amount from about 30.0 mg to about 140.0 mg, inuline is present in the amount from about 125.0 mg to about 375.0 mg, silver is present in the amount from about 0.10 mg to about 0.50 mg, zinc, present in the amount from 10.0 mg to about 20.0 mg, chromium is present in the amount from about 0.05 mg to about
0.20 mg, orotic acid is present in the amount from about 150.0 mg to about 500.0 mg, the desferrin is present in the amount from about 100.0 mg to about 300.0 mg, : the taraxasterol is present in the amount from about 250mg to about 400 mg, and the B-sitosterol is present in the amount from about 300 mg to about 500 mg.
10. The therapeutic composition of claim 8, wherein the allocryptopine is present in the amount of about 10.0 mg, the nimodipine is present in the amount of about 100.0 mg, the potassium iodide is present in the amount of about 560.0 mg, the potassium iodate is present in the amount of about 140.0 mg, the inuline is present in the amount of about 375.0 mg, the silver is present in the amount of about 0.50 mg, the zinc is present in the amount of about 20.0 mg, the chromium is present in the amount of about 0.20 mg, the orotic acid is present in the amount of about 500.0 mg, the desferrin is present in the amount of about 300.0 mg, the taraxasterol is present in the amount of about 400 mg, and the B-sitosterol is present in the amount of about 500 mg.
11 The therapeutic composition of claim 8, wherein the allocryptopine is present in the amount of about 4.5 mg, the nimodipine is present in the amount of about 60.0 mg, the potassium iodide is present in the amount of about 340.0 mg, the potassium iodate is present in the amount of about 85.0 mg, the inuline is present in the amount of about 250.0 mg, the silver is present in the amount of . about 0.30 mg, the zinc is present in the amount of about 15.0 mg, the chromium is present in the amount of about 0.125 mg, the orotic acid is present in the amount of about 325.0 mg, the desferrin is present in the amount of about 200.0 mg, the taraxasterol is present in the amount of about 350 mg, and the B-sitosterol is ’ present in the amount of about 400 mg.
12. The therapeutic composition of claim 8, wherein the allocryptopine is present in the amount of about 1.0 mg, the nimodipine is present in the amount of about 20.0 mg, the potassium iodide is present in the amount of about 120.0 mg, the potassium iodate is present in the amount of about 30.0 mg, the inuline is present in the amount of about 125.0 mg, the siiver is present in the amount of about 0.10 mg, the zinc is present in the amount of about 10.0 mg, the chromium is present in the amount of about 0.05 mg, the orotic acid is present in the amount of about 250.0 mg, the desferrin is present in the amount of about 100.0 mg, the taraxasterol is present in the amount of about 250 mg, and the B-sitosterol is present in the amount of about 300 mg.
13. A method of preparing a pharmaceutical mixture for blocking HIV virus replication, comprising the step of mixing together pharmaceutically effective amounts of allocryptopine, nimodipine, potassium iodide, potassium iodate, inuline, silver, zinc, chromium, orotic acid, and desferrin to provide the pharmaceutical mixture for blocking HIV-1 and HIV-2 virus replication.
14. The method of claim 13, wherein the step of mixing is performed at room temperature.
15. The method of claim 13, wherein the allocryptopine is present in the amount from about 1.0 mg to about 10.0 mg, nimodipine is present in the amount ) from about 20.0 mg to about 100.0 mg, potassium iodide is present in the amount . from about 120.0 mg to about 560.0 mg, potassium iodate is present in the amount from about 30.0 mg to about 140.0 mg, inuline is present in the amount from about
125.0 mg to about 375.0 mg, silver is present in the amount from about 0.10 mg to about 0.50 mg, zinc, present in the amount from 10.0 mg to about 20.0 mg, chromium is present in the amount from about 0.05 mg to about 0.20 mg, orotic acid is present in the amount from about 150.0 mg to about 500.0 mg, and the desferrin is present in the amount from about 100.0 mg to about 300.0 mg.
16. The method of claim 13, wherein the allocryptopine is present in the amount of about 10.0 mg, the nimodipine is present in the amount of about 100.0 mg, the potassium iodide is present in the amount of about 560.0 mg, the potassium iodate is present in the amount of about 140.0 mg, the inuline is present in the amount of about 375.0 mg, the silver is present in the amount of about 0.50 mg, the zinc is present in the amount of about 20.0 mg, the chromium is present in the amount of about 0.20 mg, the orotic acid is present in the amount of about
500.0 mg, and the desferrin is present in the amount of about 300.0 mg.
17. The method of claim 13, wherein the allocryptopine is present in the . amount of about 4.5 mg, the nimodipine is present in the amount of about 60.0 mg, the potassium iodide is present in the amount of about 340.0 mg, the potassium iodate is present in the amount of about 85.0 mg, the inuline is present in the amount of about 250.0 mg, the silver is present in the amount of about 0.30 mg, the zinc is present in the amount of about 15.0 mg, the chromium is present in the . amount of about 0.125 mg, the orotic acid is present in the amount of about 325.0 mg, and the desferrin is present in the amount of about 200.0 mg.
18. The method of claim 13, wherein the allocryptopine is present in the amount of about 1.0 mg, the nimodipine is present in the amount of about 20.0 mg, the potassium iodide is present in the amount of about 120.0 mg, the potassium iodate is present in the amount of about 30.0 mg, the inuline is present in the amount of about 125.0 mg, the silver is present in the amount of about 0.10 mg, the zinc is present in the amount of about 10.0 mg, the chromium is present in the amount of about 0.05 mg, the orotic acid is present in the amount of about 250.0 - mg, and the desferrin is present in the amount of about 100.0 mg.
19. The method of claim 13, wherein the pharmaceutical mixture comprises a 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 of about 1:20:120:30:125:0.1:10:0.05:250: 100, respectively.
20. The method of claim 13 further comprising converting the . pharmaceutical mixture into a form suitable for administering to a patient, wherein the form is selected from the group consisting of a tablet, coated tablet, wafer,
suppository, effervescent powder, gel, and a colloid.
21. A method of treating a HIV infection, the method comprising administering to a patient in need of such treatment a pharmaceutical mixture comprising of pharmaceutically effective amounts of allocryptopine, nimodipine, potassium iodide, potassium iodate, inuline, silver, zinc, chromium, orotic acid and desferrin.
22. The method of claim 21, wherein the pharmaceutical mixture is administered intramuscularly.
23. The method of claim 21, wherein the pharmaceutical mixture is administered by intravenous injection.
24. A method of preparing a pharmaceutical mixture for blocking HIV virus replication, comprising the step of mixing together pharmaceutically effective amounts of allocryptopine, nimodipine, potassium iodide, potassium iodate, inuline, silver, zinc, chromium, orotic acid, desferrin, taraxasterol, and B-sitosterol to provide the pharmaceutical mixture for blocking HIV-1 and HIV-2 virus replication.
25. The method of claim 24, wherein the step of mixing is performed at room temperature.
26. The method of claim 24, wherein the allocryptopine is present in the amount from about 1.0 mg to about 10.0 mg, nimodipine is present in the amount from about 20.0 mg to about 100.0 mg, potassium iodide is present in the amount from about 120.0 mg to about 560.0 mg, potassium iodate is present in the amount from about 30.0 mg to about 140.0 mg, inuline is present in the amount from about 125.0 mg to about 375.0 mg, silver is present in the amount from about 0.10 mg to about
0.50 mg, zinc, present in the amount from 10.0 mg to about 20.0 mg, chromium is present in the amount from about 0.05 mg to about 0.20 mg, orotic acid is present in the amount from about 150.0 mg to about 500.0 mg, the desferrin is present in the amount from about 100.0 mg to about 300.0 mg, the taraxasterol is present in the amount from about 250mg to about 400 mg, and the B-sitosterol is present in the amount from about 300 mg to about 500 mg.
27. The method of claim 24, wherein the pharmaceutical mixture comprises a weight ratio of allocryptopine to nimodipine to potassium iodide to potassium jodate to inuline to silver to zinc to chromium to orotic acid to desferrin to taraxasterol to B- sitosterol of about 1:20:120:30:125:0.1:10:0.05:250:100:250:300, respectively.
28. The method of claim 24 further comprising converting the pharmaceutical mixture into a form suitable for administering to a patient, wherein the form is selected from the group consisting of a tablet, coated tablet, wafer, ] suppository, effervescent powder, gel, and a colloid.
29. A method of treating a HIV infection, the method comprising administering to a patient in need of such treatment a pharmaceutical mixture comprising of pharmaceutically effective amounts of allocryptopine, nimodipine, potassium iodide, potassium iodate, inuline, silver, zinc, chromium, orotic acid, desferrin, taraxasterol, and B-sitosterol.
30. The method of claim 29, wherein the pharmaceutical mixture is administered intramuscularly.
31. The method of claim 29, wherein the pharmaceutical mixture is administered by intravenous injection.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US10/353,483 US20030203045A1 (en) | 2002-04-30 | 2003-01-29 | Therapeutic composition for the treatment of HIV-1 and HIV-2 |
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ZA200505977B true ZA200505977B (en) | 2006-05-31 |
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ZA200505977A ZA200505977B (en) | 2003-01-29 | 2005-07-26 | A therapeutic compsotion for the treatment of HIV-1 and HIV-2 |
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EP (1) | EP1589961A4 (en) |
JP (1) | JP2006516633A (en) |
KR (1) | KR20050094461A (en) |
CN (1) | CN1747726A (en) |
AU (1) | AU2004206996A1 (en) |
CA (1) | CA2514252A1 (en) |
RU (1) | RU2005123957A (en) |
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CN101810625B (en) * | 2010-04-09 | 2012-05-23 | 上海新康制药厂 | Application of taraxasterol |
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US4970212A (en) * | 1982-05-18 | 1990-11-13 | Nowicky Wassili | Method of treating human illnesses which compromise the ability to mount an effective immunological response |
CA1337047C (en) * | 1988-08-18 | 1995-09-19 | Peter Dodd Cooper | Gamma inulin compositions |
US5053419A (en) * | 1989-03-31 | 1991-10-01 | The Children's Medical Center Corporation | Treatment of AIDS dementia, myelopathy and blindness |
US5977073A (en) * | 1991-06-06 | 1999-11-02 | Life Sciences' Technologies, Inc. | Nutrient composition for treatment of immune disorders |
RU2107502C1 (en) * | 1997-03-27 | 1998-03-27 | Открытое акционерное общество "Ветеринарные препараты" | Iodine monochloride, veterinary preparation possessing wide range of action |
AU4944500A (en) * | 1999-06-29 | 2001-01-31 | Robert H. Jacobs | A method for optimizing immune activity in the treatment of auto-immune diseases and chronic immune conditions |
RU2195277C2 (en) * | 2001-02-09 | 2002-12-27 | Третьяков Василий Васильевич | Method of treatment of hiv-infection |
GB2374008B (en) * | 2001-04-04 | 2005-03-16 | John Carter | Pharmaceutical compositions comprising copper and zinc |
PL353693A1 (en) * | 2002-04-30 | 2003-11-03 | Bogusław Jeleń | Compound pharmaceutical for inhibiting replication of hiv-1 and hiv-2 viruses in the cd4+ cells of human immunological system at all stages of infection and in the aids syndrome as well as method of manufacture of compound pharmaceutical for inhibiting replication of hiv-1 and hiv-2 viruses in the cd+ cells of human immunological system at all stages of infection and in the aids syndrome |
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2004
- 2004-01-29 JP JP2006503151A patent/JP2006516633A/en active Pending
- 2004-01-29 RU RU2005123957/15A patent/RU2005123957A/en not_active Application Discontinuation
- 2004-01-29 CA CA002514252A patent/CA2514252A1/en not_active Abandoned
- 2004-01-29 CN CNA2004800039434A patent/CN1747726A/en active Pending
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EP1589961A2 (en) | 2005-11-02 |
JP2006516633A (en) | 2006-07-06 |
WO2004066954A3 (en) | 2005-03-17 |
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EP1589961A4 (en) | 2006-02-15 |
CN1747726A (en) | 2006-03-15 |
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