WO2006038900A1 - Composition pharmaceutique possedant un effet actibacterien et antiviral - Google Patents

Composition pharmaceutique possedant un effet actibacterien et antiviral Download PDF

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Publication number
WO2006038900A1
WO2006038900A1 PCT/UA2005/000041 UA2005000041W WO2006038900A1 WO 2006038900 A1 WO2006038900 A1 WO 2006038900A1 UA 2005000041 W UA2005000041 W UA 2005000041W WO 2006038900 A1 WO2006038900 A1 WO 2006038900A1
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WO
WIPO (PCT)
Prior art keywords
pharmaceutical composition
composition according
complexing agent
active component
preceding paragraphs
Prior art date
Application number
PCT/UA2005/000041
Other languages
English (en)
Russian (ru)
Inventor
Volodymyr Petrovych Vladyko
Tamara Petrivna Kiselyova
Carlo-Federico Perno
P. Jacques Simpore
Eficio Locci
Stefano Aquaro
Original Assignee
Volodymyr Petrovych Vladyko
Tamara Petrivna Kiselyova
Carlo-Federico Perno
Simpore P Jacques
Eficio Locci
Stefano Aquaro
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Volodymyr Petrovych Vladyko, Tamara Petrivna Kiselyova, Carlo-Federico Perno, Simpore P Jacques, Eficio Locci, Stefano Aquaro filed Critical Volodymyr Petrovych Vladyko
Publication of WO2006038900A1 publication Critical patent/WO2006038900A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K33/18—Iodine; 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
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40—Cyclodextrins; Derivatives thereof

Definitions

  • the present invention relates, in general, to the field of medicine and general chemistry, and more particularly, to a pharmaceutical composition that has antibacterial and antiviral effects and is intended for use in therapeutic practice as an effective medical drug against infectious diseases.
  • a fairly large number of medications are known which contain a free chemical element or its ion as an active component.
  • the simplest example is free iodine-based drugs, since its properties have long been known to provide a powerful antibacterial and antiviral effect even when diluted to a ratio
  • Iodine-based drugs have a very wide range of effects, ranging from superficial disinfection of wounds to hormone therapy.
  • Complexing agents that can bind to the active component are also known, including for pharmaceutical purposes, and include complexing and active substances of a wide variety of nature.
  • DE 3819498 discloses an iodine inclusion compound and a cyclodextrin polymer (oligomer) that can release iodine in a controlled manner.
  • a granular composition which contains a complex of cyclodextrin with iodine and has a gradual and long-term antiseptic effect, and also discloses a method for its preparation.
  • CN 1377584 discloses an aqueous solution of atomic iodine which contains cyclodextrin as a co-solvent, has a strong sterilization effect and is characterized by the absence of side effects.
  • Lithium salts are used in medical practice mainly for the treatment of gout and some mental disorders by enhancing the replication of viruses. It is also known that lithium cations stimulate the proliferation of leukocytes and accelerated growth of bone marrow mass.
  • the basis of the invention is the creation of a new pharmaceutical composition with antibacterial and antiviral effects, which would have improved therapeutic properties compared with compositions of a similar purpose, known from the prior art.
  • composition containing an active component which is a free chemical element and / or a substance capable of
  • a complexing agent that can bind to the active component or the ion that it forms, a lithium ion donor and a pharmaceutically acceptable carrier is a pharmaceutical composition having excellent therapeutic properties due to the synergistic effect of its constituents. Such properties are significantly higher activity and resistance of the active substance, as well as reduced toxicity of the composition and, therefore, the possibility of its intravenous administration.
  • the active component which is a free chemical element and / or a substance capable of forming ions, 5 preferably use free iodine.
  • a complexing agent is preferably used a substance that contains elements with non-separated electron pairs, more preferably a substance that contains nitrogen and / or oxygen and / or sulfur, more preferably a substance that contains cycles in its structure, even more preferably a cyclic oligomer and most preferably cyclodextrin.
  • a pharmaceutically acceptable soluble lithium salt is preferably used as a lithium ion donor.
  • a solution more preferably an aqueous solution, which in its physicochemical properties is close to the liquid component of the body of a mammal, including humans, and most preferably saline.
  • the solution further comprises a viscosity regulator, in which quality 20 preferably a polymer, more preferably polyvinyl alcohol or polyvinylpyrrolidone, is used.
  • quality 20 preferably a polymer, more preferably polyvinyl alcohol or polyvinylpyrrolidone, is used.
  • the mass fraction of the active component is from 0.0002 to 2.0% of the total mass of the composition
  • the mass fraction of the complexing agent is from 0.5 to 20.0% of the total mass
  • the mass fraction of the donor of lithium ion is from 0.00002 to 0.2% of the total weight of the composition.
  • the composition according to the invention is a colloidal polymer solution in which inorganic and organic substances are dissolved.
  • the active component is a free chemical element and / or substance that is capable of forming ions, and thanks to various reactions taking place in solution, this component can simultaneously be in several forms: molecular, ionic, complex.
  • the solution may be in the form of a gel, which allows the active component to interact with virtually all classes of substances that are part of the human or animal body, as well as in the composition of the membranes and the cells themselves. In this case, reactions take place, the sequence of which leads to the binding of the active component with biologically active substances with the formation of their new forms (active substance-protein, active substance-enzyme, active substance-hormone, active substance-biological membrane, and the like).
  • Such a new form of biologically active substance, as well as the free active component, can distort the normal course of biochemical reactions of a foreign bacterial cell or virus by blocking the action of proteins and enzymes that are vital for them or by modifying the information that RNA or DNA of a bacterium or virus carries.
  • a complexing agent which can coordinate molecules and ions due to donor-acceptor interactions of the zwitterion type, provides reduced toxicity of the active component, its increased resistance, in particular to hydrolysis, prolonged action and other properties inherent to a thixotropic gel.
  • a drug is introduced on the basis of the proposed composition into the blood, its components and blood interact with the viruses or bacterial cells that it contains, and the drug also takes place to the site of the localization of viruses and bacteria in various organs. Lithium ions generated by the donor of such ions improve the conductivity of cell membranes and promote lateral diffusion into the bilayer of cell membranes due to the small size of the cations.
  • the active component is free iodine, iodine molecules and triiodide ions, coordinated into the spatial network using a complexing agent, iodine purine and pyrimidine bases, which are part of the nucleic acids of viruses and bacteria, effectively inhibiting their replication.
  • the pharmaceutical composition according to the invention has antibacterial and antiviral effects, has improved therapeutic properties compared with compositions of a similar purpose known from the prior art, including an increased degree of activity and resistance of the active component and a reduced degree of its toxicity, which allows the use of a medicinal product on its basis intravenously in the treatment of various infectious diseases.
  • compositions of a similar purpose known from the prior art including an increased degree of activity and resistance of the active component and a reduced degree of its toxicity, which allows the use of a medicinal product on its basis intravenously in the treatment of various infectious diseases.
  • the hermetic virus virus titer was administered intravenously to two groups of outbred white mice.
  • a pharmaceutical solution was administered to one group the composition obtained in example 1, calculated on the weight of each mouse.
  • Another group was a control.
  • mortality in the control group was 100%, and in the main - 10%.
  • Subsequent studies of a biological nature revealed the complete recovery of mice from the group in which the solution of the pharmaceutical composition proposed in accordance with the present invention was used.
  • the proposed pharmaceutical composition which has antibacterial and antiviral effects, can be used as an effective medical drug in the practice of treating all kinds of infectious diseases of mammals, including humans, and the reduced toxicity of its components allows the drug to be administered intravenously.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Dermatology (AREA)
  • Virology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne une composition pharmaceutique possédant un effet actibactérien et antiviral comprenant un composant actif qui est un élément chimique libre, par exemple, le iode, et/ou un composé capable de former des ions, un complexant capable de se lier avec le composant actif ou un ion qu'il forme, un donneur d'ion de lithium et un excipient pharmaceutiquement acceptable; la composition peut s'utiliser dans le traitement de diverses maladies infectieuses et être destinée à l'usage interne.
PCT/UA2005/000041 2004-10-05 2005-09-27 Composition pharmaceutique possedant un effet actibacterien et antiviral WO2006038900A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
UA20041008067 2004-10-05
UA20041008067 2004-10-05

Publications (1)

Publication Number Publication Date
WO2006038900A1 true WO2006038900A1 (fr) 2006-04-13

Family

ID=35539539

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/UA2005/000041 WO2006038900A1 (fr) 2004-10-05 2005-09-27 Composition pharmaceutique possedant un effet actibacterien et antiviral

Country Status (1)

Country Link
WO (1) WO2006038900A1 (fr)

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4693894A (en) * 1986-01-16 1987-09-15 Ppg Industries, Inc. Halophor composition
DE3819498A1 (de) * 1987-06-08 1988-12-29 Consortium Elektrochem Ind Cyclodextrinpolymerjodeinschlussverbindungen mit kontrollierter jodfreisetzung
JPH10203916A (ja) * 1997-01-20 1998-08-04 Mitsui Chem Inc 固形ヨードホール組成物
JPH1135413A (ja) * 1997-07-15 1999-02-09 Mitsui Chem Inc 固形ヨードホール成形物
EP0978289A1 (fr) * 1998-07-29 2000-02-09 Aleksandr Ivanovic Iljin Virucide contenant de l'iode
WO2001078751A1 (fr) * 2000-04-17 2001-10-25 'armenicum+' Jsc Preparation pharmaceutique antivirale et antibacterienne 'armenicum' et son utilisation dans le traitement de maladies infectieuses

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4693894A (en) * 1986-01-16 1987-09-15 Ppg Industries, Inc. Halophor composition
DE3819498A1 (de) * 1987-06-08 1988-12-29 Consortium Elektrochem Ind Cyclodextrinpolymerjodeinschlussverbindungen mit kontrollierter jodfreisetzung
JPH10203916A (ja) * 1997-01-20 1998-08-04 Mitsui Chem Inc 固形ヨードホール組成物
JPH1135413A (ja) * 1997-07-15 1999-02-09 Mitsui Chem Inc 固形ヨードホール成形物
EP0978289A1 (fr) * 1998-07-29 2000-02-09 Aleksandr Ivanovic Iljin Virucide contenant de l'iode
WO2001078751A1 (fr) * 2000-04-17 2001-10-25 'armenicum+' Jsc Preparation pharmaceutique antivirale et antibacterienne 'armenicum' et son utilisation dans le traitement de maladies infectieuses

Non-Patent Citations (9)

* Cited by examiner, † Cited by third party
Title
DATABASE MEDLINE [online] US NATIONAL LIBRARY OF MEDICINE (NLM), BETHESDA, MD, US; September 2005 (2005-09-01), "[Pharmacological modulation of phagocytosis of granulocytes and monocytes in patients with familial Mediterranean fever]", XP002363886, Database accession no. NLM16277210 *
DATABASE MEDLINE [online] US NATIONAL LIBRARY OF MEDICINE (NLM), BETHESDA, MD, US; September 2005 (2005-09-01), "[The effect of colcichine and iodine-lithium-alpha-dextrin on the phagocytosis of granulocytes and monocytes in patients with familial Mediterranean fever]", XP002363887, Database accession no. NLM16277209 *
DAVTYAN, T. K. ET AL: "HIV-infection and brain function: neuro-immune humoral regulation", NEIROKHIMIYA , 19(3), 219-226 CODEN: NERODV; ISSN: 1027-8133, 2002, XP009060230 *
EKSPERIMENTAL'NAIA I KLINICHESKAIA FARMAKOLOGIIA. 2005 SEP-OCT, vol. 68, no. 5, September 2005 (2005-09-01), pages 36 - 39, ISSN: 0869-2092 *
EKSPERIMENTAL'NAIA I KLINICHESKAIA FARMAKOLOGIIA. 2005 SEP-OCT, vol. 68, no. 5, September 2005 (2005-09-01), pages 40 - 43, ISSN: 0869-2092 *
KOCZON P ET AL: "m-Iodobenzoic acid complexes with selected metals: molecular structure and antimicrobial activity.", JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY. JUN 2001, vol. 49, no. 6, June 2001 (2001-06-01), pages 2982 - 2986, XP009060220, ISSN: 0021-8561 *
NOLTEMEYER M ET AL: "STRUCTURAL CHEMISTRY OF LINEAR ALPHA CYCLO DEXTRIN POLY IODINE COMPLEXES X-RAY CRYSTAL STRUCTURES OF BIS-ALPHA CYCLO DEXTRIN LITHIUM TRI IODIDE DI IODINE OCTA HYDRATE AND ALPHA CYCLO DEXTRIN CADMIUM PENTA IODIDE 2 0.5 1 HEPTACOSA HYDRATE MODELS FOR THE BLUE AMYLOSE IODINE COMPLEX", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 102, no. 8, 1980, pages 2710 - 2722, XP009060213, ISSN: 0002-7863 *
PATENT ABSTRACTS OF JAPAN vol. 1998, no. 13 30 November 1998 (1998-11-30) *
PATENT ABSTRACTS OF JAPAN vol. 1999, no. 05 31 May 1999 (1999-05-31) *

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