WO2018093343A1 - Substance biologique active et préparation à base de celle-ci - Google Patents

Substance biologique active et préparation à base de celle-ci Download PDF

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Publication number
WO2018093343A1
WO2018093343A1 PCT/UA2017/000109 UA2017000109W WO2018093343A1 WO 2018093343 A1 WO2018093343 A1 WO 2018093343A1 UA 2017000109 W UA2017000109 W UA 2017000109W WO 2018093343 A1 WO2018093343 A1 WO 2018093343A1
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WO
WIPO (PCT)
Prior art keywords
essential oil
eucalyptus
atcc
active biological
biological substance
Prior art date
Application number
PCT/UA2017/000109
Other languages
English (en)
Russian (ru)
Inventor
Вадим Александрович САФОНОВ
Елена Юрьевна ГОЛИК
Николай Андреевич КОМИСАРЕНКО
Андрей Николаевич КОМИСАРЕНКО
Дарья Валентиновна НИКОЛОВА
Дмитрий Иванович ИСАЕВ
Дмитрий Михайлович КОЖУШКО
Original Assignee
Вадим Александрович САФОНОВ
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 Вадим Александрович САФОНОВ filed Critical Вадим Александрович САФОНОВ
Publication of WO2018093343A1 publication Critical patent/WO2018093343A1/fr

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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
    • A61K31/13—Amines
    • A61K31/14—Quaternary ammonium compounds, e.g. edrophonium, choline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/13—Coniferophyta (gymnosperms)
    • A61K36/15—Pinaceae (Pine family), e.g. pine or cedar
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/23—Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
    • A61K36/282—Artemisia, e.g. wormwood or sagebrush
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/53—Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
    • A61K36/534—Mentha (mint)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/61—Myrtaceae (Myrtle family), e.g. teatree or eucalyptus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/73—Rosaceae (Rose family), e.g. strawberry, chokeberry, blackberry, pear or firethorn
    • A61K36/738—Rosa (rose)

Definitions

  • the claimed invention relates to an active biological or pharmaceutical substance, which has antibacterial activity, has bactericidal, bacteriostatic and antifungal effects,
  • the invention also relates to a topical preparation obtained on the basis of the above active biological substance.
  • the invention can be used for the prevention and treatment of infectious and inflammatory diseases.
  • the invention can be used to deodorize 15 oral cavities.
  • the invention can also be used to inhibit the growth activity of the strains: Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Proteus vulgaris ATCC 4636, Pseudomonas aeruginosa ATCC 27853, Basillus subtilis ATCC 6633 and Candida albicans ATCC 653/885.
  • the claimed invention can be used in the chemical, pharmaceutical, cosmetic and food industries.
  • herbal preparations are becoming more common, which are topical preparations that include herbal components (eucalyptus, mint, sage and others).
  • herbal preparations contain complexes of biologically active substances that are close to the metabolites of the body and are biologically compatible with them.
  • Another advantage of topical preparations of phytopreparations is their normalizing effect on altered body functions in the absence of influence on other indicators.
  • Chlorophyllipt (Clorophylliptum), which is obtained from the leaves of ball eucalyptus (Eucalyptus globulus L) or rod eucalyptus (Eucaliptus viminalis. L) by extraction with 95% ethanol, which has antibacterial activity against staphylococci, streptococcus and A.S. Ns SU1123706). In practice, 0.25%, 1% alcohol and 2% oil solutions of Chlorophyllipt are used.
  • the main biologically active substances of the drug are lipophilic substances: a mixture of euglobals (phenol aldehydes), terpenoids and chlorophylls (Kurkin VA, Pharmacognosy, Samara, LLC Etching, 2004, p. 327-333).
  • a solution of “Chlorophyllipt” (see A.S. see Nfi SU 801341) is obtained by extraction of the leaves of the eucalyptus rod (Eucaliptus viminalis. L) with 96% ethanol and subsequent processing of the concentrated extract with a divalent copper salt, namely 4% copper sulfate solution subsequent extraction of the target product is the amount of hydrophobic components. Extraction with benzene is carried out three times with stirring each time for 15 minutes and settling for 5-6 hours. The settled benzene extract is washed 3 times with purified water and evaporated in vacuo at a temperature of 40 ° C, and then dissolved in alcohol or in oil.
  • Chlorophyllipt and preparations made on its basis is that its antimicrobial effect is directed mainly to bacteria of the genus Staphylococcus and cannot be used against fungi.
  • the Nsl table shows the growth retardation diameter of 1% Chlorophyllipt extract.
  • the objective of the invention is the creation of an active biological substance that has antibacterial activity, has bactericidal, bacteriostatic and antifungal effects.
  • Another objective of the invention is the creation of a topical preparation, which is obtained on the basis of an active biological substance that has antibacterial activity, has bactericidal, bacteriostatic and antifungal effects.
  • Another object of the invention is to suppress the growth activity of the strains: Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Proteus vulgaris ATCC 4636, Pseudomonas aeruginosa ATCC 27853, Basillus subtilis ATCC 6633 and Candida aibicans ATCC 653/885.
  • Another objective of the invention is to increase the effectiveness of the spectrum of action for the prevention and treatment of infectious and inflammatory diseases.
  • Another objective of the invention is to increase the effectiveness of the spectrum of action during deodorization of the oral cavity.
  • Another objective of the invention is to reduce the toxicity of exposure to the body during its use.
  • the above active biological substance additionally contains 1-15% polyvinylpyrrolidone.
  • the above active biological substance additionally contains 10-50% polysorbate 80.
  • the preferred composition of the aforementioned active biological substance has, in the following ratio of components, May. %:
  • the inventors believe that the combination of active components an extract of eucalyptus, benzalkonium chloride and a complex of essential oils in an active biological substance, provides a synergistic pharmacological action, as a result of which the use of the obtained active biological substance leads to inhibition of the growth activity of the strains: Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Proteus vulgaris ATCConas aerosas P36 4636, Proteus vulgaris ATCCosaas3636, ATCC 27853, Basillus subtilis ATCC 6633, and Candida albicans ATCC 653/885.
  • the resulting active biological substance has antibacterial activity, has bactericidal, bacteriostatic and antifungal effects.
  • polyvinylpyrrolidone in an active biological substance leads to the prolongation of the antimicrobial and antifungal action, which consists in the fact that the presence of polyvinylpyrrolidone creates a film on the surface of the organ that is being processed, and this leads to improved adhesion, which leads to the prolongation of the antimicrobial and antifungal action .
  • polysorbate 80 in the active biological substance leads to the fact that the stability of the solution is increased.
  • a topical preparation characterized by the fact that it contains an active biological substance according to the invention, glycerin and purified water in the following ratio, May. %
  • a package of a topical preparation according to the invention is a topical preparation that is placed in a bottle with a metering device.
  • the active components are mixed: eucalyptus extract, benzalkonium chloride and essential oils of eucalyptus, mint, fir, pine, lavender, tea tree, rosemary, coriander, rose and wormwood, and with the addition of additional components of polyvinylpyrrolidone and polysorbate 80.
  • Table Ne2 shows the three obtained samples of active biological substance that suppress the growth activity of the strains: Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Proteus vulgaris ATCC 4636, Pseudomonas aeruginosa ATCC 27853, Basillus subtilis ATCC 6633 and Candida albicans ATCC 6633.
  • Peppermint oil was used as peppermint oil. Table ⁇ 2
  • Example Ns1 Based on the obtained sample of Ns3 of an active biological substance, see Example Ns1, a topical preparation was prepared. For this, purified water was mixed with glycerin followed by the addition of an active biological substance (sample Ns3), as a result of which three samples of a topical preparation were obtained, see table ⁇ 3.
  • a microbial suspension of strains was prepared, which was carried out using a Densi- La-Meter device (manufactured by PUVA-Lachema, Czech Republic; wavelength 540 nm). Microbial suspension of the strains was carried out according to the instructions that are attached to the device, and the newsletter on innovations in health system "Standardization of the preparation of microbial suspensions", Kiev. The culture of the strains was synchronized using a low temperature (4 ° C). Microbial loads were 10 7 microbial cells per 1 ml of medium and were established according to McFarland standard 5. An 18-24 hour culture of microorganism strains was taken into the work.
  • Muller-Hinton agar was used (Production - India “HIMediaLaboratorles Pvt. Ltd lndia”, the shelf life of the medium is until XI.2016).
  • Saburo agar was used for Candidaalbicans (Production - India, “HIMedial_aboratorles Pvt. Ltd lndia” expiration date wednesday until X1.2016).
  • the method of diffusion of the drug into agar was carried out by "wells".
  • the determination of the activity of antibacterial drugs was carried out on two layers of a dense nutrient medium spilled in Petri dishes. In the lower layer used a "hungry" un seeded medium (agar-agar, water, salt).
  • the bottom layer is a substrate of 10 ml of “hungry agar”, on which 3-6 thin-walled stainless steel cylinders with a diameter of 8 mm and a height of 10 mm are installed horizontally.
  • the upper layer consisting of a nutrient agar medium, molten and cooled to 40 ° C, into which
  • the volume of medium for the upper layer ranged from 14 to 16 ml.
  • the cups were dried for 30-40 minutes at room temperature and placed in a thermostat for 18-24 hours.
  • Test data of antibacterial and antifungal activity are set out in table ⁇ 4.
  • the data in table Ns4 indicate that, in contrast to the known preparation, the invention actively suppresses the growth of strains: Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Basillus subtilis ATCC 6633, and also provides static suppression of the growth of the fungus strain Candida albicans ATCC 653/885 , that is, the resulting topical preparation obtained on the basis of biologically active substance has antibacterial activity, has bactericidal, bacteriostatic and antifungal effects.
  • the resulting topical preparation can be used in the form of a solution, spray and aerosol.
  • a package of a topical preparation is the resulting topical preparation, which is placed in a bottle with a dosing device, with the help of which the topical preparation
  • the obtained active biological substance which has antibacterial activity, has 25 bactericidal, bacteriostatic and antifungal effects called: lat. "Clorophylliptum active plus”, Ukrainian ⁇ Asset Plus, Rus. "Chlorophyllipt asset plus.”
  • the technical result of the invention is the production of an active biological substance and a local preparation based on it, which have antibacterial activity, have bactericidal, bacteriostatic and antifungal effects.

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  • Health & Medical Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Mycology (AREA)
  • Microbiology (AREA)
  • Medical Informatics (AREA)
  • Botany (AREA)
  • Biotechnology (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

L'invention concerne une substance biologique ou pharmaceutique active qui a une activité antibactérienne et possède un effet bactéricide, bactériostatique et antimycosique. Selon l'invention, la substance biologique active est caractérisée par la présence de ce qui suit : extrait d'eucalyptus, chlorure de benzalkonium et huiles essentielles d'eucalyptus, menthe, sapin sibérien, pin, lavande, arbre à thé, romarin, coriandre, rose et armoise, avec le rapport équivalent suivant, en % en masse : d'eucalyptus 18,86-55,63, chlorure de benzalkonium 18,86-44,47, huile essentielle d'eucalyptus 3,70-22,24 huile essentielle de menthe 3,70-22,24 huile essentielle de sapin sibérien 0,1-4,42 huile essentielle de pin 0,1-4,42 huile essentielle de lavande 0,1-4,42 huile essentielle d'arbre à thé 0,1-4,42 huile essentielle de romarin 0,1-4,42 huile essentielle de coriandre 0,1-4,42 huile essentielle de rose 1,34-2,24 huile essentielle d'armoise 1,34-2,24; le résultat technique consiste à obtenir une substance biologique active et préparation à action locale à base de celle-ci qui ont une activité antibactérienne et ont un effet bactéricide, bactériostatique et antimycosique.
PCT/UA2017/000109 2016-11-15 2017-11-06 Substance biologique active et préparation à base de celle-ci WO2018093343A1 (fr)

Applications Claiming Priority (2)

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UA201611593 2016-11-15
UAA201611593 2016-11-15

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111388358A (zh) * 2020-05-13 2020-07-10 黄敏 一种具有杀螨祛痘功效的植物精油组合物及制备和应用
CN115737706A (zh) * 2022-11-23 2023-03-07 海南皇隆制药股份有限公司 一种苯扎氯铵溶液及其制备方法

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2767896C1 (ru) * 2021-06-23 2022-03-22 Общество с ограниченной ответственностью "СИД" Антибактериальная композиция
CN114259430B (zh) * 2021-12-28 2024-01-19 郑州中科新兴产业技术研究院 一种植物精油抑菌喷雾及其制备方法

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RU2572231C1 (ru) * 2014-09-29 2015-12-27 Рамиль Шамилевич Хазиев Способ получения антибактериального препарата из листьев эвкалипта прутовидного

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RU2572231C1 (ru) * 2014-09-29 2015-12-27 Рамиль Шамилевич Хазиев Способ получения антибактериального препарата из листьев эвкалипта прутовидного

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111388358A (zh) * 2020-05-13 2020-07-10 黄敏 一种具有杀螨祛痘功效的植物精油组合物及制备和应用
CN115737706A (zh) * 2022-11-23 2023-03-07 海南皇隆制药股份有限公司 一种苯扎氯铵溶液及其制备方法
CN115737706B (zh) * 2022-11-23 2023-08-29 海南皇隆制药股份有限公司 一种苯扎氯铵溶液及其制备方法

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