[go: up one dir, main page]

RU2011144624A - PHARMACEUTICAL AEROSOL COMPOSITION OF PROTEAZ INHIBITORS WITH OZONE-SAVING PROPELLANT AND ITS PRODUCTION - Google Patents

PHARMACEUTICAL AEROSOL COMPOSITION OF PROTEAZ INHIBITORS WITH OZONE-SAVING PROPELLANT AND ITS PRODUCTION Download PDF

Info

Publication number
RU2011144624A
RU2011144624A RU2011144624/15A RU2011144624A RU2011144624A RU 2011144624 A RU2011144624 A RU 2011144624A RU 2011144624/15 A RU2011144624/15 A RU 2011144624/15A RU 2011144624 A RU2011144624 A RU 2011144624A RU 2011144624 A RU2011144624 A RU 2011144624A
Authority
RU
Russia
Prior art keywords
group
propellant
mixture according
protease inhibitor
mixture
Prior art date
Application number
RU2011144624/15A
Other languages
Russian (ru)
Other versions
RU2657523C2 (en
Inventor
Олег Петрович Жирнов
Original Assignee
Олег Петрович Жирнов
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 Олег Петрович Жирнов filed Critical Олег Петрович Жирнов
Priority to RU2011144624A priority Critical patent/RU2657523C2/en
Priority to EA201201362A priority patent/EA034991B1/en
Priority to PCT/RU2012/000896 priority patent/WO2013066214A2/en
Priority to GB1409877.6A priority patent/GB2511011A/en
Publication of RU2011144624A publication Critical patent/RU2011144624A/en
Application granted granted Critical
Publication of RU2657523C2 publication Critical patent/RU2657523C2/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/008Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/12Aerosols; Foams
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/55Protease inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/55Protease inhibitors
    • A61K38/57Protease inhibitors from animals; from humans
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Dispersion Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • General Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Communicable Diseases (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Zoology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)

Abstract

1. Фармацевтический аэрозольный состав ингибитора протеаз с озонсберегающим пропеллентом, отличающийся тем, что водный раствор активного вещества из группы ингибиторов протеаз, содержащий 0,05-250 мг протеазного ингибитора на мл раствора, последовательно смешивают с ингредиентами трех-компонентной выталкивающей смеси, а именно: глицерола, этанола и водонерастворимого озонсберегающего пропеллента с соотношением водной фазы и трехкомпонентной смеси 0,5-5 и 95-99,5 об.%, соответственно, и создают гомогенный аэрозольный состав, позволяющий генерировать фармацевтический аэрозоль активного протеазного ингибитора за счет выталкивающей силы пропеллента при распылении полученного состава из аэрозольного устройства, снабженного выпускным клапаном.2. Смесь по п.1, отличающаяся тем, что водный раствор ингибитора протеаз последовательно смешивают с компонентами выталкивающей системы - глицеролом, этанолом и фтор-содержащим пропеллентом 134А, взятых в объемном соотношении 1-7:3-13:80-96%, соответственно.3. Смесь по п.1, отличающаяся тем, что активное вещество, выбранное из группы ингибиторов протеаз белковой и полипептидной природы, представлено апротинином, α 2-антиплазмином, α-1антитрипсином, антитрипсином, цистатином, преимущественно апротинином, или их комбинацией.4. Смесь по п.1, отличающаяся тем, что активное вещество выбрано из группы антипротеазных олигопептидов, состоящих из двух и более аминокислотных остатков и их модифицированных производных.5. Смесь по п.1, содержащая одну или несколько органолептических добавок, из группы растительных масел, включающей масло мяты перечной, мяты душистой, ментоловое масло в количестве 1. The pharmaceutical aerosol composition of the protease inhibitor with ozone-saving propellant, characterized in that an aqueous solution of the active substance from the group of protease inhibitors containing 0.05-250 mg of the protease inhibitor per ml of solution is sequentially mixed with the ingredients of a three-component push mixture, namely: glycerol, ethanol and a water-insoluble ozone-saving propellant with a ratio of the aqueous phase and a three-component mixture of 0.5-5 and 95-99.5 vol.%, respectively, and create a homogeneous aerosol composition that allows generating pharmaceutical aerosol of the active protease inhibitor due to the buoyancy of the propellant when spraying the resulting composition from an aerosol device equipped with an exhaust valve. 2. The mixture according to claim 1, characterized in that the aqueous solution of the protease inhibitor is sequentially mixed with components of the ejection system - glycerol, ethanol and a fluorine-containing propellant 134A, taken in a volume ratio of 1-7: 3-13: 80-96%, respectively. 3. A mixture according to claim 1, characterized in that the active substance selected from the group of protease inhibitors of protein and polypeptide nature is aprotinin, α 2-antiplasmin, α-1 antitrypsin, antitrypsin, cystatin, mainly aprotinin, or a combination thereof. A mixture according to claim 1, characterized in that the active substance is selected from the group of antiprotease oligopeptides consisting of two or more amino acid residues and their modified derivatives. The mixture according to claim 1, containing one or more organoleptic additives, from the group of vegetable oils, including peppermint oil, aromatic mint, menthol oil in an amount

Claims (7)

1. Фармацевтический аэрозольный состав ингибитора протеаз с озонсберегающим пропеллентом, отличающийся тем, что водный раствор активного вещества из группы ингибиторов протеаз, содержащий 0,05-250 мг протеазного ингибитора на мл раствора, последовательно смешивают с ингредиентами трех-компонентной выталкивающей смеси, а именно: глицерола, этанола и водонерастворимого озонсберегающего пропеллента с соотношением водной фазы и трехкомпонентной смеси 0,5-5 и 95-99,5 об.%, соответственно, и создают гомогенный аэрозольный состав, позволяющий генерировать фармацевтический аэрозоль активного протеазного ингибитора за счет выталкивающей силы пропеллента при распылении полученного состава из аэрозольного устройства, снабженного выпускным клапаном.1. The pharmaceutical aerosol composition of the protease inhibitor with ozone-saving propellant, characterized in that the aqueous solution of the active substance from the group of protease inhibitors containing 0.05-250 mg of the protease inhibitor per ml of solution is sequentially mixed with the ingredients of a three-component push mixture, namely: glycerol, ethanol and a water-insoluble ozone-saving propellant with a ratio of the aqueous phase and a three-component mixture of 0.5-5 and 95-99.5 vol.%, respectively, and create a homogeneous aerosol composition that allows generating to inject a pharmaceutical aerosol of an active protease inhibitor due to the buoyancy of the propellant when spraying the resulting composition from an aerosol device equipped with an exhaust valve. 2. Смесь по п.1, отличающаяся тем, что водный раствор ингибитора протеаз последовательно смешивают с компонентами выталкивающей системы - глицеролом, этанолом и фтор-содержащим пропеллентом 134А, взятых в объемном соотношении 1-7:3-13:80-96%, соответственно.2. The mixture according to claim 1, characterized in that the aqueous solution of the protease inhibitor is sequentially mixed with the components of the ejection system - glycerol, ethanol and a fluorine-containing propellant 134A, taken in a volume ratio of 1-7: 3-13: 80-96%, respectively. 3. Смесь по п.1, отличающаяся тем, что активное вещество, выбранное из группы ингибиторов протеаз белковой и полипептидной природы, представлено апротинином, α 2-антиплазмином, α-1антитрипсином, антитрипсином, цистатином, преимущественно апротинином, или их комбинацией.3. The mixture according to claim 1, characterized in that the active substance selected from the group of protease inhibitors of protein and polypeptide nature, is aprotinin, α 2-antiplasmin, α-1 antitrypsin, antitrypsin, cystatin, mainly aprotinin, or a combination thereof. 4. Смесь по п.1, отличающаяся тем, что активное вещество выбрано из группы антипротеазных олигопептидов, состоящих из двух и более аминокислотных остатков и их модифицированных производных.4. The mixture according to claim 1, characterized in that the active substance is selected from the group of antiprotease oligopeptides consisting of two or more amino acid residues and their modified derivatives. 5. Смесь по п.1, содержащая одну или несколько органолептических добавок, из группы растительных масел, включающей масло мяты перечной, мяты душистой, ментоловое масло в количестве 0,05-0,9% от общего объема.5. The mixture according to claim 1, containing one or more organoleptic additives from the group of vegetable oils, including peppermint oil, aromatic mint, menthol oil in an amount of 0.05-0.9% of the total volume. 6. Смесь по п.1, содержащая одну или несколько добавок, из группы поверхностно-активных веществ, включающих твин-20, твин-80, сран-20, сран-80, олеиновую кислоту, глицерил моноолеат, диметилсульфоксид, полиэтилен гликоль, в количестве 0,1-3,0% от общего объема.6. The mixture according to claim 1, containing one or more additives, from the group of surfactants, including tween-20, tween-80, sran-20, sran-80, oleic acid, glyceryl monooleate, dimethyl sulfoxide, polyethylene glycol, the amount of 0.1-3.0% of the total volume. 7. Аэрозоль по п.1 имеет диаметр частиц в диапазоне 0,5-250 мкм. 7. The aerosol according to claim 1 has a particle diameter in the range of 0.5-250 microns.
RU2011144624A 2011-11-03 2011-11-03 Pharmaceutical aerosol composition of protease inhibitors with ozone-preserving propellant and its preparation RU2657523C2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
RU2011144624A RU2657523C2 (en) 2011-11-03 2011-11-03 Pharmaceutical aerosol composition of protease inhibitors with ozone-preserving propellant and its preparation
EA201201362A EA034991B1 (en) 2011-11-03 2012-10-27 Pharmaceutical aerosol formulation of a protease inhibitor
PCT/RU2012/000896 WO2013066214A2 (en) 2011-11-03 2012-11-01 Aerosol pharmaceutical composition of protease inhibitors and production thereof
GB1409877.6A GB2511011A (en) 2011-11-03 2012-11-01 Aerosol pharmaceutical composition of protease inhibitors and production thereof

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
RU2011144624A RU2657523C2 (en) 2011-11-03 2011-11-03 Pharmaceutical aerosol composition of protease inhibitors with ozone-preserving propellant and its preparation

Publications (2)

Publication Number Publication Date
RU2011144624A true RU2011144624A (en) 2013-05-10
RU2657523C2 RU2657523C2 (en) 2018-06-14

Family

ID=48192963

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2011144624A RU2657523C2 (en) 2011-11-03 2011-11-03 Pharmaceutical aerosol composition of protease inhibitors with ozone-preserving propellant and its preparation

Country Status (4)

Country Link
EA (1) EA034991B1 (en)
GB (1) GB2511011A (en)
RU (1) RU2657523C2 (en)
WO (1) WO2013066214A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2711080C2 (en) * 2015-06-15 2020-01-15 Олег Петрович Жирнов Combined aerosol composition based on protease inhibitors and preparation thereof
US20240415944A1 (en) * 2021-04-06 2024-12-19 Andrey Alexandrovich Ivashchenko Aqueous aprotinin-containing antiviral pharmaceutical composition

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2656944B2 (en) * 1987-04-30 1997-09-24 クーパー ラボラトリーズ Aerosolization of protein therapeutics
RU2054180C1 (en) * 1991-08-21 1996-02-10 Жирнов Олег Петрович (н/п) Method and aerosol for treating respiratory virus infections
US6524557B1 (en) * 1994-12-22 2003-02-25 Astrazeneca Ab Aerosol formulations of peptides and proteins
US20010006939A1 (en) * 1997-10-03 2001-07-05 Ralph W. Niven Secretory leukocyte protease inhibitor dry powder pharmaceutical compositions
US6849263B2 (en) * 1998-12-21 2005-02-01 Generex Pharmaceutical Incorporated Pharmaceutical compositions for buccal delivery of pain relief medications
US6294153B1 (en) * 1998-12-21 2001-09-25 Generex Pharmaceuticals, Inc. Aerosol pharmaceutical formulation for pulmonary and nasal delivery
EP1187639A1 (en) * 1999-06-04 2002-03-20 Delrx Pharmaceutical Corporation Formulations comprising dehydrated particles of pharmaceutical agents and process for preparing the same
WO2002043750A2 (en) * 2000-12-01 2002-06-06 Battelle Memorial Institute Method for the stabilizing of biomolecules (e.g. insulin) in liquid formulations
GB0507577D0 (en) * 2005-04-14 2005-05-18 Novartis Ag Organic compounds
RU2356537C2 (en) * 2007-07-25 2009-05-27 Закрытое Акционерное Общество (ЗАО) "Пульмомед" Pharmaceutical composition of metered aerosols containing antiasthmatic agents in form of suspensions, solutions, emulsions, solutions and emulsions
RU2425691C1 (en) * 2010-07-15 2011-08-10 ВАКЕ спол с.р.о. Aprotinin aerosol for treating viral respiratory infections

Also Published As

Publication number Publication date
WO2013066214A2 (en) 2013-05-10
RU2657523C2 (en) 2018-06-14
EA034991B1 (en) 2020-04-15
WO2013066214A3 (en) 2013-08-22
GB201409877D0 (en) 2014-07-16
EA201201362A1 (en) 2013-05-30
GB2511011A (en) 2014-08-20

Similar Documents

Publication Publication Date Title
RU2015122789A (en) Aerosol composition with a propellant based on protease inhibitors and its preparation
UA102477C2 (en) Capsule composition
AR076305A1 (en) COMPOSITIONS OF ALFA- (N-SULFONAMIDE) COMPOSITE BIODISPONDS CAPSULES
ES2625075T3 (en) Aerosol compositions that eliminate odors and contain alkylene glycol (s)
BRPI0910341A2 (en) device for the conservation, spontaneous preparation and administration of an active ingredient
AR051420A1 (en) PROCESSES FOR THE PREPARATION OF OLEOUS COMPOSITIONS
AR057697A1 (en) SPRAY COMPOSITIONS
RU2012144626A (en) COMPOSITIONS AND METHODS USED FOR STABILIZING WHITE-CONTAINING READY FORMS
RU2014147365A (en) APPLICANT INJECTED COMPOSITIONS
TsUKURA et al. Effects of capsaicin on cellular damage and monolayer permeability in human intestinal Caco-2 cells
RU2011144624A (en) PHARMACEUTICAL AEROSOL COMPOSITION OF PROTEAZ INHIBITORS WITH OZONE-SAVING PROPELLANT AND ITS PRODUCTION
EA201270745A1 (en) IMPROVED STABLE AQUEOUS COMPOSITION (E) -4-CARBOXYSTYRYL-4-HLORBENZYLESULPHONE
AR053977A1 (en) PHARMACEUTICAL COMPOSITIONS WITH FLAVOR MASK
CO6341531A2 (en) FOOD ACID FOOD PRODUCT WITH CHIA BASE, RICH IN OMEGA-3, WITH GOOD STABILITY
Gupta et al. Preparation of prospective plant oil derived micro-emulsion vehicles for drug delivery
AR084235A1 (en) PHARMACEUTICAL COMPOSITIONS THAT INCLUDE ALISPORIVIR
ES2497667T3 (en) Emulsification system for use in cosmetics
RU2013137782A (en) WATER IONIC SOLUTION CONTAINING SEA WATER, AT LEAST ONE COMPOUND, NOT MIXED INITIATELY MIXED WITH SEA WATER
MX2016008729A (en) Pharmaceutical composition containing clomipramine and preparation method therefor.
CN104367569A (en) Nano coenzyme Q10 oral liquid
ATE376834T1 (en) COMPOSITION IN SPRAY FORM WITH A COMBINATION OF CLOBETASOL PROPIONATE AND CALCITRIOL, AN ALCOHOL PHASE AND OIL PHASE
RU2013111743A (en) NON-AQUATIC OIL INJECTION COMPOSITION MANIFESTING ANTISEPTIC EFFICIENCY
US20140134124A1 (en) Sanitary compound for use on skin
JP5194337B2 (en) Aerosol
JP4997767B2 (en) Ubidecarenone-containing composition

Legal Events

Date Code Title Description
FA93 Acknowledgement of application withdrawn (no request for examination)

Effective date: 20150111

FZ9A Application not withdrawn (correction of the notice of withdrawal)

Effective date: 20151118