WO2022060251A1 - Gouttes oculaires pour la prévention et le traitement de la cataracte liée à l'âge - Google Patents

Gouttes oculaires pour la prévention et le traitement de la cataracte liée à l'âge Download PDF

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Publication number
WO2022060251A1
WO2022060251A1 PCT/RU2021/050244 RU2021050244W WO2022060251A1 WO 2022060251 A1 WO2022060251 A1 WO 2022060251A1 RU 2021050244 W RU2021050244 W RU 2021050244W WO 2022060251 A1 WO2022060251 A1 WO 2022060251A1
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Prior art keywords
eye drops
substances
contain
medium
formula
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English (en)
Russian (ru)
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Надежда Витальевна КОРСАКОВА
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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents

Definitions

  • the invention relates to pharmacology, specifically to the preparation of improved compositions based on a serotonin receptor antagonist, which can be used in ophthalmology, therapy and geriatrics.
  • the invention contributes to the improvement of approaches to targeted prevention and treatment of age-related opacification of the lens (age-related cataract) of the nuclear type and other age-related degenerative diseases of the organ of vision with similar pathogenesis.
  • Non-Patent Literature 1 - 4 Modern medicine has proven that with age-related cataracts, various chemical, morphological and clinical changes occur in the lens [Non-Patent Literature 1 - 4]. Therefore, it is necessary to apply a differentiated pathogenetically substantiated approach to the prevention and treatment of various types of age-related dystrophic lesions of the lens [Patent Literature 1 - 2]. This approach made it possible to supplement the list of modern anti-cataract eye drops with anti-dystrophic drugs based on a serotonin receptor antagonist, which in experiments demonstrates its therapeutic potential in relation to the nuclear cataract model on the lenses of laboratory rats and rabbits.
  • Patent Literature 3 which exhibits the properties of an antagonist of 5 - HT 3 - serotonin receptors, has anti-emetic activity [Patent Literature 4] and is currently used exclusively as a regulator of motor activity of the upper gastrointestinal tract with nausea and vomiting of various origins.
  • Patent Literature 6 experience in the experimental use of this pharmaceutical composition, allows us to conclude that the previously proposed eye drops contain too narrow a range of prophylactic dosages of the active anti-cataract component, while not providing for the presence of components that increase the duration of contact of eye drops with the surface eyeball (prolongators), which leads to rapid leaching of the drug instilled into the conjunctival sac of the eye and, as a result, to a decrease in its preventive and therapeutic effect.
  • the second closest analogue of this invention according to the proposed essence are "Eye drops for the treatment of age-related nuclear cataract” [Patent Literature 7].
  • these eye drops contain a higher therapeutic dosage range of the active ingredient (serotonin receptor antagonist - ondansetron hydrochloride dihydrate), since these eye drops have an exclusively therapeutic, and not prophylactic, purpose of use and are intended for use in conditions of an already formed cataract process, accompanied by severe organic changes in the substance of the lens.
  • Eye drops are proposed, containing as an active ingredient a serotonin receptor antagonist in a wider range of reduced dosage, according to the invention also additionally containing auxiliary components that increase the therapeutic effect of the active ingredient: substances that provide the viscosity of the medium (prolongator), substances that maintain the pH of the medium (pH regulator ), a stabilizer of biological, physico-chemical properties and / or resistance to contamination by microorganisms in the following ratio of components in 1 ml of solution: Ondansetron hydrochloride dihydrate, g - 0.000001 - 0.00029 Substances that provide the viscosity of the medium in the range of 5 - 100 mm 2 / s Substances that maintain the pH of the environment in the range of 3.5 - 8.5 Stabilizer, g - 0.00005 - 0.1 Solvent, g - 0.001 - 0.05 Distilled water, ml - the rest.
  • substances that provide the viscosity of the medium prolongator
  • eye drops as substances that provide the viscosity of the medium (prolongator) contain one of the following substances: polyvinylpyrrolidone, polyvinyl alcohol, hydroxymethylcellulose, methylcellulose, hydroxypropylmethylcellulose or sodium carboxymethylcellulose, or a mixture thereof.
  • Eye drops as substances that maintain the pH of the medium contain an acetate or citrate, or phosphate, or borate buffer, or a mixture thereof.
  • Eye drops as a stabilizer of biological properties and / or resistance to contamination by microorganisms contain quaternary ammonium compounds or nipagin, or boric acid, or chlorhexidine, or methyl paraben.
  • eye drops contain one of the following substances or their derivatives: aethonium, benzethonium chloride or benzalkonium chloride, or a mixture thereof.
  • Eye drops contain a stabilizer of physico-chemical properties (antioxidant): Trilon B or butylated hydroxytoluene in the amount of 0.0001 - 0.1 g in 1 ml of solution.
  • eye drops contain one of the following substances: sodium chloride, dextrose, sodium nitrate or sodium sulfate, or a mixture thereof.
  • the choice of a reduced dosage of the active ingredient is determined depending on the values of the optimal viscosity range of the solution (within 5–100 mm 2 / s) and the pH of the medium (within 3.5–8.5) of the eye drops.
  • eye drops are proposed containing, as an active component, a serotonin receptor antagonist in a wider range of reduced dosage, according to the invention, they also additionally contain auxiliary components that increase the therapeutic effect of the active component: substances that provide the viscosity of the medium (prolongator), substances that support medium pH (pH regulator), stabilizer of biological, physico-chemical properties and/or resistance to contamination by microorganisms.
  • auxiliary components that increase the therapeutic effect of the active component: substances that provide the viscosity of the medium (prolongator), substances that support medium pH (pH regulator), stabilizer of biological, physico-chemical properties and/or resistance to contamination by microorganisms.
  • a positive effect of the invention is the creation of improved eye drops for the prevention and treatment of early manifestations of age-related nuclear cataracts, containing an extended range of reduced dosage of a serotonin receptor antagonist, which has a dosed preventive and therapeutic antidystrophic effect, which is due to the optimal physicochemical properties of the solution that promote penetration into the intraocular structures small doses of the active ingredient.
  • compositions make it possible to provide a dosed preventive and therapeutic antidystrophic effect of the reduced doses of the active component contained in them, as well as sterility and the necessary physicochemical properties of the solution (viscosity, pH, transparency, color).
  • MALTSEV Edward. Biological features and diseases of the lens. Odessa: Astroprint, 2002, ISBN 966-549-716-2, pages 448.
  • KORSAKOVA N.
  • bioamine profile of the lens in the conditions of the formation of different types of age-related cataracts in humans. Ophthalmosurgery. 2007, No. 3, pages 42-45, ISSN 0235-4160.
  • KORSAKOVA Immunohistochemical analysis of lens cells under conditions of formation of different types of age-related cataracts in humans. Morphology. 2007, Vol. 132, No. 5, pages 47-51, ISSN 1026-3543.
  • KORSAKOVA N. Immnohistochemical analysis of lens cells on formation of different types of age-related cataract in humans. Neuroscience and behavioral physiology. 2008, Vol.38, No.9, pages 887-890, ISSN 0097-0549. DOI: 10.1007/s11055-008-9066-6.
  • OGANEZOVA J. Catalin is an effective drug for the treatment of cataracts. breast cancer.
  • NAGAI N. Effect of disulfiram eye drops on lipid peroxide formation via excessive nitric oxide in lenses of hereditary cataract ICR/f rats. Biol. Pharm. Bull. 2008, Vol.31, No.5, pages 981-985, ISSN 1347-5215 (Electronic). DOI: 10.1248/bpb.31.981.

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  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Ophthalmology & Optometry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

L'invention se rapporte au domaine de la pharmacologie et concerne plus précisément la préparation de compositions à base d'antagoniste de récepteurs de sérotonine, qui peuvent être utilisées en ophtalmologie, en thérapie et en gériatrie. Ces gouttes oculaires comprennent, en qualité de composant actif, un antagoniste de récepteurs de sérotonine, notamment du dihydrate d'hydrochlorure d'ondansétron dans une plage plus large de dosage réduit, et comprennent également des excipients augmentant l'effet thérapeutique de faibles doses du composant actif. Le résultat technique consiste en la production de gouttes oculaires améliorées pour la prévention et le traitement d'occurrences précoces de la cataracte liée à l'âge de type nucléaire, lesquelles possèdent un spectre étendu de dosage réduit de l'antagoniste des récepteurs de sérotonine, possèdent une action anti-dystrophique préventive et thérapeutique dosée qui est liée à des propriétés physico-chimiques optimales de la solution, assurant la pénétration dans les structures intra-oculaires de faibles doses du composant actif.
PCT/RU2021/050244 2020-09-15 2021-07-27 Gouttes oculaires pour la prévention et le traitement de la cataracte liée à l'âge Ceased WO2022060251A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
RU2020130273A RU2748598C1 (ru) 2020-09-15 2020-09-15 Усовершенствованные глазные капли для профилактики и лечения ранних проявлений возрастной катаракты ядерного вида
RU2020130273 2020-09-15

Publications (1)

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WO2022060251A1 true WO2022060251A1 (fr) 2022-03-24

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RU (1) RU2748598C1 (fr)
WO (1) WO2022060251A1 (fr)

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1899304A (zh) * 2006-07-07 2007-01-24 中国科学院南海海洋研究所 一种白内障滴眼液及其制备方法
RU2411926C2 (ru) * 2009-01-13 2011-02-20 Надежда Витальевна Корсакова Способ консервативного лечения и профилактики ядерного вида возрастной катаракты
RU2536958C2 (ru) * 2012-11-14 2014-12-27 Открытое Акционерное Общество "Татхимфармпрепараты" Лекарственное средство для лечения катаракты и способ его получения (варианты)
RU2637875C2 (ru) * 2015-09-21 2017-12-07 Надежда Витальевна Корсакова Новые глазные капли для консервативного лечения и профилактики возрастной катаракты ядерного вида
RU2662364C2 (ru) * 2016-12-02 2018-07-25 Общество с ограниченной ответственностью "ПРОФИТ ФАРМ" Способ лечения катаракты и глазные капли для его осуществления

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1899304A (zh) * 2006-07-07 2007-01-24 中国科学院南海海洋研究所 一种白内障滴眼液及其制备方法
RU2411926C2 (ru) * 2009-01-13 2011-02-20 Надежда Витальевна Корсакова Способ консервативного лечения и профилактики ядерного вида возрастной катаракты
RU2536958C2 (ru) * 2012-11-14 2014-12-27 Открытое Акционерное Общество "Татхимфармпрепараты" Лекарственное средство для лечения катаракты и способ его получения (варианты)
RU2637875C2 (ru) * 2015-09-21 2017-12-07 Надежда Витальевна Корсакова Новые глазные капли для консервативного лечения и профилактики возрастной катаракты ядерного вида
RU2662364C2 (ru) * 2016-12-02 2018-07-25 Общество с ограниченной ответственностью "ПРОФИТ ФАРМ" Способ лечения катаракты и глазные капли для его осуществления

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