WO2014114124A1 - Composition d'entretien de lentille de contact cornéenne contenant un sel d'ammonium quaternaire de tréhalose - Google Patents

Composition d'entretien de lentille de contact cornéenne contenant un sel d'ammonium quaternaire de tréhalose Download PDF

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Publication number
WO2014114124A1
WO2014114124A1 PCT/CN2013/086855 CN2013086855W WO2014114124A1 WO 2014114124 A1 WO2014114124 A1 WO 2014114124A1 CN 2013086855 W CN2013086855 W CN 2013086855W WO 2014114124 A1 WO2014114124 A1 WO 2014114124A1
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WO
WIPO (PCT)
Prior art keywords
quaternary ammonium
ammonium salt
contact lens
chloride
agent
Prior art date
Application number
PCT/CN2013/086855
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English (en)
Chinese (zh)
Inventor
何坚
Original Assignee
江苏海伦隐形眼镜有限公司
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.)
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Application filed by 江苏海伦隐形眼镜有限公司 filed Critical 江苏海伦隐形眼镜有限公司
Publication of WO2014114124A1 publication Critical patent/WO2014114124A1/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
    • A61K9/0048—Eye, e.g. artificial tears
    • A61K9/0051—Ocular inserts, ocular implants
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N47/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid
    • A01N47/40—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having a double or triple bond to nitrogen, e.g. cyanates, cyanamides
    • A01N47/42—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having a double or triple bond to nitrogen, e.g. cyanates, cyanamides containing —N=CX2 groups, e.g. isothiourea
    • A01N47/44—Guanidine; Derivatives thereof
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Definitions

  • the present invention relates to a composition for contact lens care.
  • the composition is a contact lens care composition comprising a trehalose quaternary ammonium salt.
  • Contact lenses can be divided into hard, semi-rigid and soft.
  • Hard contact lenses are made of polymethyl methacrylate (PMMA) which is substantially impermeable to oxygen and siloxane and acrylate copolymerizable with oxygen.
  • the semi-rigid contact lens is made of silicone rubber that is permeable to oxygen and maintains normal breathing on the surface of the cornea.
  • a special wetting solution is used to maintain wetting to meet comfort and physiological requirements;
  • Soft contact lenses the most commonly used are lenses made of polyhydroxyethyl methacrylate (HEMA).
  • HEMA polyhydroxyethyl methacrylate
  • the HEMA molecule is a network structure, which makes the lens have the function of adsorbing and releasing low molecular liquid. The looser the lens network structure and the higher the water content, there are now more than a dozen soft contact lens lenses.
  • the existing soft contact lens has high hydrophilicity. Because the contact lens is worn in the eye, it is placed in front of the cornea, which hinders the contact of the cornea with the air and causes corneal hypoxia. In addition, the tear is wet except for the cornea. In addition to the conjunctiva, the lens is also wetted, resulting in a lack of tears, causing the lens wearer's eyes to dry up and sore.
  • Trehalose ( ct -D-glucopyranosyl - a -D-glucopyra-noside) is a stable non-reducing disaccharide composed of two pyranose glucose molecules linked to 1, 1-glycosidic bonds. Because trehalose is a non-reducing sugar composed of special disaccharide molecules, it is very stable and can form a special protective film on the cell surface under the harsh conditions of high temperature, cold, dryness and water loss, effectively protecting the biomolecular structure. Destroyed to maintain the life process and biological characteristics of the living body. Because trehalose has unique biological properties that protect biological cells and active substances from damage under adverse conditions such as drying, foreign researchers are actively studying trehalose derivatives and using them in contact lens care compositions. feasibility.
  • a contact lens care composition which is an aqueous solution comprising an isotonicity adjusting agent, a buffering agent, a complexing agent, a trehalose quaternary ammonium salt, a surfactant, and an antimicrobial agent. Storage, disinfection, cleaning, lubrication, moisturization and rewetting of the lens of the contact lens.
  • the contact lens is stored in the composition at the time of use or the above composition is added dropwise onto the contact lens or directly into the eye.
  • a contact lens care composition containing a trehalose quaternary ammonium salt which comprises, by weight percent, consisting of the following components:
  • the quaternary ammonium salt of the trehalose is 0. 001 - 2%, the isotonicity adjusting agent is 0.01 - 2%, the surfactant is 0. 05 - 2%, the complexing agent is 0.01-1%, and the buffering agent is 0. 01— 3%, the antimicrobial compound is 0. 00001—1%, and the water is 89-99. 91899%.
  • the above isotonicity adjusting agent is at least one of sodium chloride, potassium chloride, calcium chloride, magnesium chloride, monosaccharide of glucose, propylene glycol, glycerin, sorbitol, and mannitol.
  • the above surfactants may be Poloxamer, Poloxamines, Tylo Xa pol, polysorbate, sodium lauroyl glutamate, lauryl propyl hydroxy sulfoyl. At least one of betaine.
  • the above complexing agent is at least one of ethylenediaminetetraacetic acid, 2-amino-2-methyl-1-propanol (AMP-95), and N-dodecylamethylenediaminetriacetic acid.
  • the above buffering agent is at least one of boric acid, borax, disodium hydrogen phosphate, sodium dihydrogen phosphate, citric acid, sodium citrate, and tromethamine (TRIS AMINO).
  • the above antimicrobial agents are Polyquaternium-1, polyhexamethylene biguanide ( P), polyaminopropyl biguanide (PAPB), and alexidine (Alexidine). And at least one of benzalkonium chloride, benzethonium chloride, cetylpyridinium chloride, and sorbic acid.
  • the method for preparing the care solution composition of the present invention is: putting the above components into water in order of weight percentage Dissolve, adjust the pH with NaOH and hydrochloric acid at 6.5-7.8, osmotic pressure at 260-340 mosm/Kg* 3 ⁇ 40, and sterilize the solution through a 0.22 ⁇ m pore size membrane filter.
  • the invention has the functions of storage, disinfection, cleaning, lubrication, moisturizing and anti-drying of the contact lens, which is effective for relieving dryness and soreness of the eye, reducing the mortality of the corneal epithelial cells in a dry environment, promoting the corneal epithelium and Repair of intradermal cells.
  • the killing rate of each composition against Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus was more than 99.9%, and the killing rate against Candida albicans and Fusarium solani was greater than 90.0%.
  • a contact lens care composition containing a trehalose quaternary ammonium salt consisting of the following components by weight: trehalose quaternary ammonium salt content 0.001-2%, isotonicity adjusting agent content 0.01-2%, surfactant The content is 0.05-2%, the complexing agent content is 0.01-1%, the buffering agent content is 0.01-3%, the antimicrobial compound content is 0.00001-1%, and the water is 89-99.91899%.
  • isotonicity adjusting agent sodium chloride 0.36%
  • surfactant poloxamer 0.2%
  • complexing agent disodium edetate 0.1%
  • Buffer 0.64% boric acid
  • antimicrobial agent polyhexamethylene biguanide (PHMB) 0.000018%
  • water 96 ⁇ 569992% water 96 ⁇ 569992%.
  • the osmotic pressure is 260-340 mosm/Kg.
  • the osmotic pressure is 260-340 mosm/Kg.
  • the osmotic pressure is 260-340 mosm/Kg. * 0,
  • the solution was sterilized by a membrane filter of 0.22 ⁇ m pore size.
  • the contact lens is immersed in the composition during use or the above composition is added dropwise onto the contact lens or directly into the eye.
  • compositions of different schemes have been tested, indicating that the compositions containing different levels of trehalose quaternary ammonium salt have a moisturizing and anti-drying effect proportional to the amount used.
  • 001— 8 % ( Indeed, the preferred amount of trehalose quaternary ammonium salt in the composition of the present invention is 0.001 - 8 %.
  • the compositions of the present invention are suitable for disinfecting a soaked contact lens, and thus the preferred composition further comprises at least one antimicrobial agent. Since the contact lens of the composition is placed directly into the eye, the antimicrobial agent should be in good biocompatibility with the eye. In conventional contact lens soaking and disinfecting solutions, the antimicrobial is present in an amount effective to disinfect the contact lens, and the preferred amount of disinfection is to reduce the microbial load at a certain logarithmic level over time.
  • the bactericidal efficiency was tested for different compositions prepared according to the method, and the bactericidal efficiency tests were carried out on Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Candida albicans, and Fusarium solani. As a result, each composition was against Escherichia coli.
  • the killing rate of Pseudomonas aeruginosa and Staphylococcus aureus is greater than 99.0%, and the killing rate of Candida albicans and Solanum blazei is greater than 90.0%.
  • the pH of the composition of the present invention is compatible with the eye, a suitable pH of about 6. 5 - 7. 8, preferably in the 6. 8-7.
  • the composition of the present invention is suitable for contact lens cleaning, disinfection, lubrication, moisturizing, storage, relieving dry eyes and soreness, effectively reducing the mortality of corneal cells in a dry environment, and promoting Repair of corneal epithelium and intradermal cells.
  • a complexing agent is added to the composition of the present invention, and the complexing agent is combined with heavy metal ions.
  • the composition of the present invention needs to be a solution which is isotonic with eye liquid.
  • the composition has an osmotic pressure of about 260 - 340 mosm / Kg * H 2 0 , more preferably an osmotic pressure of 280 - 320 mosm / Kg * H 2 0.
  • composition of the present invention comprises an anti-drying humectant, and the anti-drying humectant is a trehalose quaternary ammonium salt to ensure that the eye dryness and soreness are alleviated during use.
  • the quaternary ammonium salt of trehalose is very stable in chemical properties, and has great research progress in eye liquid preparation, dry eye treatment, corneal preservation and the like.
  • composition of the present invention comprises a surfactant, which may be a cationic surfactant, an anionic surfactant, a nonionic surfactant, an amphoteric surfactant, which surfactant is not irritated to the eye, and has good Eye compatibility, this substance primarily removes contaminants from contact lenses.
  • a surfactant which may be a cationic surfactant, an anionic surfactant, a nonionic surfactant, an amphoteric surfactant, which surfactant is not irritated to the eye, and has good Eye compatibility, this substance primarily removes contaminants from contact lenses.
  • the animal test of the present invention shows that the composition of the present invention is biocompatible, has no systemic toxicity and is irritating to animal conjunctiva and iris and corneal tissue.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pest Control & Pesticides (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Ophthalmology & Optometry (AREA)
  • Agronomy & Crop Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Plant Pathology (AREA)
  • Engineering & Computer Science (AREA)
  • Dentistry (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Environmental Sciences (AREA)
  • Detergent Compositions (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne une composition d'entretien de lentille de contact cornéenne contenant un sel d'ammonium quaternaire de tréhalose qui comprend les pourcentages en poids de composant suivants : un sel d'ammonium quaternaire de tréhalose de 0,001 à 2 %, un régulateur isotonique de 0,01 à 2 %, un tensioactif de 0,05 à 2 %, un agent complexant de 0,01 à 1 %, un tampon de 0,01 à 3 %, un composé antimicrobien de 0,00001 à 1 % et de l'eau de 89 à 99,91899 %. La composition est utilisée pour stocker, stériliser, nettoyer, lubrifier, et hydrater des lentilles de contact cornéennes, a une fonction de résistance à la sécheresse, est efficace pour soulager la sécheresse et la rigidité des yeux, peut réduire le taux de mortalité des cellules épithéliales cornéennes dans un environnement sec, et stimule la réparation de cellules épithéliales et endothéliales cornéennes. Le taux d'élimination de chaque composition d'Escherichia coli, Pseudomonas aeruginosa et Staphylococcus aureus est supérieur à 99,9 %, et le taux d'élimination de Candida albicans et Solanaceae fusarium est supérieur à 90,0 %.
PCT/CN2013/086855 2013-01-23 2013-11-11 Composition d'entretien de lentille de contact cornéenne contenant un sel d'ammonium quaternaire de tréhalose WO2014114124A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201310023843.9 2013-01-23
CN2013100238439A CN103083710A (zh) 2013-01-23 2013-01-23 含海藻糖季铵盐的角膜接触镜护理组合物

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WO2014114124A1 true WO2014114124A1 (fr) 2014-07-31

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023229667A1 (fr) * 2022-05-24 2023-11-30 The Cleveland Clinic Foundation Agents bloquants topiques de récepteur de l'angiotensine ii (arbs) destinés au traitement d'affections oculaires
WO2024089166A1 (fr) * 2022-10-26 2024-05-02 Bausch + Lomb Ireland Limited Solution de traitement de lentilles de contact

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103083710A (zh) * 2013-01-23 2013-05-08 江苏海伦隐形眼镜有限公司 含海藻糖季铵盐的角膜接触镜护理组合物
CN105031705A (zh) * 2015-06-24 2015-11-11 黄红林 一种隐形眼镜消毒保湿药水
JPWO2017077655A1 (ja) * 2015-11-06 2018-08-16 株式会社Ｊｃｕ ニッケルめっき用添加剤およびこれを含有するサテンニッケルめっき浴
CN109722347B (zh) * 2019-01-03 2020-12-29 山东省药学科学院 一种含有黄原胶的保湿润滑组合物及其应用
CN113144207A (zh) * 2021-02-07 2021-07-23 山西利普达医药科技有限公司 一种包括聚季铵盐-1的组合物及其应用
IT202100017396A1 (it) * 2021-07-01 2023-01-01 Azienda Unita Sanitaria Locale Della Romagna Metodica di conservazione a temperatura ambiente di tessuti e organi destinati all’uso clinico

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101343293A (zh) * 2008-08-22 2009-01-14 烟台海岸带可持续发展研究所 一种采用海藻糖季铵盐的吸湿保湿剂及其制备方法
WO2009113161A1 (fr) * 2008-03-12 2009-09-17 株式会社メニコン Composition de solution pour des lentilles de contact
CN101691478A (zh) * 2009-09-25 2010-04-07 海昌隐形眼镜有限公司 含海藻糖的角膜接触镜护理组合物及其制备方法
CN101691479A (zh) * 2009-09-25 2010-04-07 海昌隐形眼镜有限公司 一种角膜接触镜保存液组合物及其制备方法
WO2011070613A1 (fr) * 2009-12-08 2011-06-16 株式会社メニコン Composition pour lentilles de contact et procédé pour supprimer une interaction négative l'utilisant
CN103083710A (zh) * 2013-01-23 2013-05-08 江苏海伦隐形眼镜有限公司 含海藻糖季铵盐的角膜接触镜护理组合物

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009113161A1 (fr) * 2008-03-12 2009-09-17 株式会社メニコン Composition de solution pour des lentilles de contact
CN101343293A (zh) * 2008-08-22 2009-01-14 烟台海岸带可持续发展研究所 一种采用海藻糖季铵盐的吸湿保湿剂及其制备方法
CN101691478A (zh) * 2009-09-25 2010-04-07 海昌隐形眼镜有限公司 含海藻糖的角膜接触镜护理组合物及其制备方法
CN101691479A (zh) * 2009-09-25 2010-04-07 海昌隐形眼镜有限公司 一种角膜接触镜保存液组合物及其制备方法
WO2011070613A1 (fr) * 2009-12-08 2011-06-16 株式会社メニコン Composition pour lentilles de contact et procédé pour supprimer une interaction négative l'utilisant
CN103083710A (zh) * 2013-01-23 2013-05-08 江苏海伦隐形眼镜有限公司 含海藻糖季铵盐的角膜接触镜护理组合物

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023229667A1 (fr) * 2022-05-24 2023-11-30 The Cleveland Clinic Foundation Agents bloquants topiques de récepteur de l'angiotensine ii (arbs) destinés au traitement d'affections oculaires
WO2024089166A1 (fr) * 2022-10-26 2024-05-02 Bausch + Lomb Ireland Limited Solution de traitement de lentilles de contact

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