TW202320811A - Eyewash composition - Google Patents

Eyewash composition Download PDF

Info

Publication number
TW202320811A
TW202320811A TW111129138A TW111129138A TW202320811A TW 202320811 A TW202320811 A TW 202320811A TW 111129138 A TW111129138 A TW 111129138A TW 111129138 A TW111129138 A TW 111129138A TW 202320811 A TW202320811 A TW 202320811A
Authority
TW
Taiwan
Prior art keywords
composition
eyewash
salts
present disclosure
acid
Prior art date
Application number
TW111129138A
Other languages
Chinese (zh)
Inventor
見目晃平
Original Assignee
日商小林製藥股份有限公司
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.)
Filing date
Publication date
Application filed by 日商小林製藥股份有限公司 filed Critical 日商小林製藥股份有限公司
Publication of TW202320811A publication Critical patent/TW202320811A/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4415Pyridoxine, i.e. Vitamin B6
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726Glycosaminoglycans, i.e. mucopolysaccharides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726Glycosaminoglycans, i.e. mucopolysaccharides
    • A61K31/728Hyaluronic acid
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material 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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Ophthalmology & Optometry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

To provide an eyewash composition that contains propylene glycol but yet has excellent antiseptic properties. An eyewash composition contains 0.01 w/v% or more of at least one selected from the group consisting of hyaluronic acid and salts thereof and propylene glycol but does not contain an antiseptic agent selected from quaternary ammonium salt-based antiseptics, paraoxybenzoates, chlorobutanol, and sorbic acids.

Description

洗眼用組成物Composition for eyewash

本發明是有關於一種洗眼用組成物。The present invention relates to an eyewash composition.

關於洗眼藥的滲透壓,認為理想的是調整為接近淚液的值,且作為其等張化劑而大多調配丙二醇。但是,若調配丙二醇,則有防腐性劣化的問題。另一方面,已知有藉由使用如氯化苯銨(benzalkonium chloride)般的防腐劑來提高防腐性的情況(專利文獻1),但擔心其對角膜的影響或向隱形眼鏡的吸附,並不希望使用防腐劑。 [現有技術文獻] [專利文獻] It is thought that the osmotic pressure of the eyewash is preferably adjusted to a value close to tear fluid, and propylene glycol is often formulated as the isotonic agent. However, when propylene glycol is blended, there is a problem of deterioration of corrosion resistance. On the other hand, it is known that antiseptic properties are improved by using preservatives such as benzalkonium chloride (Patent Document 1), but there are concerns about its influence on the cornea or adsorption to contact lenses, and The use of preservatives is undesirable. [Prior art literature] [Patent Document]

[專利文獻1]日本專利特開2012-167095號公報[Patent Document 1] Japanese Patent Laid-Open No. 2012-167095

[發明所欲解決之課題] 因此,本發明者的目的在於提供一種於調配有丙二醇的同時防腐性亦優異的洗眼用組成物。 [Problem to be Solved by the Invention] Therefore, an object of the inventors of the present invention is to provide an eyewash composition that is excellent in antiseptic properties while blending propylene glycol.

[解決課題之手段] 本發明者鑒於上述課題進行了努力研究,結果發現,藉由在洗眼用組成物中與丙二醇組合使用0.01 w/v%以上的玻尿酸(hyaluronic acid),儘管未調配防腐劑、且儘管調配有丙二醇,亦可對洗眼用組成物賦予防腐性。本發明是於該見解的基礎上經進一步反覆研究後完成的,且為以下所揭示者。 項1.一種洗眼用組成物,含有:(A)0.01 w/v%以上的選自由玻尿酸及其鹽所組成的群組中的至少一種、以及(B)丙二醇,且不含有選自四級銨鹽系防腐劑、對羥基苯甲酸酯類、氯丁醇及山梨酸類中的防腐劑。 項2.如項1所述的洗眼用組成物,更含有(C)0.05 w/v%以上的選自由依地酸(edetic acid)及其鹽所組成的群組中的至少一種。 項3.如項1或項2所述的洗眼用組成物,更含有(D)選自由吡哆醇、硫酸軟骨素及該些的鹽所組成的群組中的至少一種。 項4.如項1至項3中任一項所述的洗眼組成物,於佩戴隱形眼鏡的過程中使用。 [Means to solve the problem] The inventors of the present invention conducted diligent research in view of the above-mentioned problems, and as a result, found that by using 0.01 w/v% or more hyaluronic acid in combination with propylene glycol in an eyewash composition, even though no preservative was formulated and propylene glycol was formulated, , Antiseptic properties can also be imparted to the eyewash composition. The present invention has been accomplished after further studies based on this finding, and is disclosed below. Item 1. An eyewash composition containing: (A) 0.01 w/v% or more of at least one selected from the group consisting of hyaluronic acid and its salts, and (B) propylene glycol, and does not contain Ammonium salt-based preservatives, parabens, chlorobutanol and sorbic acid preservatives. Item 2. The eyewash composition according to Item 1, further comprising (C) 0.05 w/v% or more of at least one selected from the group consisting of edetic acid and its salts. Item 3. The eyewash composition according to Item 1 or Item 2, further comprising (D) at least one selected from the group consisting of pyridoxine, chondroitin sulfate, and salts thereof. Item 4. The eyewash composition according to any one of Items 1 to 3, which is used during wearing of contact lenses.

[發明的效果] 藉由將0.01 w/v%以上的選自由玻尿酸及其鹽所組成的群組中的至少一種與丙二醇組合使用,可提供一種即使不含有選自四級銨鹽系防腐劑、對羥基苯甲酸酯類、氯丁醇及山梨酸類中的防腐劑,防腐性亦優異的洗眼用組成物。 [Effect of the invention] By using 0.01 w/v% or more of at least one selected from the group consisting of hyaluronic acid and its salts in combination with propylene glycol, it is possible to provide a A preservative among esters, chlorobutanol, and sorbic acid, and an eyewash composition with excellent antiseptic properties.

以下,對本揭示中包含的實施形態進一步進行詳細說明。Hereinafter, the embodiments included in the present disclosure will be described in more detail.

本揭示包含一種洗眼用組成物,其含有0.01 w/v%以上的選自由玻尿酸及其鹽所組成的群組中的至少一種、以及丙二醇,且不含有選自四級銨鹽系防腐劑、對羥基苯甲酸酯類、氯丁醇及山梨酸類中的防腐劑。The disclosure includes an eyewash composition, which contains at least 0.01 w/v% of at least one selected from the group consisting of hyaluronic acid and its salts, and propylene glycol, and does not contain quaternary ammonium salt-based preservatives, Preservatives in parabens, chlorobutanol and sorbic acid.

選自由玻尿酸及其鹽所組成的群組中的至少一種(有時稱為成分(A))是現有公知的物質,作為玻尿酸的鹽,較佳可例示鈉鹽等鹼金屬鹽等。該些可單獨使用一種,亦可組合使用兩種以上。At least one selected from the group consisting of hyaluronic acid and its salts (sometimes referred to as component (A)) is a conventionally known substance, and examples of the salt of hyaluronic acid preferably include alkali metal salts such as sodium salts, and the like. These may be used alone or in combination of two or more.

成分(A)的含量只要於本揭示的洗眼用組成物中為0.01 w/v%以上,則不受限制,較佳可例示為0.01 w/v%~0.08 w/v%,更佳可例示為0.01 w/v%~0.02 w/v%,進而較佳可例示為0.015 w/v%~0.02 w/v%。The content of component (A) is not limited as long as it is 0.01 w/v% or more in the eyewash composition of the present disclosure, preferably 0.01 w/v% to 0.08 w/v%, more preferably exemplified It is 0.01 w/v% - 0.02 w/v%, and more preferably, it is 0.015 w/v% - 0.02 w/v%.

丙二醇(有時稱為成分(B))為現有公知的。丙二醇的含量只要可獲得本揭示的效果,則不受限制,但於該洗眼用組成物中,較佳可例示為0.01 w/v%~2 w/v%,更佳可例示為0.05 w/v%~1.5 w/v%,進而較佳可例示為0.1 w/v%~1 w/v%。另外,丙二醇的含量只要可獲得本揭示的效果,則不受限制,但於該洗眼用組成物中,相對於成分(A)1質量份,較佳可例示為1質量份~100質量份,更佳可例示為10質量份~55質量份,進而較佳可例示為20質量份~50質量份。Propylene glycol (sometimes referred to as ingredient (B)) is conventionally known. The content of propylene glycol is not limited as long as the effect of the present disclosure can be obtained, but in the eyewash composition, preferably 0.01 w/v% to 2 w/v%, more preferably 0.05 w/v% v% - 1.5 w/v%, more preferably 0.1 w/v% - 1 w/v%. In addition, the content of propylene glycol is not limited as long as the effects of the present disclosure can be obtained, but in the eyewash composition, preferably 1 to 100 parts by mass is exemplified with respect to 1 part by mass of component (A), More preferably, it is 10-55 mass parts, More preferably, it is 20-50 mass parts.

本揭示的洗眼用組成物不含有選自四級銨鹽系防腐劑、對羥基苯甲酸酯類、氯丁醇及山梨酸類中的防腐劑。該防腐劑是於滴眼、洗眼領域中現有公知的防腐劑。作為四級銨系防腐劑,可例示氯化苯銨、氯化苯釷(benzethonium chloride)等。作為對羥基苯甲酸酯類,可例示:對羥基苯甲酸甲酯、對羥基苯甲酸丙酯、對羥基苯甲酸丁酯等對羥基苯甲酸酯;對羥基苯甲酸酯的鹽(鈉鹽等鹼金屬鹽等)等。作為山梨酸類,可例示山梨酸、山梨酸的鹽(鈉鹽、鉀鹽等鹼金屬鹽;鈣鹽、鎂鹽等鹼土金屬等)等。The eyewash composition disclosed herein does not contain preservatives selected from quaternary ammonium preservatives, parabens, chlorobutanol and sorbic acid. The preservative is a known preservative in the fields of eye drops and eye washes. Examples of the quaternary ammonium preservative include aniline ammonium chloride, benzothorium chloride (benzethonium chloride), and the like. Examples of parabens include: parabens such as methyl paraben, propyl paraben, and butyl paraben; salts of parabens (sodium salts) Alkali metal salts, etc.) etc. Examples of sorbic acids include sorbic acid and salts of sorbic acid (alkali metal salts such as sodium salts and potassium salts; alkaline earth metal salts such as calcium salts and magnesium salts, etc.) and the like.

本揭示的洗眼用組成物可更含有選自由依地酸及其鹽所組成的群組中的至少一種(有時稱為成分(C))。依地酸亦稱為乙二胺四乙酸(ethylene diamine tetraacetic acid,EDTA),且為現有公知的。作為依地酸的鹽,可例示:依地酸單鈉、依地酸二鈉、依地酸三鈉、依地酸四鈉、依地酸二鉀、依地酸三鉀、依地四鉀等(包含水合物)。該些可單獨使用一種,亦可組合使用兩種以上。The eyewash composition of the present disclosure may further contain at least one selected from the group consisting of edetic acid and its salts (sometimes referred to as component (C)). Edetic acid is also known as ethylene diamine tetraacetic acid (EDTA), and is conventionally known. Examples of salts of edetate include monosodium edetate, disodium edetate, trisodium edetate, tetrasodium edetate, dipotassium edetate, tripotassium edetate, and tetrapotassium edetate etc. (including hydrates). These may be used alone or in combination of two or more.

在本揭示的洗眼用組成物含有成分(C)的情況下,其含量只要可獲得本揭示的效果,則不受限制,但於該洗眼用組成物中,成分(C)可例示為0.02 w/v%以上,較佳可例示為0.05 w/v%以上,更佳可例示為0.05 w/v%~0.1 w/v%,進而較佳可例示為0.05 w/v%~0.08 w/v%。另外,成分(C)的含量只要可獲得本揭示的效果,則不受限制,但於該洗眼用組成物中,相對於成分(A)1質量份,較佳可例示為1質量份~8質量份,更佳可例示為2質量份~6質量份,進而較佳可例示為2.5質量份~5質量份。When the eyewash composition of the present disclosure contains component (C), the content is not limited as long as the effect of the present disclosure can be obtained, but in the eyewash composition, the component (C) can be exemplified at 0.02w /v% or more, preferably 0.05 w/v% or more, more preferably 0.05 w/v% to 0.1 w/v%, more preferably 0.05 w/v% to 0.08 w/v %. In addition, the content of the component (C) is not limited as long as the effect of the present disclosure can be obtained, but in the eyewash composition, preferably 1 to 8 parts by mass is exemplified with respect to 1 part by mass of the component (A). Parts by mass are more preferably 2 to 6 parts by mass, and more preferably 2.5 to 5 parts by mass.

本揭示的洗眼用組成物可更含有選自由吡哆醇、硫酸軟骨素及該些的鹽所組成的群組中的至少一種(有時稱為成分(D))。The eyewash composition of the present disclosure may further contain at least one selected from the group consisting of pyridoxine, chondroitin sulfate, and salts thereof (sometimes referred to as component (D)).

吡哆醇及其鹽為公知的物質且不受限制,但作為吡哆醇的鹽,可例示鹽酸鹽(鹽酸吡哆醇)、磷酸鹽等無機酸鹽。Pyridoxine and salts thereof are known substances and are not limited, but examples of pyridoxine salts include inorganic acid salts such as hydrochloride (pyridoxine hydrochloride) and phosphate.

硫酸軟骨素是具有硫酸和D-葡萄糖醛酸與N-乙醯基半乳胺糖此兩糖重覆的糖鏈進行酯鍵結而成的結構的黏多醣(mucopolysaccharide)。作為硫酸軟骨素的鹽,對本發明並無限制,但可例示:鈉鹽、鉀鹽等鹼金屬鹽;鎂鹽、鈣鹽等鹼土金屬鹽等。雖對本發明並無限制,但作為硫酸軟骨素的鹽,較佳可例示軟骨素硫酸酯鈉等。Chondroitin sulfate is a mucopolysaccharide having a structure in which sulfuric acid, D-glucuronic acid, and N-acetylgalactamine sugar, two repeating sugar chains, are ester-bonded. The salt of chondroitin sulfate is not limited to the present invention, and examples thereof include alkali metal salts such as sodium salts and potassium salts; alkaline earth metal salts such as magnesium salts and calcium salts; and the like. Although the present invention is not limited, as the salt of chondroitin sulfate, sodium chondroitin sulfate and the like can be exemplified preferably.

本揭示中使用的硫酸軟骨素或其鹽於以上範圍內不受限制,但作為其分子量,重量平均分子量較佳可例示為0.5萬~4.5萬左右,更佳可例示為1萬~4萬左右,進而較佳可例示為1.5萬~3萬左右。重量平均分子量可藉由凝膠過濾層析法來測定。硫酸軟骨素或其鹽已有市售,例如以商品名日本藥局方外醫藥品規格硫酸軟骨素鈉(生化學工業股份有限公司製造,重量平均分子量20000)銷售。Chondroitin sulfate or a salt thereof used in the present disclosure is not limited within the above range, but as its molecular weight, the weight average molecular weight is preferably about 5,000 to 45,000, more preferably about 10,000 to 40,000 , and more preferably about 15,000 to 30,000. The weight average molecular weight can be determined by gel filtration chromatography. Chondroitin sulfate or a salt thereof is commercially available, for example, under the trade name of Japanese Pharmacopoeia Prescription Chondroitin Sulfate Sodium (manufactured by Seikagaku Kogyo Co., Ltd., weight average molecular weight: 20,000).

吡哆醇或其鹽、硫酸軟骨素或其鹽可單獨使用一種,亦可組合使用兩種以上。Pyridoxine or its salt, chondroitin sulfate or its salt may be used alone or in combination of two or more.

在本揭示的洗眼用組成物含有成分(D)的情況下,其含量只要可獲得本揭示的效果,則不受限制,但於該洗眼用組成物中,成分(D)較佳可例示為0.001 w/v%~0.1 w/v%,更佳可例示為0.01 w/v%~0.07 w/v%,進而較佳可例示為0.04 w/v%~0.06 w/v%。另外,成分(D)的含量只要可獲得本揭示的效果,則不受限制,但於該洗眼用組成物中,相對於成分(A)1質量份,較佳可例示為1質量份~10質量份,更佳可例示為2質量份~6質量份,進而較佳可例示為2質量份~4質量份。When the eyewash composition of the present disclosure contains component (D), the content is not limited as long as the effect of the present disclosure can be obtained, but in the eyewash composition, component (D) is preferably exemplified as 0.001 w/v% - 0.1 w/v%, more preferably 0.01 w/v% - 0.07 w/v%, more preferably 0.04 w/v% - 0.06 w/v%. In addition, the content of the component (D) is not limited as long as the effect of the present disclosure can be obtained, but in the eyewash composition, preferably 1 to 10 parts by mass is exemplified with respect to 1 part by mass of the component (A). Parts by mass are more preferably 2 to 6 parts by mass, and more preferably 2 to 4 parts by mass.

另外,雖對本揭示並無限制,但選自由吡哆醇及其鹽所組成的群組中的至少一種於該洗眼用組成物中更佳可例示為0.008 w/v%~0.01 w/v%,進而較佳可例示為0.001 w/v%~0.01 w/v%,特佳可例示為0.005 w/v%~0.01 w/v%。In addition, although the present disclosure is not limited, at least one selected from the group consisting of pyridoxine and its salts is more preferably 0.008 w/v% to 0.01 w/v% in the eyewash composition , and more preferably 0.001 w/v% to 0.01 w/v%, particularly preferably 0.005 w/v% to 0.01 w/v%.

另外,雖對本揭示並無限制,但選自由硫酸軟骨素及其鹽所組成的群組中的至少一種於該洗眼用組成物中更佳可例示為0.0055 w/v%~0.05 w/v%,進而較佳可例示為0.01 w/v%~0.05 w/v%,特佳可例示為0.025 w/v%~0.05 w/v%。In addition, although the present disclosure is not limited, at least one selected from the group consisting of chondroitin sulfate and its salts is more preferably 0.0055 w/v% to 0.05 w/v% in the eyewash composition , and more preferably 0.01 w/v% to 0.05 w/v%, particularly preferably 0.025 w/v% to 0.05 w/v%.

本揭示的洗眼用組成物可更含有在滴眼或洗眼的用途中能夠容許的任意其他成分。雖對本揭示並無限制,但作為所述其他成分,可例示:緩衝劑、穩定劑、等張化劑、溶劑(水等)、pH調節劑、藥效成分、清涼劑、刺激劑、增稠劑等。所述其他成分以不妨礙本揭示的效果為限度且根據目的等適宜選擇即可,可單獨使用一種,亦可組合使用兩種以上,其調配量亦適宜決定即可。再者,所述成分(A)~成分(D)根據其成分而例如亦已知為藥效成分、穩定劑、增稠劑等,但於本揭示中,所述成分(A)~成分(D)不包含於所述任意其他成分中。The eyewash composition of the present disclosure may further contain any other ingredients that are acceptable for eye drops or eyewashes. Although the present disclosure is not limited, examples of the other components include buffers, stabilizers, isotonic agents, solvents (water, etc.), pH regulators, medicinal ingredients, cooling agents, stimulants, thickeners, etc. agent etc. Such other components may be appropriately selected according to purposes and the like as long as they do not interfere with the effects of the present disclosure. One type may be used alone or two or more types may be used in combination, and the compounding amount may be appropriately determined. Furthermore, the components (A) to (D) are also known as medicinal ingredients, stabilizers, thickeners, etc. according to their components, but in this disclosure, the components (A) to ( D) is not contained in any of the other ingredients.

作為所述其他成分的一例,可列舉緩衝劑,作為緩衝劑,可例示硼酸、硼砂等。緩衝劑可單獨使用一種,亦可組合使用兩種以上。例如,於所述組成物含有硼酸的情況下,硼酸的含量只要不妨礙本揭示的效果,則不受限制,於所述組成物中,較佳可例示為0.1 w/v%~2.5 w/v%,更佳可例示為0.5 w/v%~2 w/v%。例如,於所述組成物含有硼砂的情況下,硼砂的含量只要不妨礙本揭示的效果,則不受限制,於所述組成物中,較佳可例示為0.005 w/v%~0.5 w/v%,更佳可例示為0.005 w/v%~0.05 w/v%。所述組成物可含有硼酸、硼砂以外的緩衝劑,亦可不含有硼酸、硼砂以外的緩衝劑。另外,所述組成物亦可調配硼酸或硼砂中的僅任一者。A buffer agent is mentioned as an example of the said other component, Boric acid, borax, etc. are illustrated as a buffer agent. A buffer may be used alone or in combination of two or more. For example, when the composition contains boric acid, the content of boric acid is not limited as long as it does not hinder the effect of the present disclosure. In the composition, it is preferably 0.1 w/v% to 2.5 w/ v%, more preferably 0.5 w/v% to 2 w/v%. For example, when the composition contains borax, the content of borax is not limited as long as it does not hinder the effect of the present disclosure. In the composition, it is preferably 0.005 w/v% to 0.5 w/ v%, more preferably 0.005 w/v% to 0.05 w/v%. The composition may contain buffers other than boric acid and borax, or may not contain buffers other than boric acid and borax. In addition, only any one of boric acid and borax may be prepared in the composition.

當作為所述其他成分的一例而列舉穩定劑時,作為穩定劑,可例示:聚山梨醇酯(聚山梨醇酯80、聚山梨醇酯60等)、聚氧乙烯(polyoxyethylene,POE)硬化蓖麻油(POE(80)硬化蓖麻油、POE(60)硬化蓖麻油等,括弧內的數字是指氧化乙烯的平均加成莫耳數)、POE聚氧丙二醇、胺基丁三醇(trometamol)等。該些可單獨使用一種,亦可組合使用兩種以上。於所述組成物含有穩定劑的情況下,其含量只要不妨礙本揭示的效果,則不受限制,於所述組成物中,較佳可例示為0.01 w/v%~1 w/v%,更佳可例示為0.05 w/v%~0.1 w/v%。於所述組成物含有穩定劑的情況下,例如可含有選自聚山梨醇酯、POE硬化蓖麻油、POE聚氧丙二醇及胺基丁三醇中的僅任一種,或者可含有僅兩種,另外,例如於含有聚山梨醇酯的情況下,亦可不調配POE硬化蓖麻油、POE聚丙二醇及/或胺基丁三醇而進行製備。When a stabilizer is mentioned as an example of the other components, examples of the stabilizer include: polysorbate (polysorbate 80, polysorbate 60, etc.), polyoxyethylene (polyoxyethylene, POE) hardened castor Sesame oil (POE (80) hardened castor oil, POE (60) hardened castor oil, etc., the numbers in brackets refer to the average added moles of ethylene oxide), POE polyoxypropylene glycol, trometamol, etc. . These may be used alone or in combination of two or more. When the composition contains a stabilizer, its content is not limited as long as it does not hinder the effect of the present disclosure. In the composition, it is preferably 0.01 w/v% to 1 w/v% , more preferably 0.05 w/v% to 0.1 w/v%. In the case where the composition contains a stabilizer, for example, only one selected from polysorbate, POE hardened castor oil, POE polyoxypropylene glycol, and tromethamine may be included, or only two kinds thereof may be included, Moreover, for example, when polysorbate is contained, it can also prepare without compounding POE hardened castor oil, POE polypropylene glycol, and/or tromethamine.

當作為其他成分的一例而列舉藥效成分時,作為藥效成分,可列舉:胺基酸類、抗炎劑、維生素類、抗組胺劑等。該些可單獨使用一種,亦可組合使用兩種以上。When a medicinal ingredient is mentioned as an example of other ingredients, amino acids, an anti-inflammatory agent, vitamins, an antihistamine, etc. are mentioned as a medicinal ingredient. These may be used alone or in combination of two or more.

雖對本揭示並無限制,但例如作為胺基酸類,可例示:麩胺酸及其鹽等胺基酸及其鹽;牛磺酸等胺基酸類似物等。該些可單獨使用一種,亦可組合使用兩種以上。本揭示的洗眼用組成物亦可不調配胺基酸及/或其鹽來製備。此處提及的所謂胺基酸是指能夠形成具有胺基與羧基此兩個官能基的蛋白質的結構單元的胺基酸,例如包含L-天冬胺酸等。另外,本揭示的洗眼用組成物亦可不調配胺基酸類似物來製備。Although the present disclosure is not limited, for example, as amino acids, amino acids such as glutamic acid and its salts, salts thereof; amino acid analogs such as taurine, and the like can be illustrated. These may be used alone or in combination of two or more. The eyewash composition disclosed herein can also be prepared without formulating amino acids and/or salts thereof. The so-called amino acid mentioned here refers to an amino acid capable of forming a structural unit of a protein having two functional groups of an amino group and a carboxyl group, for example including L-aspartic acid and the like. In addition, the eyewash composition of the present disclosure can also be prepared without formulating amino acid analogues.

雖對本揭示並無限制,但例如作為抗炎劑,可例示:硫酸鋅、乳酸鋅、ε-胺基己酸、尿囊素、甘草苷酸(glycyrrhizic acid)及其鹽、甘菊藍(azulene)類(甘菊藍、二甲基異丙基甘菊藍、二甲基乙基甘菊藍、該些的鹽等)等。該些可單獨使用一種,亦可組合使用兩種以上。雖對本揭示並無限制,但所述組成物較佳為不含有硫酸鋅及/或乳酸鋅。另外,所述組成物亦可不調配ε-胺基己酸、尿囊素、甘草苷酸及其鹽來製備。Although the present disclosure is not limited, for example, as an anti-inflammatory agent, zinc sulfate, zinc lactate, ε-aminocaproic acid, allantoin, glycyrrhizic acid (glycyrrhizic acid) and its salts, azulene ) class (chamomile blue, dimethyl isopropyl chamomile blue, dimethylethyl chamomile blue, salts of these, etc.), etc. These may be used alone or in combination of two or more. Although not limiting to the present disclosure, the composition preferably does not contain zinc sulfate and/or zinc lactate. In addition, the composition can also be prepared without blending ε-aminocaproic acid, allantoin, glycyrrhizinic acid and salts thereof.

雖對本揭示並無限制,但例如作為維生素類,可列舉:維生素A(視黃醇棕櫚酸酯、視黃醇乙酸酯、視黃醇、視黃醛、視黃酸等)、維生素B(黃素腺嘌呤二核苷酸(flavin adenine dinucleotide)、氰鈷胺(cyanocobalamin)等)、維生素E(生育酚乙酸酯、生育酚琥珀酸酯、生育酚煙酸酯、生育酚亞麻酸酯等)等。該些可單獨使用一種,亦可組合使用兩種以上。雖對本揭示並無限制,但所述組成物亦可不調配至少一種維生素類來製備。Although the present disclosure is not limited, examples of vitamins include vitamin A (retinyl palmitate, retinyl acetate, retinol, retinal, retinoic acid, etc.), vitamin B ( Flavin adenine dinucleotide (flavin adenine dinucleotide, cyanocobalamin, etc.), vitamin E (tocopheryl acetate, tocopheryl succinate, tocopheryl nicotinate, tocopheryl linolenate, etc. )wait. These may be used alone or in combination of two or more. Although not limiting to the present disclosure, the composition can also be prepared without at least one vitamin.

雖對本揭示並無限制,但例如作為抗組胺劑,可例示:氯菲安明(chlorpheniramine)及其鹽(氯菲安明馬來酸鹽等)、苯海拉明(diphenhydramine)及其鹽(苯海拉明鹽酸鹽等)等。該些可單獨使用一種,亦可組合使用兩種以上。本揭示的組成物亦可不調配抗組胺劑來製備。Although the present disclosure is not limited, examples of antihistamines include chlorpheniramine and its salts (chlorpheniramine maleate, etc.), diphenhydramine and its salts (diphenhydramine hydrochloride, etc.), etc. These may be used alone or in combination of two or more. The composition of the present disclosure can also be prepared without formulating an antihistamine.

於本揭示的組成物含有藥效成分的情況下,只要不妨礙本揭示的效果,則藥效成分的含量不受限制,於所述組成物中,藥效成分的含量較佳可例示為0.05 w/v%~0.3 w/v%,更佳可例示為0.1 w/v%~0.3 w/v%,進而較佳可例示為0.2 w/v%~0.27 w/v%。When the composition of the present disclosure contains medicinal ingredients, the content of the medicinal ingredients is not limited as long as the effect of the disclosure is not hindered. In the composition, the content of the medicinal ingredients is preferably 0.05 w/v% - 0.3 w/v%, more preferably 0.1 w/v% - 0.3 w/v%, more preferably 0.2 w/v% - 0.27 w/v%.

當作為所述其他成分的一例而列舉清涼劑時,作為清涼劑,可例示:薄荷腦、樟腦、冰片等。清涼劑可單獨使用一種,亦可組合使用兩種以上。本揭示的組成物可含有清涼劑,亦可不調配清涼劑來製備。When a cooling agent is mentioned as an example of the said other component, Menthol, camphor, borneol, etc. are illustrated as a cooling agent. The cooling agents may be used alone or in combination of two or more. The composition of the present disclosure may contain a cooling agent, or may be prepared without a cooling agent.

當作為所述其他成分的一例而列舉刺激劑時,作為刺激劑,可例示丙醛等醛等。雖對本揭示並無限制,但本揭示的組成物可含有刺激劑,亦可不調配刺激劑來製備。When a stimulant is mentioned as an example of the said other component, as a stimulant, aldehydes, such as propionaldehyde, etc. can be illustrated. Although there is no limitation to the present disclosure, the composition disclosed in the present disclosure may contain a stimulant, or may be prepared without a stimulant.

當作為所述其他成分的一例而列舉增稠劑時,作為增稠劑,可例示:海藻酸或其鹽、羥乙基纖維素、甲基纖維素、羥丙基甲基纖維素、羧甲基纖維素、聚乙二醇、聚乙烯吡咯啶酮、聚乙烯醇、羧基乙烯基聚合物、該些的鹽、丙三醇等。該些可單獨使用一種,亦可組合使用兩種以上。本揭示的洗眼用組成物亦可不調配該些增稠劑來製備。When a thickener is mentioned as an example of the other components, examples of the thickener include alginic acid or its salt, hydroxyethyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, carboxymethyl cellulose, polyethylene glycol, polyvinylpyrrolidone, polyvinyl alcohol, carboxyvinyl polymer, salts thereof, glycerin, and the like. These may be used alone or in combination of two or more. The eyewash composition of the present disclosure can also be prepared without formulating these thickeners.

本揭示的洗眼用組成物可藉由將所述成分(A)及成分(B)、視需要的所述成分(C)、成分(D)、所述其他成分混合來製造。所述混合只要可將該些成分混合,則不受限制,依照通常的程序進行混合即可。The eyewash composition of the present disclosure can be produced by mixing the above-mentioned component (A) and component (B), if necessary, the above-mentioned component (C), component (D), and the above-mentioned other components. The mixing is not limited as long as these components can be mixed, and what is necessary is to mix them according to a usual procedure.

本揭示的洗眼用組成物的pH只要為能夠用作滴眼劑或洗眼劑的範圍則不受限制,但於室溫(25℃)下可例示pH5~pH8,較佳可例示pH5.5~pH6.5,更佳可例示pH5.5~pH6,進而較佳可例示pH5.5~pH5.8。The pH of the eyewash composition of the present disclosure is not limited as long as it is within the range that can be used as eye drops or eyewash, but at room temperature (25° C.), it can be exemplified from pH 5 to pH 8, and preferably exemplified from pH 5.5 to pH6.5, More preferably, pH5.5-pH6 can be illustrated, More preferably, pH5.5-pH5.8 can be illustrated.

本揭示的洗眼用組成物的形態於室溫下為液狀,且只要可與現有公知的方法同樣地對眼睛進行清洗,則其使用方法不受限制,通常用於使用洗眼杯(eyecup)進行的洗眼,或者用於藉由滴眼進行的洗眼。The form of the eyewash composition disclosed in the present disclosure is liquid at room temperature, and as long as the eye can be washed in the same way as the conventionally known method, the method of use is not limited, and it is usually used for eyewashing with an eyecup (eyecup). for eyewashing, or for eyewashing by eye drops.

本揭示的洗眼用組成物可於佩戴著隱形眼鏡的狀態下使用,亦可於未佩戴隱形眼鏡的狀態下使用。關於隱形眼鏡,不區分硬性隱形眼鏡、軟性隱形眼鏡。The eyewash composition disclosed herein can be used with or without contact lenses. Regarding contact lenses, there is no distinction between hard contact lenses and soft contact lenses.

本揭示的洗眼用組成物只要可如上所述般使用,則不受限制,但於使用洗眼杯來使用的情況下,通常收容於現有公知的一般洗眼劑用容器(例如,包括容器主體、蓋體)中即可。所述容器的容量亦不受限制,但就使用便利性佳等觀點而言,容量較佳可例示為450 mL~550 mL。The composition for eyewash of the present disclosure is not limited as long as it can be used as described above, but in the case of using an eyewash cup, it is usually contained in a conventionally known general eyewash container (for example, including a container body, a lid body) can be. The capacity of the container is not limited either, but from the viewpoint of good usability and the like, the capacity is preferably 450 mL to 550 mL.

使用洗眼杯進行的洗眼只要依照通常的程序進行即可,例如可藉由如下方式使用:自所述容器向洗眼杯中注入適量、例如每只眼睛一次4 mL~6 mL的本揭示的洗眼用組成物,繼而,將該杯按壓至單側的眼睛周邊,使該杯內的洗眼用組成物與眼睛接觸,並進行多次眨眼。The eyewash using the eyewash cup can be carried out according to the usual procedures, for example, it can be used in the following way: inject an appropriate amount, such as 4 mL to 6 mL per eye, of the eyewash of the present disclosure from the container into the eyewash cup. Composition Next, the cup was pressed against one side of the eye, the eyewash composition in the cup was brought into contact with the eye, and the eyes were blinked several times.

另外,於本揭示的洗眼用組成物用於藉由滴眼進行的洗眼的情況下,通常收容於滴眼容器中來使用。作為滴眼容器,只要可收容所述組成物來進行滴眼,則不受限制,例如可例示現有公知的滴眼劑或滴眼型洗眼劑等中使用的滴眼容器(例如,容器主體、中塞(噴嘴)及蓋體中的至少兩個為一體型的類型)。所述容器的容量不受限制,但就使用便利性佳等觀點而言,容量可例示為8 mL~20 mL。In addition, when the eyewash composition of the present disclosure is used for eyewashing by eyedrops, it is usually accommodated in an eyedrop container and used. The eye drop container is not limited as long as it can contain the above-mentioned composition for instillation. For example, eye drop containers (for example, container main body, At least two of the middle plug (nozzle) and the cover are integral type). The capacity of the container is not limited, but from the viewpoint of good usability and the like, the capacity can be exemplified as 8 mL to 20 mL.

藉由滴眼進行的洗眼只要依照通常的使用方法即可,藉由每只眼睛一次滴入4滴~6滴的本揭示的洗眼用組成物來使用。每滴的滴加量亦不受限制,但每滴較佳可例示為35 μL~40 μL。Eyewashing by eyedrops can be performed by instilling 4 to 6 drops of the eyewashing composition of the present disclosure at a time in accordance with the usual method of use. The dropping amount per drop is also not limited, but it is preferably 35 μL to 40 μL per drop.

藉由本揭示的洗眼用組成物,儘管未調配選自四級銨鹽系防腐劑、對羥基苯甲酸酯類、氯丁醇及山梨酸類中的防腐劑,但藉由將0.01 w/v%以上的選自由玻尿酸及其鹽所組成的群組中的至少一種與丙二醇組合使用,亦可對洗眼用組成物賦予優異的防腐性。另外,藉由進一步調配選自由依地酸及其鹽所組成的群組中的至少一種、或者調配選自由吡哆醇、硫酸軟骨素及該些的鹽所組成的群組中的至少一種,儘管如後述的實施例所示般未調配防腐劑,亦可對洗眼用組成物賦予更優異的防腐性。另外,於所述組成物更含有所述藥效成分等的情況下,亦可獲得基於所述藥效成分等的有效作用。 [實施例] According to the eyewash composition of the present disclosure, although no preservative selected from quaternary ammonium salt preservatives, parabens, chlorobutanol and sorbic acid is formulated, by adding 0.01 w/v% or more The use of at least one selected from the group consisting of hyaluronic acid and its salts in combination with propylene glycol can also impart excellent antiseptic properties to the eyewash composition. In addition, by further compounding at least one selected from the group consisting of edetic acid and its salts, or compounding at least one selected from the group consisting of pyridoxine, chondroitin sulfate and their salts, Even if no antiseptic is compounded as shown in the Examples described later, more excellent antiseptic properties can be imparted to the eyewash composition. In addition, when the composition further contains the medicinal ingredient and the like, the effective action due to the medicinal ingredient and the like can be obtained. [Example]

以下,示出例子來對本揭示更詳細地進行說明,但本揭示並不限定於該些例子。Hereinafter, examples are shown to describe the present disclosure in more detail, but the present disclosure is not limited to these examples.

試驗例 1.洗眼用組成物的製備 依照下表1所示的調配比例將各成分混合,並使所獲得的混合物於滅菌過濾器中通過(實施例1~實施例5、參考例、比較例1~比較例3)。測定了製備後不久的各組成物的pH。pH是於室溫(25℃)下使用桌上型pH計F-52(堀場製作所股份有限公司製造)來測定。再者,表中的軟骨素硫酸酯鈉使用了日本藥局方外醫藥品規格硫酸軟骨素鈉(重量平均分子量20000)。 Test case 1. Preparation of eyewash composition Each component was mixed according to the compounding ratio shown in Table 1 below, and the obtained mixture was passed through a sterile filter (Example 1-Example 5, Reference Example, Comparative Example 1-Comparative Example 3). The pH of each composition was measured immediately after preparation. The pH was measured at room temperature (25° C.) using a desktop pH meter F-52 (manufactured by Horiba Seisakusho Co., Ltd.). In addition, the chondroitin sulfate sodium in the table|surface used the Japanese Pharmacopoeia prescription and medicine specification chondroitin sulfate sodium (weight average molecular weight 20000).

2.防腐力評價 <念珠菌> 使念珠菌(白色念珠菌(Candida albicans))懸浮於滅菌後的生理鹽水中而製備了菌液(1×10 8cfu/mL)。於如上所述般獲得的各組成物10 mL中接種菌液以達到1×10 6cfu/mL,並於30℃下於暗處保存14天。保存後,利用接菌棒將接種了念珠菌的各組成物0.1 mL塗佈於市售的具有卵磷脂與聚山梨醇酯的葡萄糖蛋白腖(Glucose Peptone with Lecithin&Polysorbate,GPLP)瓊脂培養基(GPLP瓊脂培養基「大湖(DAIGO)」,富士軟片和光純藥股份有限公司製造),於30℃下培養48小時後,以目視對菌落數進行計數,將計數值乘以100而得的值設為自保存起14天後的各組成物的菌數。將接種時的菌數設為100%,算出保存14天後的各組成物中菌數的比例(生存率)。根據所算出的值,依照以下的基準對洗眼用組成物的防腐力進行評價。 [評價基準] ◎:生存率減少至接種量的0.1%以下 ○:生存率減少至接種量的1%以下 △:生存率減少至接種量的10%以下 ×:不滿足所述△的基準 2. Evaluation of preservative power <Candida> Candida (Candida albicans) was suspended in sterilized physiological saline to prepare a bacterial solution (1×10 8 cfu/mL). The bacterial solution was inoculated to 1×10 6 cfu/mL in 10 mL of each composition obtained as described above, and stored at 30° C. in a dark place for 14 days. After storage, 0.1 mL of each composition inoculated with Candida was spread on a commercially available Glucose Peptone with Lecithin & Polysorbate (GPLP) agar medium (GPLP agar medium " Daigo (DAIGO), manufactured by Fujifilm Wako Pure Chemical Industries, Ltd.), after culturing at 30°C for 48 hours, the number of colonies was counted visually, and the value obtained by multiplying the count value by 100 was set as 14 since storage. The number of bacteria in each composition after days. The number of bacteria at the time of inoculation was set as 100%, and the ratio (survival rate) of the number of bacteria in each composition after storage for 14 days was calculated. Based on the calculated value, the antiseptic power of the eyewash composition was evaluated according to the following criteria. [Evaluation criteria] ◎: Survival rate decreased to less than 0.1% of the inoculated amount ○: Survival rate decreased to less than 1% of the inoculated amount △: Survival rate decreased to less than 10% of the inoculated amount ×: The criterion for △ was not met

<金黃色葡萄球菌> 使金黃色葡萄球菌(Staphylococcus aureus)懸浮於滅菌後的生理鹽水中而製備了菌液(1×10 8cfu/mL)。於如上所述般獲得的各組成物10 mL中接種菌液以達到1×10 6cfu/mL,並於35℃下於暗處保存14天。保存後,利用接菌棒將接種了金黃色葡萄球菌的各組成物0.1 mL塗佈於市售的大豆卵磷脂-酪蛋白消化物-聚山梨醇酯(Soya Casein Digest Lecithin Polysorbate,SCDLP)瓊脂培養基(SCDLP瓊脂培養基「大湖(DAIGO)」,富士軟片和光純藥股份有限公司製造),於35℃下培養48小時後,以目視對菌落數進行計數,將計數值乘以100而得的值設為自保存起14天後的各組成物的菌數。將接種時的菌數設為100%,算出保存14天後的各組成物中菌數的比例(生存率)。根據所算出的值,依照與上述相同的基準對洗眼用組成物的防腐力進行評價。 <Staphylococcus aureus> A bacterial liquid (1×10 8 cfu/mL) was prepared by suspending Staphylococcus aureus in sterilized physiological saline. A bacterial solution was inoculated to 1×10 6 cfu/mL in 10 mL of each composition obtained as described above, and stored at 35° C. in a dark place for 14 days. After storage, spread 0.1 mL of each composition inoculated with Staphylococcus aureus on a commercially available soybean lecithin-casein digest-polysorbate (Soya Casein Digest Lecithin Polysorbate, SCDLP) agar medium (SCDLP agar medium "DAIGO", manufactured by Fujifilm Wako Pure Chemical Industries, Ltd.), after culturing at 35°C for 48 hours, the number of colonies was counted visually, and the value obtained by multiplying the count value by 100 was set as It is the number of bacteria of each composition after 14 days from storage. The number of bacteria at the time of inoculation was set as 100%, and the ratio (survival rate) of the number of bacteria in each composition after storage for 14 days was calculated. Based on the calculated value, the antiseptic power of the eyewash composition was evaluated in accordance with the same criteria as above.

3.結果 將結果示於表1及表2中。 3. Results The results are shown in Table 1 and Table 2.

[表1] (單位:w/v%)    參考例 比較例1 比較例2 比較例3 實施例1 實施例2 實施例3 實施例4 實施例5 氯化苯銨 0.03 - - - - - - - - 丙二醇 - 0.5 - 0.5 0.5 0.5 0.5 0.5 0.5 玻尿酸鈉 -    0.01 0.001 0.01 0.02 0.02 0.01 0.02 依地酸鈉 - - - - - - 0.02 0.05 0.05 硼酸 1.2 1.2 1.2 1.2 1.2 1.2 1.2 1.2 1.2 聚山梨醇酯80 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 鹽酸 適量 適量 適量 適量 適量 適量 適量 適量 適量 氫氧化鈉 適量 適量 適量 適量 適量 適量 適量 適量 適量 精製水 剩餘部分 剩餘部分 剩餘部分 剩餘部分 剩餘部分 剩餘部分 剩餘部分 剩餘部分 剩餘部分 合計 100 100 100 100 100 100 100 100 100 pH 5.7 5.7 5.7 5.7 5.7 5.7 5.7 5.7 5.7 防腐力:念珠菌 × [Table 1] (Unit: w/v%) Reference example Comparative example 1 Comparative example 2 Comparative example 3 Example 1 Example 2 Example 3 Example 4 Example 5 Aniline ammonium chloride 0.03 - - - - - - - - Propylene Glycol - 0.5 - 0.5 0.5 0.5 0.5 0.5 0.5 Sodium Hyaluronate - 0.01 0.001 0.01 0.02 0.02 0.01 0.02 Sodium edetate - - - - - - 0.02 0.05 0.05 boric acid 1.2 1.2 1.2 1.2 1.2 1.2 1.2 1.2 1.2 Polysorbate 80 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 hydrochloric acid Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount sodium hydroxide Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount purified water The remaining part The remaining part The remaining part The remaining part The remaining part The remaining part The remaining part The remaining part The remaining part total 100 100 100 100 100 100 100 100 100 pH 5.7 5.7 5.7 5.7 5.7 5.7 5.7 5.7 5.7 Preservative Power: Candida x

[表2] (單位:w/v%)    實施例6 實施例7 丙二醇 0.5 0.5 玻尿酸鈉 0.02 0.02 依地酸鈉 0.05 0.05 軟骨素硫酸酯鈉 0.05 0.05 吡哆醇鹽酸鹽 - 0.01 硼酸 1.2 1.2 聚山梨醇酯80 0.05 0.05 鹽酸 適量 適量 氫氧化鈉 適量 適量 精製水 剩餘部分 剩餘部分 合計 100 100 pH 5.7 5.7 防腐力:念珠菌 防腐力:金黃色葡萄球菌 [Table 2] (Unit: w/v%) Example 6 Example 7 Propylene Glycol 0.5 0.5 Sodium Hyaluronate 0.02 0.02 Sodium edetate 0.05 0.05 Sodium Chondroitin Sulfate 0.05 0.05 Pyridoxine hydrochloride - 0.01 boric acid 1.2 1.2 Polysorbate 80 0.05 0.05 hydrochloric acid Appropriate amount Appropriate amount sodium hydroxide Appropriate amount Appropriate amount purified water The remaining part The remaining part total 100 100 pH 5.7 5.7 Preservative Power: Candida Antiseptic power: Staphylococcus aureus

調配了作為防腐劑的氯化苯銨的參考例是指本試驗例的陽性對照(positive control),如表1所示,評價結果為◎,防腐力優異。相對於此,於未調配氯化苯銨且調配了丙二醇的比較例1中,評價結果為×,未獲得所期望的防腐力。另外,於未調配氯化苯銨或丙二醇且調配了0.01 w/v%的玻尿酸鈉的比較例2中,評價結果為△,未獲得所期望的防腐力。另外,於未調配氯化苯銨且調配了玻尿酸鈉0.001 w/v%與丙二醇的比較例3中,評價結果為△,未獲得所期望的防腐力。The reference example in which aniline ammonium chloride was prepared as a preservative is the positive control (positive control) of this test example, and as shown in Table 1, the evaluation result was ◎, and the preservative power was excellent. On the other hand, in the comparative example 1 which did not mix aniline ammonium chloride but mix|blended propylene glycol, the evaluation result was x, and the desired anticorrosion power was not acquired. In addition, in Comparative Example 2 in which 0.01 w/v% of sodium hyaluronate was formulated without the addition of aniline ammonium chloride or propylene glycol, the evaluation result was △, and the desired antiseptic power was not obtained. In addition, in Comparative Example 3 in which aniline ammonium chloride was not blended but sodium hyaluronate 0.001 w/v% and propylene glycol were blended, the evaluation result was △, and the desired antiseptic power was not obtained.

相對於此,於未調配氯化苯銨且調配了玻尿酸鈉0.01 w/v%與丙二醇的實施例1中,評價結果為○,可見防腐力的提升。於提高了實施例1中的玻尿酸鈉含量的實施例2中,評價結果亦為○,可見防腐力的提升。根據該情況,令人驚訝地確認到,藉由將玻尿酸鈉以0.01 w/v%以上與防腐性差的丙二醇組合使用,可提高洗眼用組成物的防腐性。On the other hand, in Example 1 in which aniline ammonium chloride was not blended and sodium hyaluronate 0.01 w/v% and propylene glycol were blended, the evaluation result was ◯, and the antiseptic power was improved. In Example 2 in which the content of sodium hyaluronate in Example 1 was increased, the evaluation result was also ◯, and the antiseptic power was improved. From this situation, it was surprisingly confirmed that the antiseptic properties of the eyewash composition can be improved by using sodium hyaluronate at 0.01 w/v% or more in combination with propylene glycol having poor antiseptic properties.

另外,於在實施例1、實施例2中進一步調配了依地酸鈉的實施例3~實施例5、及在實施例5中進一步調配了軟骨素硫酸酯鈉的實施例6、以及在實施例6中進一步調配了吡哆醇鹽酸鹽的實施例7中,評價結果亦為○或◎,可見防腐力的提升。另外,於將實施例1~實施例7的pH設為6.2的情況下,亦分別可見與實施例1~實施例7相同程度的防腐性的提升。In addition, in Example 3 to Example 5 in which edetate sodium was further formulated in Example 1 and Example 2, and Example 6 in which chondroitin sulfate sodium was further formulated in Example 5, and in the implementation In Example 7 in which pyridoxine hydrochloride was further formulated in Example 6, the evaluation result was also ◯ or ⊚, and the antiseptic power was improved. Moreover, when the pH of Example 1-Example 7 was 6.2, the improvement of the corrosion resistance of the same level as Example 1-Example 7 was seen, respectively.

根據該些情況確認到,藉由將玻尿酸鈉以0.01 w/v%以上與防腐性差的丙二醇組合使用,進而藉由組合使用依地酸鈉、軟骨素硫酸酯鈉或吡哆醇鹽酸鹽,可提高洗眼用組成物的防腐性。另外,實施例1~實施例7的洗眼用組成物可於不使用氯化苯銨般的擔心吸附於隱形眼鏡的防腐劑的情況下提高防腐性,因此能夠於佩戴著隱形眼鏡的狀態下進行洗眼。Based on these circumstances, it was confirmed that by using sodium hyaluronate at 0.01 w/v% or more in combination with propylene glycol having poor preservative properties, and further by using sodium edetate, sodium chondroitin sulfate, or pyridoxine hydrochloride in combination, The antiseptic property of the eyewash composition can be improved. In addition, the eyewash compositions of Examples 1 to 7 can improve antiseptic properties without using an aniline ammonium chloride preservative that may be adsorbed to contact lenses, so they can be performed while wearing contact lenses. Wash your eyes.

處方例 依照表3所示的調配比例製備洗眼組成物,並藉由與試驗例相同的方法進行防腐力評價,結果於處方例1~處方例7的任一洗眼組成物中,可見防腐性以與實施例7相同的程度提升。 Prescription The eyewash composition was prepared according to the formulation ratio shown in Table 3, and the preservative power was evaluated by the same method as the test example. As a result, in any eyewash composition of prescription example 1 to prescription example 7, it can be seen that the antiseptic property is the same as that of the practice Example 7 is promoted to the same extent.

[表3] (單位:w/v%)    處方例1 處方例2 處方例3 處方例4 處方例5 處方例6 處方例7 丙二醇 0.5 0.5 0.5 0.5 0.5 0.5 0.5 玻尿酸鈉 0.02 0.02 0.02 0.02 0.02 0.02 0.02 依地酸鈉 0.05 0.05 0.05 0.05 0.05 0.05 0.05 軟骨素硫酸酯鈉 0.05 0.05 0.05 0.05 0.05 0.05 0.05 吡哆醇鹽酸鹽 0.01 0.01 0.01 0.01 0.01 0.01 0.01 ε-胺基己酸 - 0.2 0.2 0.2 0.2 0.2 0.2 尿囊素 0.03 - - - 0.03 0.03 0.03 甘草苷酸二鉀 0.015 - - 0.015 0.015 0.015 0.015 氯菲安明馬來酸鹽 0.003 0.003 0.003 - 0.003 0.003 0.003 氰鈷胺 0.002 0.002 0.002 0.002 0.002 0.002 0.002 生育酚乙酸酯 - - - 0.005 - - 0.005 l-薄荷腦 0.005 0.005 0.005 0.005 0.005 0.005 0.005 d-冰片 0.002 0.002 0.002 0.002 0.002 0.002 0.002 硼酸 1.6 1.6 1.6 1.6 1.6 1.6 1.6 硼砂 0.03 0.03 0.03 0.03 0.03 0.03 0.03 聚山梨醇酯80 0.01 0.01 0.01 0.01 0.01 0.01 0.01 氫氧化鈉 適量 適量 適量 適量 適量 適量 適量 鹽酸 適量 適量 適量 適量 適量 適量 適量 精製水 剩餘部分 剩餘部分 剩餘部分 剩餘部分 剩餘部分 剩餘部分 剩餘部分 合計 100 100 100 100 100 100 100 pH 5.7 5.7 6.2 6.2 5.7 6.2 5.7 [table 3] (Unit: w/v%) Prescription example 1 Prescription example 2 Prescription example 3 Prescription example 4 Prescription example 5 Prescription example 6 Prescription example 7 Propylene Glycol 0.5 0.5 0.5 0.5 0.5 0.5 0.5 Sodium Hyaluronate 0.02 0.02 0.02 0.02 0.02 0.02 0.02 Sodium edetate 0.05 0.05 0.05 0.05 0.05 0.05 0.05 Sodium Chondroitin Sulfate 0.05 0.05 0.05 0.05 0.05 0.05 0.05 Pyridoxine hydrochloride 0.01 0.01 0.01 0.01 0.01 0.01 0.01 ε-aminocaproic acid - 0.2 0.2 0.2 0.2 0.2 0.2 Allantoin 0.03 - - - 0.03 0.03 0.03 Dipotassium Glycyrrhizinate 0.015 - - 0.015 0.015 0.015 0.015 Chlorpheniramine maleate 0.003 0.003 0.003 - 0.003 0.003 0.003 Cyanocobalamin 0.002 0.002 0.002 0.002 0.002 0.002 0.002 tocopheryl acetate - - - 0.005 - - 0.005 l-menthol 0.005 0.005 0.005 0.005 0.005 0.005 0.005 d-borneol 0.002 0.002 0.002 0.002 0.002 0.002 0.002 boric acid 1.6 1.6 1.6 1.6 1.6 1.6 1.6 Borax 0.03 0.03 0.03 0.03 0.03 0.03 0.03 Polysorbate 80 0.01 0.01 0.01 0.01 0.01 0.01 0.01 sodium hydroxide Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount hydrochloric acid Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount purified water The remaining part The remaining part The remaining part The remaining part The remaining part The remaining part The remaining part total 100 100 100 100 100 100 100 pH 5.7 5.7 6.2 6.2 5.7 6.2 5.7

none

none

Claims (4)

一種洗眼用組成物,含有:(A)0.01 w/v%以上的選自由玻尿酸及其鹽所組成的群組中的至少一種、以及(B)丙二醇,且不含有選自四級銨鹽系防腐劑、對羥基苯甲酸酯類、氯丁醇及山梨酸類中的防腐劑。An eyewash composition, containing: (A) 0.01 w/v% or more of at least one selected from the group consisting of hyaluronic acid and its salts, and (B) propylene glycol, and does not contain quaternary ammonium salts Preservatives, parabens, chlorobutanol and preservatives in sorbic acid. 如請求項1所述的洗眼用組成物,更含有(C)0.05 w/v%以上的選自由依地酸及其鹽所組成的群組中的至少一種。The eyewash composition according to Claim 1 further contains (C) 0.05 w/v% or more of at least one selected from the group consisting of edetic acid and its salts. 如請求項1或請求項2所述的洗眼用組成物,更含有(D)選自由吡哆醇、硫酸軟骨素及該些的鹽所組成的群組中的至少一種。The eyewash composition according to Claim 1 or Claim 2 further contains (D) at least one selected from the group consisting of pyridoxine, chondroitin sulfate, and salts thereof. 如請求項1至請求項3中任一項所述的洗眼組成物,於佩戴隱形眼鏡的過程中使用。The eyewash composition as described in any one of claim 1 to claim 3 is used in the process of wearing contact lenses.
TW111129138A 2021-08-03 2022-08-03 Eyewash composition TW202320811A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2021127507A JP2023022569A (en) 2021-08-03 2021-08-03 Eyewash composition
JP2021-127507 2021-08-03

Publications (1)

Publication Number Publication Date
TW202320811A true TW202320811A (en) 2023-06-01

Family

ID=85155711

Family Applications (1)

Application Number Title Priority Date Filing Date
TW111129138A TW202320811A (en) 2021-08-03 2022-08-03 Eyewash composition

Country Status (4)

Country Link
JP (1) JP2023022569A (en)
CN (1) CN117835988A (en)
TW (1) TW202320811A (en)
WO (1) WO2023013628A1 (en)

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH09227385A (en) * 1996-02-29 1997-09-02 Ofutekusu:Kk Adjuvant for ophthalmic operation
CA2736380C (en) * 2008-09-15 2013-05-28 Bausch & Lomb Incorporated Compositions comprising polymers having amino sugar units and methods of making and using same
JP6653123B2 (en) * 2014-03-26 2020-02-26 ロート製薬株式会社 Ophthalmic composition for color contact lenses
CN104474009A (en) * 2014-11-26 2015-04-01 杭州光祺力实业有限公司 Eye cleaning liquid and preparation method thereof
KR102607126B1 (en) * 2015-03-06 2023-11-27 산텐 세이야꾸 가부시키가이샤 Ophthalmic composition
CN106265720A (en) * 2015-05-12 2017-01-04 上海昊海生物科技股份有限公司 A kind of combined artificial tear and preparation method thereof
JP2017066065A (en) * 2015-09-29 2017-04-06 小林製薬株式会社 Ophthalmic composition

Also Published As

Publication number Publication date
CN117835988A (en) 2024-04-05
JP2023022569A (en) 2023-02-15
WO2023013628A1 (en) 2023-02-09

Similar Documents

Publication Publication Date Title
JP2014074044A (en) Soft contact lens composition and adsorption-suppressing method
CA2290461A1 (en) Antiseptic composition
JP2020073606A (en) Eye drops for nonionic silicone hydrogel contact lenses
JP2002316926A (en) Ophthalmic composition for contact lens and method for mitigating ocular irritation
JPH10203960A (en) Eye lotion composition
JP5834427B2 (en) Adsorption suppression method for soft contact lenses
JP3050898B2 (en) Aqueous pharmaceutical preparation
TW202320811A (en) Eyewash composition
WO2022138075A1 (en) Eye drop-type eyewash composition
JP2019194273A (en) Aqueous composition iii
JP5246182B2 (en) Eye drops, preservatives and preservatives
JP2000086536A (en) Preservative composition
JP4157988B2 (en) Water-soluble preparations with no contraindications
JP4524538B2 (en) Ophthalmic composition
JP2006000170A (en) Contact lens composition
JP2007269673A (en) Preservative
JP2022099575A (en) Eyewash composition
JP4470393B2 (en) Eye drops that are stable
JP4624018B2 (en) Eye wash set
JP2016135780A (en) Aqueous composition
JP2011221464A (en) Ophthalmologic composition for contact lens
JP2006104114A (en) Mucous membrane application composition
TW202408473A (en) Ophthalmic composition
WO2005072727A1 (en) Eye drop composition
JP5542511B2 (en) Contact lens ophthalmic composition