WO2016181998A1 - 眼科用組成物 - Google Patents
眼科用組成物 Download PDFInfo
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- WO2016181998A1 WO2016181998A1 PCT/JP2016/064032 JP2016064032W WO2016181998A1 WO 2016181998 A1 WO2016181998 A1 WO 2016181998A1 JP 2016064032 W JP2016064032 W JP 2016064032W WO 2016181998 A1 WO2016181998 A1 WO 2016181998A1
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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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
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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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
- A61K31/23—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
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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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- A61K31/375—Ascorbic acid, i.e. vitamin C; Salts thereof
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- 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
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- 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
Definitions
- the present invention relates to an ophthalmic composition.
- the tear film is composed of lipids secreted from the meibomian glands. It is known that saturated lipids increase in the oil film due to aging and changes in hormone balance. The tear film oil film with increased saturated lipids has poor stability and contributes to dry eye and eyestrain.
- Patent Document 1 It has been reported that lecithin is used to stabilize the tear film oil film (Patent Document 1). However, there has been a problem that separation such as creaming occurs during storage of the preparation and the usability is significantly reduced.
- the present invention has been made in view of the above problems, and an object thereof is to provide an ophthalmic composition that can stabilize a tear film oil film and has good storage stability.
- the present inventor contains at least one selected from branched aliphatic carboxylic acids having 12 to 20 carbon atoms and esters having a branched alkyl chain having 12 to 20 carbon atoms.
- the present inventors have found that the ophthalmic composition can stabilize the tear film oil film in which the saturated lipid is increased and that the storage stability is also good, and the present invention has been completed.
- Ophthalmology containing one or more selected from (A) (A-1) a branched aliphatic carboxylic acid having 12 to 20 carbon atoms and (A-2) an ester having at least one branched alkyl chain having 12 to 20 carbon atoms Composition. [2].
- the (A-2) ester is an ester of a branched aliphatic carboxylic acid having 12 to 20 carbon atoms and a polyhydric alcohol or ascorbic acid, or an ester of a branched alcohol having 12 to 20 carbon atoms and a polyvalent carboxylic acid.
- the ophthalmic composition according to [1]. [3].
- a method for stabilizing a tear film oil film comprising eye-dropping a composition containing at least one selected from a branched aliphatic carboxylic acid having 12 to 20 carbon atoms and an ester having a branched alkyl chain having 12 to 20 carbon atoms .
- the ophthalmic composition of the present invention can stabilize a tear film oil film in which saturated lipids are increased, and has good storage stability.
- the ophthalmic composition of the present invention contains one or more selected from the group consisting of the following (A-1) and (A-2).
- (A-1) Branched aliphatic carboxylic acid having 12 to 20 carbon atoms
- Examples of the branched aliphatic carboxylic acid having 12 to 20 carbon atoms include isopalmitic acid, isostearic acid, isomyristic acid, and isolauric acid. Of these, isostearic acid is preferred.
- the number of carbon atoms of the branched aliphatic carboxylic acid is preferably 16-18.
- An ester having at least one branched alkyl chain having 12 to 20 carbon atoms The number of branched alkyl chains per molecule of an ester having at least one branched alkyl chain having 12 to 20 carbon atoms is 1 to 5 Preferably, 1 to 3 is more preferable, and 2 is most preferable.
- the branched alkyl chain preferably has 16 to 18 carbon atoms.
- the number of branched chains (side chains) in the branched alkyl chain is preferably 1 to 4, more preferably 1 to 3, still more preferably 1 or 2, and most preferably 1.
- the number of carbon atoms in the branched chain (side chain) in the branched alkyl chain is preferably 1 to 8, more preferably 1 to 6, and still more preferably 1 to 4.
- ester examples include esters of a branched aliphatic carboxylic acid having 12 to 20 carbon atoms and alcohol or ascorbic acid.
- Examples of the branched aliphatic carboxylic acid having 12 to 20 carbon atoms include isolauric acid, isomyristic acid, isopalmitic acid, and isostearic acid.
- Examples of the alcohol include monohydric alcohols having 1 to 18 carbon atoms such as methanol, ethanol, propanol and stearyl alcohol; polyhydric alcohols such as ethylene glycol, polyethylene glycol, glycerin, polyglycerin and sorbitan; and saccharides such as dextrin. .
- the ester of a branched aliphatic carboxylic acid having 12 to 20 carbon atoms and an alcohol or ascorbic acid is preferably an ester of a branched aliphatic carboxylic acid having 12 to 20 carbon atoms and a polyhydric alcohol or ascorbic acid.
- an ester of a branched alcohol having 12 to 20 carbon atoms and a carboxylic acid may be mentioned, and an ester of a branched alcohol having 12 to 20 carbon atoms and a polyvalent carboxylic acid is more preferable.
- Examples of the branched alcohol having 12 to 20 carbon atoms include isopalmityl alcohol, isostearyl alcohol, isomyristyl alcohol, and isolauryl alcohol.
- carboxylic acid examples include monovalent carboxylic acids having 1 to 18 carbon atoms such as myristic acid, palmitic acid, stearic acid, and acetic acid; and polyvalent carboxylic acids such as sebacic acid, adipic acid, malic acid, and citric acid. Of these, polyvalent carboxylic acids are preferable, and divalent carboxylic acids such as sebacic acid, adipic acid, malic acid, and the like are particularly preferable.
- component (A) examples include isostearic acid, polyglyceryl pentaisostearate such as polyglyceryl pentaisostearate, diisostearyl malate, ascorbyl tetraisopalmitate, propylene glycol isostearate, cholesteryl isostearate, and dextrin isostearate. Sorbitan isostearate, polyglyceryl-2 diisostearate and the like. Of these, diisostearyl malate is preferred.
- the blending amount of the component (A) is preferably 0.01 to 1.0 w / v% (g / 100 mL) in the composition, more preferably 0.05 to 0.5 w / v%, and 0.05 to 0.5. 2 w / v% is more preferable, and 0.05 to 0.1 w / v% is most preferable.
- eye irritation is favorable and a tear film oil film can be stabilized effectively.
- the ophthalmic composition of the present invention can be blended with other components in appropriate amounts within a range not impairing the effects of the present invention.
- other components include surfactants, polyhydric alcohols, thickeners, sugars, buffers, pH adjusters, tonicity agents, cooling agents, drugs, and the like.
- Surfactants include polyoxyethylene polyoxypropylene glycol, polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, glycine-type amphoteric surfactants such as alkyldiaminoethylglycine, alkyl quaternary ammonium salts (specifically Are cationic surfactants such as benzalkonium chloride and benzethonium chloride.
- the blending amount of the surfactant is preferably 0.0001 to 10 w / v% in the composition.
- polyhydric alcohol examples include glycerin, propylene glycol, butylene glycol, and polyethylene glycol.
- the blending amount of the polyhydric alcohol is preferably 0.001 to 5 w / v% in the ophthalmic composition.
- the thickener examples include polyvinylpyrrolidone, hydroxyethylcellulose, hydroxypropylmethylcellulose, methylcellulose, polyvinyl alcohol, sodium hyaluronate, sodium chondroitin sulfate, polyacrylic acid, carboxyvinyl polymer, and the like.
- the blending amount of the thickening agent is preferably 0.003 to 3 w / v% in the composition.
- sugars examples include glucose, cyclodextrin, xylitol, sorbitol, mannitol and the like. These may be any of d-form, l-form, and dl-form.
- the blending amount of the saccharide is preferably 0.001 to 5 w / v% in the composition.
- the buffer examples include citric acid, sodium citrate, boric acid, borax, phosphoric acid, sodium hydrogen phosphate, sodium dihydrogen phosphate, glacial acetic acid, trometamol, sodium hydrogen carbonate and the like.
- the blending amount of the buffer is preferably 0.003 to 4 w / v% in the composition.
- an inorganic acid or an inorganic alkali agent can be used as the pH adjusting agent.
- (diluted) hydrochloric acid etc. are mentioned as an inorganic acid.
- the inorganic alkaline agent include sodium hydroxide, potassium hydroxide, sodium carbonate, sodium hydrogen carbonate and the like.
- the pH is measured at 20 ° C. using a pH osmometer (HSMO-1, Toa DKK).
- the isotonic agent examples include sodium chloride and potassium chloride.
- the blending amount of the isotonizing agent is preferably 0.001 to 3 w / v% in the composition.
- the stabilizer examples include sodium edetate, cyclodextrin, sulfite, dibutylhydroxytoluene and the like.
- the blending amount of the stabilizer is preferably 0.003 to 2 w / v% in the composition.
- the refreshing agent examples include menthol, camphor, borneol, geraniol, cineol, linalool and the like.
- the blending amount of the refreshing agent is preferably 0.0001 to 0.2 w / v% in the composition.
- drugs pharmaceutical active ingredients
- decongestants eg, naphazoline hydrochloride, tetrahydrozoline hydrochloride, phenylephrine hydrochloride, epinephrine, ephedrine hydrochloride, dl-methylephedrine hydrochloride, tetrahydrozoline nitrate, naphazoline nitrate
- anti-inflammatory / astringent agents For example, neostigmine methyl sulfate, ⁇ -aminocaproic acid, allantoin, berberine chloride, zinc sulfate, zinc lactate, lysozyme chloride, dipotassium glycyrrhizinate, ammonium glycyrrhizinate, glycyrrhetinic acid, methyl salicylate, tranexamic acid, sodium azulene sulfonate) , Antihistamine
- the effective content of each drug can be selected as the content of the drug, but is preferably 0.001 to 5 w / v% in the composition from the viewpoint of irritation to the eye and stability of the composition. .
- the other components can be blended singly or in appropriate combination of two or more.
- the pH of the ophthalmic composition of the present invention is preferably 3.8 to 8.0, more preferably 5.0 to 7.5 from the viewpoint of eye irritation.
- the osmotic pressure of the ophthalmic composition of the present invention is preferably 200 to 800 mOsm, more preferably 200 to 500 mOsm from the viewpoint of eye irritation.
- each component is mixed in water at 50 to 90 ° C. using a propeller blade, a homomixer, a high-pressure emulsifier, or the like, and the pH is adjusted.
- the final volume can be obtained by adding water (amount of water: balance).
- the ester having at least one branched aliphatic carboxylic acid having 12 to 20 carbon atoms and branched alkyl chain having 12 to 20 carbon atoms has a function of stabilizing the tear film oil film. Therefore, a branched aliphatic carboxylic acid having 12 to 20 carbon atoms and an ester having at least one branched alkyl chain having 12 to 20 carbon atoms can be used as a tear film oil film stabilizer. When using these as a tear film oil film stabilizer, it can be used individually by 1 type or in combination of 2 or more types.
- the ophthalmic composition of the present invention can be suitably used as an eye drop, an eye drop for contact lenses, an eye wash, and the like, but can be particularly preferably used as an eye drop.
- the effect of the present invention can be further exerted by instilling 30 to 60 ⁇ L per time and 3 to 6 times per day.
- the effect of the present invention can be further exerted by washing the eyes 3 to 6 mL per time and 3 to 6 times per day.
- the present invention relates to one kind selected from (A) (A-1) a branched aliphatic carboxylic acid having 12 to 20 carbon atoms and (A-2) an ester having at least one branched alkyl chain having 12 to 20 carbon atoms.
- a tear film oil film stabilizer containing the above as an active ingredient is provided. It is also effective as a dry eye prevention agent and dry eye improving agent.
- a suitable thing, a range, etc. are the same as that of the above.
- the effective amount is preferably 0.009 to 3.6 mg / day per adult.
- Examples 1 to 10 Comparative Examples 1 to 4
- Ophthalmic compositions (eye drops) having the compositions shown in Tables 1 to 3 below were prepared and evaluated as follows. The results are also shown in the table. Moreover, the image used for the oil film stability evaluation result of Example 3, 4 and 9 is shown in FIG. 1, and the image used for the oil film stability evaluation result of Comparative Examples 1 and 4 is shown in FIG.
- the tear film oil film mainly contains wax ester (oleyl oleate, etc.), cholesterol ester (cholesterol oleate, etc.), and phosphatidylcholine.
- wax ester oleyl oleate, etc.
- cholesterol ester cholesterol ester
- phosphatidylcholine a group consisting of C16F1, C18F1 fatty acids.
- C16F0, C18F0 saturated lipids
- oleyl oleate 3.8 ⁇ g, cholesterol oleate 5.8 ⁇ g, phosphatidylcholine (C18F0 / C18F0) 0.2 ⁇ g, phosphatidylcholine (C18F0 / C18F1) 0.2 ⁇ g and perylene 0.1 ⁇ g was dissolved in 1,000 ⁇ L chloroform, and an oil film prepared by the procedure of spreading 10 ⁇ L of the solution on a water film prepared with 1 mL of water in a 35 mm plastic dish was used. After allowing the oil film to stand at room temperature for 10 minutes, 50 ⁇ L of the prepared eye drop was added, placed on a 37 ° C. hot plate, and allowed to stand for 30 minutes.
- Oil film stability evaluation ⁇ : Uniform oil film ⁇ : Uneven but water film is not exposed ⁇ : Uneven water film is not exposed ⁇ : Water film is exposed
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Abstract
Description
[1].(A)(A-1)炭素数12~20の分岐脂肪族カルボン酸及び(A-2)炭素数12~20の分岐アルキル鎖を少なくとも1つ有するエステルから選ばれる1種以上を含有する眼科用組成物。
[2].前記(A-2)エステルが、炭素数12~20の分岐脂肪族カルボン酸と多価アルコール若しくはアスコルビン酸とのエステル、又は炭素数12~20の分岐アルコールと多価カルボン酸とのエステルである[1]記載の眼科用組成物。
[3].(A)成分が、イソステアリン酸、ペンタイソステアリン酸ポリグリセリル、リンゴ酸ジイソステアリル又はテトライソパルミチン酸アスコルビルである[1]又は[2]記載の眼科用組成物。
[4].(A)成分の配合量が、0.01~1.0w/v%である[1]~[3]のいずれかに記載の眼科用組成物。
[5].点眼剤又は洗眼剤である[1]~[4]のいずれかに記載の眼科用組成物。
[6].(A)(A-1)炭素数12~20の分岐脂肪族カルボン酸及び(A-2)炭素数12~20の分岐アルキル鎖を有するエステルから選ばれる1種以上を有効成分として含有する涙液層油膜安定化剤。
[7].炭素数12~20の分岐脂肪族カルボン酸及び炭素数12~20の分岐アルキル鎖を有するエステルから選ばれる1種以上を含有する組成物を点眼することを特徴とする涙液層油膜安定化方法。
本発明の眼科用組成物は、下記(A-1)及び(A-2)からなる群から選ばれる1種以上を含有するものである。
炭素数12~20の分岐状脂肪族カルボン酸としては、イソパルミチン酸、イソステアリン酸、イソミリスチン酸、イソラウリン酸等が挙げられる。これらのうち、イソステアリン酸が好ましい。
炭素数12~20の分岐アルキル鎖を少なくとも1つ有するエステル1分子あたりの分岐アルキル鎖の数は、1~5が好ましく、1~3がより好ましく、2が最も好ましい。前記分岐アルキル鎖の炭素数は、16~18であることが好ましい。更に、分岐アルキル鎖中の分岐鎖(側鎖)の数は、1~4が好ましく、1~3がより好ましく、1又は2が更に好ましく、1が最も好ましい。また、前記分岐アルキル鎖中の分岐鎖(側鎖)の炭素数は、1~8が好ましく、1~6がより好ましく、1~4が更に好ましい。
本発明の眼科用組成物には、本発明の効果を損なわない範囲で、その他の成分を適量配合することができる。その他の成分としては、界面活性剤、多価アルコール、粘稠剤、糖類、緩衝剤、pH調整剤、等張化剤、清涼化剤、薬物等が挙げられる。
・ペンタイソステアリン酸ポリグリセリル-10(NIKKOL Decaglyn5-ISV、日光ケミカルズ(株)製)
・リンゴ酸ジイソステアリル(NIKKOL DISM、日光ケミカルズ(株)製)
・イソステアリン酸(イソステアリン酸EX、高級アルコール(株)製)
・テトライソパルミチン酸アスコルビル(VCI-1、(株)アイ・ティー・オー製)
・ステアリン酸(和光純薬工業(株)製)
・レシチン(卵製、和光純薬工業(株)製)
・エデト酸ナトリウム(クレワットN、ナガセケムテックス(株)製)
・トロメタモール(関東化学(株)製)
・ひまし油(小堺製薬(株)製)
・ヒアルロン酸ナトリウム(資生堂(株)製)
・ホウ酸(小堺製薬(株)製)
・ホウ砂(小堺製薬(株)製)
・塩化ナトリウム(和光純薬工業(株)製)
・塩化カリウム(和光純薬工業(株)製)
・水酸化ナトリウム(和光純薬工業(株)製)
・希塩酸(和光純薬工業(株)製)
・オレイルオレート(NU-CHEK PREP社製)
・コレステロールオレート(NU-CHEK PREP社製)
・ホスファチジルコリン(AVANTI POLAR LIPIDS社製)
・ペリレン(和光純薬工業(株)製)
・クロロホルム(和光純薬工業(株)製)
・浸透圧の測定:浸透圧計(ADVANCED INSTRUMENTS社製、A2O)
下記表1~3に示す組成の眼科用組成物(点眼剤)を調製し、下記評価を行った。結果を表中に併記する。また、実施例3、4及び9の油膜安定性評価結果に使用した画像を図1に示し、比較例1及び4の油膜安定性評価結果に使用した画像を図2に示す。
涙液層油膜には、ワックスエステル(オレイルオレート等)、コレステロールエステル(コレステロールオレート等)、ホスファチジルコリンが主に含まれ、これらの中でもC16F1、C18F1脂肪酸からなるものが主に含まれる(Journal of Lipid Research 2014, 55, 289-298)。しかし、加齢やホルモンバランスの変化により飽和脂質(C16F0、C18F0)の割合が増加することが知られており、涙液層油膜を不安定化させる原因となる(Cornea 2000, 19, 72-74参照)。そこで、飽和脂質が増加した涙液層油膜モデルとして、オレイルオレート3.8μg、コレステロールオレート5.8μg、ホスファチジルコリン(C18F0/C18F0)0.2μg、ホスファチジルコリン(C18F0/C18F1)0.2μg及びペリレン0.1μgを1,000μLクロロホルムに溶解し、その溶液10μLを35mmプラスチック製ディッシュ中に1mLの水で作製した水膜上に展開するという手順で作製した油膜を用いた。油膜を10分間室温で静置後、作製した点眼剤を50μL添加し、37℃のホットプレート上に置き、30分間静置した。その後、254nmの紫外光を油膜に照射し、油膜の蛍光をデジタルカメラにて撮影し、その画像により下記評価基準に従って油膜安定性を評価した。
・油膜安定性評価
◎:均一な油膜
○:ムラがあるが水膜は露出せず
△:かなりムラがあるが水膜は露出せず
×:水膜が露出した
涙液油層安定性の評価を、ドライアイ観察装置DR-1(興和株式会社製)を用いてBUT(break up time)を測定することで行った。DR-1は涙液油層表面と涙液水層との境界面で反射される光の干渉像を測定できる装置である。健常眼では、均一な灰色または白色の干渉像が観察され、涙液油層が崩壊すると干渉像が消失する。被験者に各油性点眼剤30μLを点眼し10分経過後、数度瞬目し、その瞬目から涙液油層の崩壊までの時間(BUT)を測定した。被験者はBUTが10秒以下の人3名を選択した。点眼前後の結果を油層BUTの3名の平均値から、下記評価基準で示す。
[油層安定性評価]
○:油層BUTが10秒以上
×:油層BUTが10秒未満
眼科用組成物20mLをガラスバイアル(20mL)に充填し、50℃、1ヶ月保存後の外観変化を目視により観察し、下記評価基準に従って保存安定性を評価した。
・保存安定性評価(50℃、1ヶ月)
○:均一な製剤
×:白濁、分離が発生した
眼科用組成物を50μL点眼し、下記評価基準に従って眼刺激性をスコア化した。
0:刺激を感じない
1:刺激をやや感じる
2:刺激を感じる
3:非常に刺激を感じる
結果を3名の平均値から以下の基準で示す。
◎:0.5点未満
○:0.5点以上1.5点未満
△:1.5点以上2.5点未満
×:2.5点以上
Claims (7)
- (A)(A-1)炭素数12~20の分岐脂肪族カルボン酸及び(A-2)炭素数12~20の分岐アルキル鎖を少なくとも1つ有するエステルから選ばれる1種以上を含有する眼科用組成物。
- 前記(A-2)エステルが、炭素数12~20の分岐脂肪族カルボン酸と多価アルコール若しくはアスコルビン酸とのエステル、又は炭素数12~20の分岐アルコールと多価カルボン酸とのエステルである請求項1記載の眼科用組成物。
- (A)成分が、イソステアリン酸、ペンタイソステアリン酸ポリグリセリル、リンゴ酸ジイソステアリル又はテトライソパルミチン酸アスコルビルである請求項1又は2記載の眼科用組成物。
- (A)成分の配合量が、0.01~1.0w/v%である請求項1~3のいずれか1項記載の眼科用組成物。
- 点眼剤又は洗眼剤である請求項1~4のいずれか1項記載の眼科用組成物。
- (A)(A-1)炭素数12~20の分岐脂肪族カルボン酸及び(A-2)炭素数12~20の分岐アルキル鎖を有するエステルから選ばれる1種以上を有効成分として含有する涙液層油膜安定化剤。
- 炭素数12~20の分岐脂肪族カルボン酸及び炭素数12~20の分岐アルキル鎖を有するエステルから選ばれる1種以上を含有する組成物を点眼することを特徴とする涙液層油膜安定化方法。
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Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2002038149A1 (fr) * | 2000-11-08 | 2002-05-16 | Santen Pharmaceutical Co., Ltd. | Médicaments à base de farnésyl-acétate contre des affections kératoconjonctivales |
JP2010120856A (ja) * | 2008-11-17 | 2010-06-03 | Santen Pharmaceut Co Ltd | 眼科用組成物 |
WO2011039638A2 (en) * | 2009-10-02 | 2011-04-07 | Foamix Ltd. | Topical tetracycline compositions |
JP2016027039A (ja) * | 2014-07-03 | 2016-02-18 | ロート製薬株式会社 | 局所粘膜用水性組成物 |
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- 2016-05-11 JP JP2017517968A patent/JP6760275B2/ja active Active
- 2016-05-11 KR KR1020177031335A patent/KR20180003548A/ko unknown
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2002038149A1 (fr) * | 2000-11-08 | 2002-05-16 | Santen Pharmaceutical Co., Ltd. | Médicaments à base de farnésyl-acétate contre des affections kératoconjonctivales |
JP2010120856A (ja) * | 2008-11-17 | 2010-06-03 | Santen Pharmaceut Co Ltd | 眼科用組成物 |
WO2011039638A2 (en) * | 2009-10-02 | 2011-04-07 | Foamix Ltd. | Topical tetracycline compositions |
JP2016027039A (ja) * | 2014-07-03 | 2016-02-18 | ロート製薬株式会社 | 局所粘膜用水性組成物 |
Non-Patent Citations (1)
Title |
---|
AKIKO ARIMURA ET AL.: "Developments and applications of Vitamin A for eyedrops", BIOSCIENCE & INDUSTRY, vol. 58, no. 10, 1 October 2000 (2000-10-01), pages 716 - 719 * |
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