JP2005239681A - Ophthalmic agent - Google Patents
Ophthalmic agent Download PDFInfo
- Publication number
- JP2005239681A JP2005239681A JP2004054692A JP2004054692A JP2005239681A JP 2005239681 A JP2005239681 A JP 2005239681A JP 2004054692 A JP2004054692 A JP 2004054692A JP 2004054692 A JP2004054692 A JP 2004054692A JP 2005239681 A JP2005239681 A JP 2005239681A
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- JP
- Japan
- Prior art keywords
- ophthalmic
- ophthalmic agent
- pranoprofen
- menthol
- mass
- Prior art date
- Legal status (The legal status 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 status listed.)
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- 239000003732 agents acting on the eye Substances 0.000 title claims abstract description 23
- 229940125702 ophthalmic agent Drugs 0.000 title claims abstract description 23
- OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 claims abstract description 28
- TVQZAMVBTVNYLA-UHFFFAOYSA-N Pranoprofen Chemical compound C1=CC=C2CC3=CC(C(C(O)=O)C)=CC=C3OC2=N1 TVQZAMVBTVNYLA-UHFFFAOYSA-N 0.000 claims abstract description 19
- 229960003101 pranoprofen Drugs 0.000 claims abstract description 18
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 claims abstract description 17
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims abstract description 17
- 229940041616 menthol Drugs 0.000 claims abstract description 17
- 229960004926 chlorobutanol Drugs 0.000 claims abstract description 14
- 238000002360 preparation method Methods 0.000 claims description 12
- 230000007794 irritation Effects 0.000 abstract description 10
- 239000003889 eye drop Substances 0.000 description 10
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 6
- 239000000872 buffer Substances 0.000 description 5
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 229940012356 eye drops Drugs 0.000 description 4
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 description 4
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- 235000006679 Mentha X verticillata Nutrition 0.000 description 3
- 235000002899 Mentha suaveolens Nutrition 0.000 description 3
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- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
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- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- 206010061218 Inflammation Diseases 0.000 description 2
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- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
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- KGBXLFKZBHKPEV-UHFFFAOYSA-N boric acid Chemical compound OB(O)O KGBXLFKZBHKPEV-UHFFFAOYSA-N 0.000 description 2
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- 235000019260 propionic acid Nutrition 0.000 description 2
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 2
- 235000010339 sodium tetraborate Nutrition 0.000 description 2
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- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 description 1
- SLXKOJJOQWFEFD-UHFFFAOYSA-N 6-aminohexanoic acid Chemical compound NCCCCCC(O)=O SLXKOJJOQWFEFD-UHFFFAOYSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- BTBUEUYNUDRHOZ-UHFFFAOYSA-N Borate Chemical compound [O-]B([O-])[O-] BTBUEUYNUDRHOZ-UHFFFAOYSA-N 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 102000004005 Prostaglandin-endoperoxide synthases Human genes 0.000 description 1
- 108090000459 Prostaglandin-endoperoxide synthases Proteins 0.000 description 1
- 208000003251 Pruritus Diseases 0.000 description 1
- 239000004288 Sodium dehydroacetate Substances 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- GZLGNNHEHXBCBI-UHFFFAOYSA-L [Na+].[Na+].OC(=O)C(O)C(O)C(O)=O.[O-]C(=O)C(O)C(O)C([O-])=O Chemical compound [Na+].[Na+].OC(=O)C(O)C(O)C(O)=O.[O-]C(=O)C(O)C(O)C([O-])=O GZLGNNHEHXBCBI-UHFFFAOYSA-L 0.000 description 1
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- 239000000654 additive Substances 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 229940024606 amino acid Drugs 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 229960002684 aminocaproic acid Drugs 0.000 description 1
- 230000036592 analgesia Effects 0.000 description 1
- 230000000202 analgesic effect Effects 0.000 description 1
- 239000000730 antalgic agent Substances 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 230000002421 anti-septic effect Effects 0.000 description 1
- 229960000686 benzalkonium chloride Drugs 0.000 description 1
- 229960001950 benzethonium chloride Drugs 0.000 description 1
- UREZNYTWGJKWBI-UHFFFAOYSA-M benzethonium chloride Chemical compound [Cl-].C1=CC(C(C)(C)CC(C)(C)C)=CC=C1OCCOCC[N+](C)(C)CC1=CC=CC=C1 UREZNYTWGJKWBI-UHFFFAOYSA-M 0.000 description 1
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- 238000009530 blood pressure measurement Methods 0.000 description 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
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- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 235000019438 castor oil Nutrition 0.000 description 1
- 229960001927 cetylpyridinium chloride Drugs 0.000 description 1
- YMKDRGPMQRFJGP-UHFFFAOYSA-M cetylpyridinium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 description 1
- 239000007979 citrate buffer Substances 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- KFGJICJPSZZEEP-UHFFFAOYSA-L dipotassium;hydrogen phosphate;hydrate Chemical compound O.[K+].[K+].OP([O-])([O-])=O KFGJICJPSZZEEP-UHFFFAOYSA-L 0.000 description 1
- PXEDJBXQKAGXNJ-QTNFYWBSSA-L disodium L-glutamate Chemical compound [Na+].[Na+].[O-]C(=O)[C@@H](N)CCC([O-])=O PXEDJBXQKAGXNJ-QTNFYWBSSA-L 0.000 description 1
- HXOLFXRMWWHLMH-UHFFFAOYSA-L disodium boric acid carbonate Chemical compound [Na+].[Na+].OB(O)O.[O-]C([O-])=O HXOLFXRMWWHLMH-UHFFFAOYSA-L 0.000 description 1
- CEGDCUKGIQDKKW-UHFFFAOYSA-L disodium;2-hydroxypropane-1,2,3-tricarboxylic acid;carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O.OC(=O)CC(O)(C(O)=O)CC(O)=O CEGDCUKGIQDKKW-UHFFFAOYSA-L 0.000 description 1
- XNZQCYSOYHAYII-UHFFFAOYSA-L disodium;3-carboxy-3-hydroxypentanedioate;hydrate Chemical compound [OH-].[Na+].[Na+].OC(=O)CC(O)(C([O-])=O)CC(O)=O XNZQCYSOYHAYII-UHFFFAOYSA-L 0.000 description 1
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 1
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- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
本発明は、プラノプロフェンを含有する眼科用剤に関し、更に詳しくはクロロブタノール及びメントールを含有する眼科用剤に関する。 The present invention relates to an ophthalmic agent containing pranoprofen, and more particularly to an ophthalmic agent containing chlorobutanol and menthol.
プラノプロフェンは、プロピオン酸系の酸性非ステロイド系抗炎症化合物であり、眼科用としては外眼部及び前眼部における角結膜炎等の炎症疾患に対して有用であり、点眼剤の形態で実用に供されている。しかしプラノプロフェンは眼に対する刺激性があるため、点眼剤を処方する上でその刺激性を抑えるために種々の試みがなされている。例えば、ホウ酸を配合する方法（特許文献１参照）、炭酸塩を配合する方法（特許文献２参照）及び酢酸イオンを配合する方法（特許文献３参照）等が提案されている。
しかしながら、これらの発明はプラノプロフェンによる刺激の緩和を解決するものにすぎず使用感が良好なものとはいえなかった。 However, these inventions only solve the alleviation of irritation caused by pranoprofen and cannot be said to have good usability.
本発明は以上のような課題に鑑みてなされたものであり、プラノプロフェンを含有した眼科用剤において、使用感の改善及び向上を図った眼科用剤を提供することを目的とする。 This invention is made | formed in view of the above subjects, and it aims at providing the ophthalmic agent which aimed at the improvement and improvement of the usability | use_condition in the ophthalmic agent containing a pranoprofen.
より具体的には、本発明は以下のようなものを提供する。 More specifically, the present invention provides the following.
（１） プラノプロフェン及びクロロブタノールを含有する眼科用剤。 (1) An ophthalmic agent containing pranoprofen and chlorobutanol.
（１）の発明によれば、クロロブタノールを含有したことにより、プラノプロフェンによる刺激を緩和することによって使用感を改善することが可能となる。 According to the invention of (1), by containing chlorobutanol, it is possible to improve the feeling of use by alleviating the stimulation by pranoprofen.
（２） 前記プラノプロフェン１質量部に対し、クロロブタノールを０．０５質量部から１００質量部及びメントールを０．０２５質量部から１０質量部含有する（１）に記載の眼科用剤。 (2) The ophthalmic preparation according to (1), containing 0.05 to 100 parts by mass of chlorobutanol and 0.025 to 10 parts by mass of menthol with respect to 1 part by mass of the planoprofen.
（３） 更にメントールを含有する（１）又は（２）に記載の眼科用剤。 (3) The ophthalmic agent according to (1) or (2), further containing menthol.
（３）の発明によれば、メントールを含有したことによって、眼科用剤に清涼感を付与させることが可能となるため、使用の際に対象者に爽快感や効目感を印象付けることができるため、更に使用感の良い眼科用剤を提供することができる。また、プラノプロフェンの刺激を緩和する作用を有しているため、刺激がより低減された眼科用剤を提供することが可能となる。 According to the invention of (3), since it is possible to impart a refreshing feeling to the ophthalmic preparation by containing menthol, it is possible to impress the subject with a refreshing feeling or an effect feeling. Therefore, it is possible to provide an ophthalmic agent with better usability. Moreover, since it has the effect | action which eases the irritation | stimulation of pranoprofen, it becomes possible to provide the ophthalmic agent with which irritation | stimulation was reduced more.
（４） 前記メントールは、前記プラノプロフェン１質量部に対し、０．０２５質量部から１０質量部含有する（１）から（３）いずれかに記載の眼科用剤。 (4) The ophthalmic agent according to any one of (1) to (3), wherein the menthol is contained in an amount of 0.025 to 10 parts by mass with respect to 1 part by mass of the pranoprofen.
本発明の眼科用剤によれば、プラノプロフェンにクロロブタノール及びメントールを添加させることによって、プラノプロフェンによる刺激が緩和されるだけではなく、眼科用剤の使用感を改善することが可能となった。 According to the ophthalmic preparation of the present invention, by adding chlorobutanol and menthol to pranoprofen, it is possible not only to alleviate the irritation caused by pranoprofen but also to improve the feeling of use of the ophthalmic preparation. became.
以下、本発明について詳しく説明する。 The present invention will be described in detail below.
本発明に係る眼科用剤は「プラノプロフェン」を含有する。「プラノプロフェン」とは、α−メチル−５Ｈ−〔１〕ベンゾピラノ〔２，３−ｂ〕ピリジン−７−酢酸といい、下記の構造式で示される。またプラノプロフェンは、インドメタシンに代表される非ステロイド性鎮痛消炎剤の１つであり、シクロオキシゲナーゼを阻害し、炎症の原因物質プロスタグランジンの生成を抑制することで炎症部位の消炎鎮痛作用を示す物質でもある。プロピオン酸系の非ステロイド性抗炎症剤であり、インドメタシン等に比べて副作用の少ないのが特長である。医療用としては、ニフラン（登録商標）の販売名で市販されている。 The ophthalmic agent according to the present invention contains “planoprofen”. “Pranoprofen” is called α-methyl-5H- [1] benzopyrano [2,3-b] pyridine-7-acetic acid and is represented by the following structural formula. Planoprofen is a non-steroidal analgesic / anti-inflammatory agent typified by indomethacin, which inhibits cyclooxygenase and suppresses the production of prostaglandins that cause inflammation, thereby exhibiting anti-inflammatory analgesia at the site of inflammation. It is also a substance. Propionic acid-based non-steroidal anti-inflammatory agent with fewer side effects than indomethacin. For medical use, it is marketed under the name Niflan (registered trademark).
本発明に係る眼科用剤の主薬であるプラノプロフェンの使用濃度は症状に応じて適宜選択することができるが、０．００５〜０．２ｗ／ｖ％、特に０．０２５〜０．１ｗ／ｖ％であることが好ましい。 The concentration of pranoprofen, which is the main ingredient of the ophthalmic preparation according to the present invention, can be appropriately selected according to symptoms, but is 0.005 to 0.2 w / v%, particularly 0.025 to 0.1 w / It is preferably v%.
また、本発明に係る眼科用剤は「クロロブタノール」を含有する。「クロロブタノール」とは、下記の構造式で示されるものであり、殺菌効果を有する。クロロブタノールの使用濃度は必要に応じて適宜選択することができるが、０．０１〜０．５ｗ／ｖ％、特に０．０５〜０．３ｗ／ｖ％であることが好ましい。 The ophthalmic agent according to the present invention contains “chlorobutanol”. “Chlorobutanol” is represented by the following structural formula and has a bactericidal effect. The use concentration of chlorobutanol can be appropriately selected as necessary, but is preferably 0.01 to 0.5 w / v%, particularly preferably 0.05 to 0.3 w / v%.
さらにまた、本発明に係る眼科用剤は「メントール」を含有する。「メントール」とは、下記の化学式で示されるものであり、ハッカから採れ、独特の香りを有している。清涼感を与えるため、精油成分として幅広く利用されている。また、殺菌、防腐作用があり、かゆみを防止する効果もある。メントールの使用濃度は必要に応じて適宜選択することができるが、０．００５〜０．０５ｗ／ｖ％、特に０．０１〜０．０４ｗ／ｖ％であることが好ましい。なお、本発明におけるメントールとは、上記のメントールの他、メントールを含有する精油成分（例えばハッカ油、ハッカ水等）も含まれる。 Furthermore, the ophthalmic preparation according to the present invention contains “menthol”. “Menthol” is represented by the following chemical formula and is taken from mint and has a unique scent. In order to give a refreshing feeling, it is widely used as an essential oil component. In addition, it has bactericidal and antiseptic effects and has an effect of preventing itching. The use concentration of menthol can be appropriately selected as necessary, but is preferably 0.005 to 0.05 w / v%, particularly 0.01 to 0.04 w / v%. In addition, the menthol in this invention includes the essential oil component (for example, mint oil, mint water, etc.) containing menthol other than said menthol.
本発明に係る眼科用剤にはさらに緩衝剤、等張化剤、溶解補助剤、保存剤、粘稠剤、キレート剤、ｐＨ調整剤のような各種の添加剤を適宜添加してもよい。 Various additives such as a buffer, an isotonic agent, a solubilizing agent, a preservative, a thickener, a chelating agent, and a pH adjuster may be appropriately added to the ophthalmic agent according to the present invention.
緩衝剤としては、例えばリン酸塩緩衝剤（リン酸二水素ナトリウム−リン酸水素二ナトリウム、リン酸二水素カリウム−水酸化カリウム）、ホウ酸緩衝剤（ホウ酸−ホウ砂）、クエン酸塩緩衝剤（クエン酸ナトリウム−水酸化ナトリウム）、酒石酸塩緩衝剤（酒石酸−酒石酸ナトリウム）、酢酸塩緩衝剤（酢酸−酢酸ナトリウム）、炭酸塩緩衝剤（炭酸ナトリウム−クエン酸、炭酸ナトリウム−ホウ酸）、アミノ酸（グルタミン酸ナトリウム、イプシロンアミノカプロン酸）等が挙げられる。 Examples of the buffer include phosphate buffer (sodium dihydrogen phosphate-disodium hydrogen phosphate, potassium dihydrogen phosphate-potassium hydroxide), borate buffer (boric acid-borax), citrate Buffer (sodium citrate-sodium hydroxide), tartrate buffer (tartaric acid-sodium tartrate), acetate buffer (acetic acid-sodium acetate), carbonate buffer (sodium carbonate-citric acid, sodium carbonate-boric acid) ), Amino acids (sodium glutamate, epsilon aminocaproic acid) and the like.
等張化剤としては、ソルビトール、グルコース、マンニトール等の糖類、グリセリン、プロピレングリコール等の多価アルコール類、塩化ナトリウム、ホウ砂等の塩類、ホウ酸等が挙げられる。 Examples of the isotonic agent include saccharides such as sorbitol, glucose and mannitol, polyhydric alcohols such as glycerin and propylene glycol, salts such as sodium chloride and borax, and boric acid.
溶解補助剤としては、ポリオキシエチレンソルビタンモノオレート（ポリソルベート８０）、ポリオキシエチレンモノステアレート、ポリオキシエチレン硬化ヒマシ油等の非イオン界面活性剤やポリエチレングリコール等が挙げられる。 Examples of the solubilizer include nonionic surfactants such as polyoxyethylene sorbitan monooleate (polysorbate 80), polyoxyethylene monostearate, polyoxyethylene hydrogenated castor oil, and polyethylene glycol.
保存剤としては、塩化ベンザルコニウム、塩化ベンゼトニウム、塩化セチルピリジニウム等の第四級アンモニウム塩、パラオキシ安息香酸メチル、パラオキシ安息香酸エチル、パラオキシ安息香酸プロピル、パラオキシ安息香酸ブチル等のパラオキシ安息香酸エステル類、ベンジルアルコール、フェネチルアルコール、ソルビン酸及びそれらの塩、チメロサール、デヒドロ酢酸ナトリウム等が挙げられる。 Preservatives include quaternary ammonium salts such as benzalkonium chloride, benzethonium chloride, cetylpyridinium chloride, paraoxybenzoates such as methyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, and butyl paraoxybenzoate. Benzyl alcohol, phenethyl alcohol, sorbic acid and salts thereof, thimerosal, sodium dehydroacetate and the like.
粘稠剤としては、ポリビニルピロリドン、ヒドロキシエチルセルロース、ヒドロキシプロピルセルロース、メチルセルロース、ヒドロキシプロピルメチルセルロース、カルボキシメチルセルロース及びそれらの塩等が挙げられる。 Examples of the thickener include polyvinyl pyrrolidone, hydroxyethyl cellulose, hydroxypropyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, carboxymethyl cellulose, and salts thereof.
キレート剤としては、エデト酸ナトリウム、クエン酸等が挙げられる。ｐＨ調整剤としては、塩酸、クエン酸、リン酸、酢酸、酒石酸、水酸化ナトリウム、水酸化カリウム、炭酸ナトリウム及び炭酸水素ナトリウム等が挙げられる。 Examples of chelating agents include sodium edetate and citric acid. Examples of the pH adjuster include hydrochloric acid, citric acid, phosphoric acid, acetic acid, tartaric acid, sodium hydroxide, potassium hydroxide, sodium carbonate, and sodium bicarbonate.
本発明に係る眼科用剤は、点眼剤、洗眼剤等として使用される。点眼剤として用いる場合、ｐＨは５．０〜８．５であることが好ましく、５．０〜７．０であることが更に好ましい。また洗眼剤として用いる場合、ｐＨは５．５〜８．０であることが好ましく、５．５〜７．０であることが更に好ましい。 The ophthalmic preparation according to the present invention is used as an eye drop, an eye wash or the like. When used as an eye drop, the pH is preferably 5.0 to 8.5, and more preferably 5.0 to 7.0. When used as an eye wash, the pH is preferably 5.5 to 8.0, more preferably 5.5 to 7.0.
本発明に係る眼科用剤は、従来の方法で点眼剤又は洗眼剤として調製することができる。点眼剤は１日数回、１回１滴から数滴投与することができる。また、洗眼剤は１日数回、目の洗浄をすることができる。 The ophthalmic preparation according to the present invention can be prepared as an eye drop or an eye wash by a conventional method. Eye drops can be administered several times a day, one to several drops at a time. Further, the eye wash can wash the eyes several times a day.
以下に、本発明に係る眼科用剤の製剤処方例を示すが、これらの例は本発明をよりよく理解するためのものであり、本発明の範囲を限定するものではない。 Examples of the pharmaceutical formulation of the ophthalmic agent according to the present invention are shown below, but these examples are for better understanding of the present invention and do not limit the scope of the present invention.
〔実施例１〕
以下に本発明に係る眼科用剤の製造工程を示す。なお、本実施例では点眼剤として用いている。
[Example 1]
The manufacturing process of the ophthalmic preparation according to the present invention is shown below. In this embodiment, it is used as an eye drop.
精製水（８５ｍＬ）にホウ砂、ポリソルベート８０、プラノプロフェンを溶解させた後、クロロブタノール他各成分を添加し、溶解させ、希塩酸でｐＨを５．６に調節した後、全量を１００ｍＬとした。その後濾過滅菌を行ない、無菌の点眼剤とした。この点眼剤の浸透圧は３０２ｍＯｓｍであった。なお、浸透圧の測定方法は日本薬局方１４局浸透圧測定法（オスモル濃度測定法）に従って測定を行なった。 After dissolving borax, polysorbate 80, and pranoprofen in purified water (85 mL), chlorobutanol and other components were added and dissolved, and the pH was adjusted to 5.6 with dilute hydrochloric acid. . Thereafter, the solution was sterilized by filtration to obtain a sterile eye drop. The osmotic pressure of this eye drop was 302 mOsm. The osmotic pressure was measured according to the Japanese Pharmacopoeia 14 osmotic pressure measurement method (osmolarity measurement method).
〔実施例２〕
実施例１の眼科用剤に更にメントール１０ｍｇを添加した眼科用剤を本実施例における眼科用剤とした。
[Example 2]
The ophthalmic agent obtained by further adding 10 mg of menthol to the ophthalmic agent of Example 1 was used as the ophthalmic agent in this example.
〔比較例１〕
本発明の比較例として、実施例１の眼科用剤からクロロブタノールを除去した眼科用剤を作成した。
[Comparative Example 1]
As a comparative example of the present invention, an ophthalmic agent in which chlorobutanol was removed from the ophthalmic agent of Example 1 was prepared.
〔実施例３〕
健常者１０名に対し、上記実施例及び比較例の各点眼剤を１〜２滴づつ両眼に点眼し、点眼時の刺激感を下記の評価基準に従って評価した。このときの結果を表１に示す。
＜評価基準＞
スコアー０：刺激無し。
スコアー１：ほとんど刺激なし。
スコアー２：やや刺激あり。
スコアー３：刺激あり。
スコアー４：強い刺激あり。
Example 3
For 10 healthy subjects, 1 to 2 drops of each of the eye drops of the above Examples and Comparative Examples were instilled into both eyes, and the irritation feeling at the time of instillation was evaluated according to the following evaluation criteria. The results are shown in Table 1.
<Evaluation criteria>
Score 0: No irritation.
Score 1: Almost no irritation.
Score 2: Slightly irritating.
Score 3: There is irritation.
Score 4: Strong stimulation.
Claims (4)
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| JP2004054692A JP2005239681A (en) | 2004-02-27 | 2004-02-27 | Ophthalmic agent |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009096793A (en) * | 2007-06-01 | 2009-05-07 | Rohto Pharmaceut Co Ltd | Pranoprofen-containing aqueous pharmaceutical composition |
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