JP4776282B2 - コンタクトレンズ用組成物 - Google Patents
コンタクトレンズ用組成物 Download PDFInfo
- Publication number
- JP4776282B2 JP4776282B2 JP2005183540A JP2005183540A JP4776282B2 JP 4776282 B2 JP4776282 B2 JP 4776282B2 JP 2005183540 A JP2005183540 A JP 2005183540A JP 2005183540 A JP2005183540 A JP 2005183540A JP 4776282 B2 JP4776282 B2 JP 4776282B2
- Authority
- JP
- Japan
- Prior art keywords
- acid
- contact lens
- salt
- sodium
- composition
- 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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- 239000000203 mixture Substances 0.000 title claims description 73
- 150000003839 salts Chemical class 0.000 claims description 104
- 239000003889 eye drop Substances 0.000 claims description 31
- 229960000265 cromoglicic acid Drugs 0.000 claims description 25
- VLARUOGDXDTHEH-UHFFFAOYSA-L disodium cromoglycate Chemical compound [Na+].[Na+].O1C(C([O-])=O)=CC(=O)C2=C1C=CC=C2OCC(O)COC1=CC=CC2=C1C(=O)C=C(C([O-])=O)O2 VLARUOGDXDTHEH-UHFFFAOYSA-L 0.000 claims description 25
- 235000010199 sorbic acid Nutrition 0.000 claims description 19
- 229960003291 chlorphenamine Drugs 0.000 claims description 18
- SOYKEARSMXGVTM-UHFFFAOYSA-N chlorphenamine Chemical compound C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Cl)C=C1 SOYKEARSMXGVTM-UHFFFAOYSA-N 0.000 claims description 18
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 claims description 18
- 238000000034 method Methods 0.000 claims description 18
- 239000004334 sorbic acid Substances 0.000 claims description 18
- 229940075582 sorbic acid Drugs 0.000 claims description 18
- 235000002639 sodium chloride Nutrition 0.000 description 100
- -1 polyoxyethylene Polymers 0.000 description 59
- 229940012356 eye drops Drugs 0.000 description 23
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 20
- 239000003795 chemical substances by application Substances 0.000 description 16
- 238000009736 wetting Methods 0.000 description 16
- 230000000844 anti-bacterial effect Effects 0.000 description 14
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 13
- 229920005989 resin Polymers 0.000 description 10
- 239000011347 resin 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 9
- 230000000694 effects Effects 0.000 description 9
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- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 9
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 7
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 7
- 239000000872 buffer Substances 0.000 description 7
- 239000003755 preservative agent Substances 0.000 description 7
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 6
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 6
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 description 6
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 6
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 6
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- 239000011734 sodium Substances 0.000 description 6
- 229910052708 sodium Inorganic materials 0.000 description 6
- XOAAWQZATWQOTB-UHFFFAOYSA-N taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 description 6
- 239000012085 test solution Substances 0.000 description 6
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 6
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 5
- 239000002253 acid Substances 0.000 description 5
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- UCTWMZQNUQWSLP-VIFPVBQESA-N (R)-adrenaline Chemical compound CNC[C@H](O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-VIFPVBQESA-N 0.000 description 4
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 4
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 4
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 4
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 4
- BAVYZALUXZFZLV-UHFFFAOYSA-N Methylamine Chemical compound NC BAVYZALUXZFZLV-UHFFFAOYSA-N 0.000 description 4
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- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 4
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 description 4
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 description 4
- 239000004372 Polyvinyl alcohol Substances 0.000 description 4
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 4
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 4
- KKEYFWRCBNTPAC-UHFFFAOYSA-N Terephthalic acid Chemical compound OC(=O)C1=CC=C(C(O)=O)C=C1 KKEYFWRCBNTPAC-UHFFFAOYSA-N 0.000 description 4
- 239000000654 additive Substances 0.000 description 4
- 229940024606 amino acid Drugs 0.000 description 4
- 235000001014 amino acid Nutrition 0.000 description 4
- IISBACLAFKSPIT-UHFFFAOYSA-N bisphenol A Chemical compound C=1C=C(O)C=CC=1C(C)(C)C1=CC=C(O)C=C1 IISBACLAFKSPIT-UHFFFAOYSA-N 0.000 description 4
- 229910021538 borax Inorganic materials 0.000 description 4
- 239000001768 carboxy methyl cellulose Substances 0.000 description 4
- 239000004359 castor oil Substances 0.000 description 4
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- 229920002678 cellulose Polymers 0.000 description 4
- 239000001913 cellulose Substances 0.000 description 4
- 235000010980 cellulose Nutrition 0.000 description 4
- 210000004087 cornea Anatomy 0.000 description 4
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 4
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 4
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 description 4
- 239000007951 isotonicity adjuster Substances 0.000 description 4
- 239000002736 nonionic surfactant Substances 0.000 description 4
- 239000003002 pH adjusting agent Substances 0.000 description 4
- XNGIFLGASWRNHJ-UHFFFAOYSA-N phthalic acid Chemical compound OC(=O)C1=CC=CC=C1C(O)=O XNGIFLGASWRNHJ-UHFFFAOYSA-N 0.000 description 4
- 239000011112 polyethylene naphthalate Substances 0.000 description 4
- 229920002451 polyvinyl alcohol Polymers 0.000 description 4
- SCVFZCLFOSHCOH-UHFFFAOYSA-M potassium acetate Chemical compound [K+].CC([O-])=O SCVFZCLFOSHCOH-UHFFFAOYSA-M 0.000 description 4
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- QAQSNXHKHKONNS-UHFFFAOYSA-N 1-ethyl-2-hydroxy-4-methyl-6-oxopyridine-3-carboxamide Chemical compound CCN1C(O)=C(C(N)=O)C(C)=CC1=O QAQSNXHKHKONNS-UHFFFAOYSA-N 0.000 description 3
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 description 3
- SLXKOJJOQWFEFD-UHFFFAOYSA-N 6-aminohexanoic acid Chemical compound NCCCCCC(O)=O SLXKOJJOQWFEFD-UHFFFAOYSA-N 0.000 description 3
- BTBUEUYNUDRHOZ-UHFFFAOYSA-N Borate Chemical compound [O-]B([O-])[O-] BTBUEUYNUDRHOZ-UHFFFAOYSA-N 0.000 description 3
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 description 3
- 208000002177 Cataract Diseases 0.000 description 3
- 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 3
- 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 3
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- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 3
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 3
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 3
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 3
- 229930195725 Mannitol Natural products 0.000 description 3
- 235000006679 Mentha X verticillata Nutrition 0.000 description 3
- 235000002899 Mentha suaveolens Nutrition 0.000 description 3
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- 229910002651 NO3 Inorganic materials 0.000 description 3
- DJDFFEBSKJCGHC-UHFFFAOYSA-N Naphazoline Chemical compound Cl.C=1C=CC2=CC=CC=C2C=1CC1=NCCN1 DJDFFEBSKJCGHC-UHFFFAOYSA-N 0.000 description 3
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 description 3
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Description
しかし、クロモグリク酸又はその塩、ソルビン酸又はその塩、およびクロルフェニラミン又はその塩がコンタクトレンズの濡れを増強することは知られていない。
また、本発明の他の目的は、コンタクトレンズの濡れ増強方法を提供することである。
(1)クロモグリク酸又はその塩、ソルビン酸又はその塩、およびクロルフェニラミン又はその塩を含有することを特徴とする、コンタクトレンズ用組成物。
(2)コンタクトレンズ用組成物が、コンタクトレンズ用液剤組成物である(1)に記載のコンタクトレンズ用組成物。
(3)コンタクトレンズ用組成物が、コンタクトレンズ用点眼薬、コンタクトレンズ用洗眼薬、コンタクトレンズ装着液、コンタクトレンズケア用剤である(1)または(2)に記載のコンタクトレンズ用組成物。
また、本発明はコンタクトレンズの濡れ増強方法をも包含する。
(4)クロモグリク酸又はその塩、ソルビン酸又はその塩、およびクロルフェニラミン又はその塩を配合した組成物をコンタクトレンズに接触させることを特徴とする、コンタクトレンズの濡れ増強方法。
また、本明細書中、「塩」とは薬理学的に又は生理学的に許容される塩を意味する。
これらのクロモグリク酸またはその塩は、単独で又は二種以上組み合わせて使用できる。また、クロモグリク酸又はその塩は、水和物の形態で使用できる。
これらのソルビン酸またはその塩は、単独で又は二種以上組み合わせて使用できる。
これらのクロルフェニラミンまたはその塩は、単独で又は二種以上組み合わせて使用できる。
クエン酸緩衝剤、酢酸緩衝剤、炭酸緩衝剤、ホウ酸緩衝剤、リン酸緩衝剤としては、それぞれクエン酸又はその塩(クエン酸ナトリウム、クエン酸カリウムなど)、酢酸又はその塩(酢酸カリウム、酢酸ナトリウムなど)、炭酸又はその塩(炭酸水素ナトリウム、炭酸ナトリウムなど)、ホウ酸またはその塩(テトラホウ酸カリウム、ホウ酸ナトリウム、ホウ砂、メタホウ酸カリウムなど)、リン酸又はその塩(リン酸水素二ナトリウム、リン酸二水素ナトリウム、リン酸二水素カリウム、リン酸水素二カリウムなど)などが挙げられる。
本発明のコンタクトレンズ用組成物中におけるこれらの緩衝剤の濃度は、例えば、0.001〜10%、好ましくは、0.01〜5%程度である。
本発明のコンタクトレンズ用組成物中におけるこれらのpH調整剤の濃度は、例えば、例えば、0.00001〜5%、好ましくは、0.0001〜2%程度である。
本発明のコンタクトレンズ用組成物中におけるこれらの等張化剤の濃度は、例えば、0.001〜10%、好ましくは、0.01〜5%程度である。
pHの調整は、前記緩衝剤、pH調整剤など、浸透圧の調整は前記等張化剤などを用いて行うことができる。
より具体的には,コンタクトレンズ用組成物中の各成分の含有量は、例えば、以下の通りである。
眼筋調節薬成分:例えば、0.0001〜0.5%、好ましくは、0.0005〜0.1%、さらに好ましくは0.0005〜0.01%。
抗炎症薬成分または収斂薬成分:例えば、0.0001〜10%、好ましくは0.0001〜5%。
抗ヒスタミン薬成分または抗アレルギー薬成分:例えば、0.0001〜10%、好ましくは0.001〜5%。
ビタミン類:例えば、0.0001〜1%、好ましくは、0.0001〜0.5%。
アミノ酸類:例えば、0.0001〜10%、好ましくは0.001〜3%。
抗菌薬成分または殺菌薬成分:例えば、0.00001〜10%、好ましくは、0.0001〜10%。
糖類:例えば、0.0001〜5%、好ましくは0.001〜5%、さらに好ましくは0.01〜2%。
多糖類又はその誘導体:例えば、0.0001〜2%、好ましくは0.01〜2%、さらに好ましくは0.01〜1%。
セルロース又はその誘導体又はそれらの塩:例えば、0.001〜5%、好ましくは0.01〜1%。
前述以外の水溶性高分子:例えば、0.001〜10%、好ましくは0.001〜5%、さらに好ましくは0.01〜3%。
局所麻酔薬成分:例えば、0.001〜1%、好ましくは0.01〜1%。
ステロイド成分:例えば、0.001〜1%、好ましくは0.01〜1%。
緑内障治療成分:例えば、0.001〜5%、好ましくは0.01〜1%。
白内障治療成分:例えば、0.0001〜10%、好ましくは0.001〜5%。
また、本発明のコンタクトレンズ用組成物には、発明の効果を損なわない範囲であれば、その用途や形態に応じて、常法に従い、様々な成分や添加物を適宜選択し、一種またはそれ以上を併用して含有させてもよい。それらの成分または添加物として、例えば、半固形剤や液剤などの調製に一般的に使用される担体(水、水性溶媒、水性または油性基剤など)、糖類、防腐剤、殺菌剤又は抗菌剤、香料または清涼化剤、キレート剤などの各種添加剤を挙げることができる。
以下に本発明のコンタクトレンズ用組成物に使用される代表的な成分を例示するが、これらに限定されない。
糖アルコール類:例えば、キシリトール、ソルビトール、マンニトールなど。
これらはd体、l体又はdl体のいずれでもよい。
防腐剤、殺菌剤又は抗菌剤:例えば、0.00001〜5%、好ましくは、0.0001〜2%。
香料または清涼化剤:例えば、0.00001〜5%、好ましくは、0.0001〜2%。
キレート剤:例えば、0.00001〜5%、好ましくは、0.0001〜2%。
ポリカーボネート系樹脂としては、例えば、ビスフェノール類(ビスフェノール−Aなど)をベースとする芳香族ポリカーボネートが挙げられる。
具体例としては、コンタクトレンズ用点眼薬(剤)(ハードまたはソフトコンタクトレンズ装用中にも使用することができる一般点眼薬、抗菌点眼薬、人工涙液型点眼薬を含む)をコンタクトレンズ装用中に点眼する行為、コンタクトレンズ用洗眼薬(剤)(ハードまたはソフトコンタクトレンズを装用中にも使用することができる洗眼薬を含む)をコンタクトレンズを装用したまま洗眼する行為、コンタクトレンズ装用前にコンタクトレンズ装着液でコンタクトレンズを濡らす行為、コンタクトレンズケア用剤(コンタクトレンズ消毒剤、コンタクトレンズ用保存剤、コンタクトレンズ用洗浄剤、コンタクトレンズ用洗浄保存剤など)をコンタクトレンズを脱着した後に使用する行為等を挙げる事ができるが、これらに限定されない。好ましくはコンタクトレンズ用点眼薬(剤)(ハードまたはソフトコンタクトレンズ装用中にも使用することができる一般点眼薬、抗菌点眼薬、人工涙液型点眼薬を含む)をコンタクトレンズ装用中に点眼する行為、コンタクトレンズ用洗眼薬(剤)(ハードまたはソフトコンタクトレンズを装用中にも使用することができる洗眼薬を含む)をコンタクトレンズを装用したまま洗眼する行為である。
表1に記載の実施例1および比較例1〜5の処方に従い、各成分を滅菌精製水に溶解して全量を100mLとして試験液を調製した。
次に、コンタクトレンズ(ジョンソン&ジョンソン社製 ワンデーアキュビュー(登録商標))を一昼夜生理食塩水に浸漬した後4等分し、切片の1つをフロントカーブ(角膜と接触しない側)を上にして平面状に置き、リントフリー(登録商標:旭化成社製)にてレンズ表面の水分を軽くふき取った。レンズ切片上に試験液3μLを静かに滴下し、滴下10秒後の状態をCCDカメラ(KEYENCE社製 2.1MEGAPIXEL VH8000)にてコンタクトレンズの側面から写真撮影した。
コンタクトレンズ表面、試験液、空気の接触点をPとし、Pから試験液に引いた接線と、コンタクトレンズ表面に引いた接線のなす角のうち、試験液を含む側の角を接触角θとし、以下の式により精製水の接触角との差Δを算出した。試験は各試験液について5回実施し、その平均値をΔ(平均値)とした。
Δ = 精製水のθ − 各実施例、比較例のθ
結果を表1に示す。
θが小さいほどコンタクトレンズ表面が濡れやすい状態であることを意味するため、Δが大きいほどレンズがよく濡れることを示している。
Claims (6)
- (A)クロモグリク酸又はその塩、(B)ソルビン酸又はその塩、および(C)クロルフェニラミン又はその塩を含有し、ここで前記(A)成分1重量部に対する前記(B)成分が0.01〜4重量部であることを特徴とする、コンタクトレンズ用点眼剤。
- (A)クロモグリク酸又はその塩の含有量が0.0001〜5w/v%である、請求項1に記載のコンタクトレンズ用点眼剤。
- (B)ソルビン酸又はその塩の含有量が0.001〜2w/v%である、請求項1又は2に記載のコンタクトレンズ用点眼剤。
- (A)成分1重量部に対する(C)成分が0.0003〜5重量部であることを特徴とする、請求項1〜3のいずれか1項に記載のコンタクトレンズ用点眼剤。
- (C)クロルフェニラミン又はその塩の含有量が0.0001〜3w/v%である、請求項1〜4のいずれか1項に記載のコンタクトレンズ用点眼剤。
- (A)クロモグリク酸又はその塩、(B)ソルビン酸又はその塩、および(C)クロルフェニラミン又はその塩を配合した組成物をコンタクトレンズに接触させることを特徴とする、コンタクトレンズの濡れ増強方法。
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