JP2006321790A - 眼科用剤 - Google Patents
眼科用剤 Download PDFInfo
- Publication number
- JP2006321790A JP2006321790A JP2006110138A JP2006110138A JP2006321790A JP 2006321790 A JP2006321790 A JP 2006321790A JP 2006110138 A JP2006110138 A JP 2006110138A JP 2006110138 A JP2006110138 A JP 2006110138A JP 2006321790 A JP2006321790 A JP 2006321790A
- Authority
- JP
- Japan
- Prior art keywords
- ophthalmic
- zinc
- solution
- zinc sulfate
- eye
- 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.)
- Granted
Links
- 239000003732 agents acting on the eye Substances 0.000 title claims abstract description 20
- 229940125702 ophthalmic agent Drugs 0.000 title claims abstract description 20
- -1 polyoxyethylene Polymers 0.000 claims abstract description 32
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims abstract description 29
- 239000004359 castor oil Substances 0.000 claims abstract description 28
- NWONKYPBYAMBJT-UHFFFAOYSA-L zinc sulfate Chemical compound [Zn+2].[O-]S([O-])(=O)=O NWONKYPBYAMBJT-UHFFFAOYSA-L 0.000 claims abstract description 24
- 229960001763 zinc sulfate Drugs 0.000 claims abstract description 24
- 229910000368 zinc sulfate Inorganic materials 0.000 claims abstract description 24
- 229940088594 vitamin Drugs 0.000 claims abstract description 17
- 229930003231 vitamin Natural products 0.000 claims abstract description 17
- 235000013343 vitamin Nutrition 0.000 claims abstract description 17
- 239000011782 vitamin Substances 0.000 claims abstract description 17
- CANRESZKMUPMAE-UHFFFAOYSA-L Zinc lactate Chemical compound [Zn+2].CC(O)C([O-])=O.CC(O)C([O-])=O CANRESZKMUPMAE-UHFFFAOYSA-L 0.000 claims abstract description 15
- 239000011576 zinc lactate Substances 0.000 claims abstract description 15
- 229940050168 zinc lactate Drugs 0.000 claims abstract description 15
- 235000000193 zinc lactate Nutrition 0.000 claims abstract description 15
- 239000002736 nonionic surfactant Substances 0.000 claims abstract description 8
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- 238000002360 preparation method Methods 0.000 claims description 11
- 239000002826 coolant Substances 0.000 claims description 3
- 206010015958 Eye pain Diseases 0.000 abstract description 10
- 239000003795 chemical substances by application Substances 0.000 abstract description 3
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- 238000001914 filtration Methods 0.000 description 10
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- 239000002997 ophthalmic solution Substances 0.000 description 9
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- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 description 6
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- 229910052725 zinc Inorganic materials 0.000 description 6
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- NOOLISFMXDJSKH-KXUCPTDWSA-N (-)-Menthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@H]1O NOOLISFMXDJSKH-KXUCPTDWSA-N 0.000 description 4
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 4
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- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
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- QGNJRVVDBSJHIZ-QHLGVNSISA-N retinyl acetate Chemical compound CC(=O)OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C QGNJRVVDBSJHIZ-QHLGVNSISA-N 0.000 description 3
- 208000024891 symptom Diseases 0.000 description 3
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- REPVLJRCJUVQFA-UHFFFAOYSA-N (-)-isopinocampheol Natural products C1C(O)C(C)C2C(C)(C)C1C2 REPVLJRCJUVQFA-UHFFFAOYSA-N 0.000 description 2
- OILXMJHPFNGGTO-UHFFFAOYSA-N (22E)-(24xi)-24-methylcholesta-5,22-dien-3beta-ol Natural products C1C=C2CC(O)CCC2(C)C2C1C1CCC(C(C)C=CC(C)C(C)C)C1(C)CC2 OILXMJHPFNGGTO-UHFFFAOYSA-N 0.000 description 2
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- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical compound C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 description 2
- 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 2
- FPIPGXGPPPQFEQ-UHFFFAOYSA-N 13-cis retinol Natural products OCC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-UHFFFAOYSA-N 0.000 description 2
- OQMZNAMGEHIHNN-UHFFFAOYSA-N 7-Dehydrostigmasterol Natural products C1C(O)CCC2(C)C(CCC3(C(C(C)C=CC(CC)C(C)C)CCC33)C)C3=CC=C21 OQMZNAMGEHIHNN-UHFFFAOYSA-N 0.000 description 2
- 241000723346 Cinnamomum camphora Species 0.000 description 2
- DNVPQKQSNYMLRS-NXVQYWJNSA-N Ergosterol Natural products CC(C)[C@@H](C)C=C[C@H](C)[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O)CC[C@]4(C)[C@@H]3CC[C@]12C DNVPQKQSNYMLRS-NXVQYWJNSA-N 0.000 description 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 2
- GLZPCOQZEFWAFX-UHFFFAOYSA-N Geraniol Chemical compound CC(C)=CCCC(C)=CCO GLZPCOQZEFWAFX-UHFFFAOYSA-N 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- FPIPGXGPPPQFEQ-BOOMUCAASA-N Vitamin A Natural products OC/C=C(/C)\C=C\C=C(\C)/C=C/C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-BOOMUCAASA-N 0.000 description 2
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 description 2
- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical compound NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 description 2
- 230000003110 anti-inflammatory effect Effects 0.000 description 2
- CKDOCTFBFTVPSN-UHFFFAOYSA-N borneol Natural products C1CC2(C)C(C)CC1C2(C)C CKDOCTFBFTVPSN-UHFFFAOYSA-N 0.000 description 2
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- DTGKSKDOIYIVQL-UHFFFAOYSA-N dl-isoborneol Natural products C1CC2(C)C(O)CC1C2(C)C DTGKSKDOIYIVQL-UHFFFAOYSA-N 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- DNVPQKQSNYMLRS-SOWFXMKYSA-N ergosterol Chemical compound C1[C@@H](O)CC[C@]2(C)[C@H](CC[C@]3([C@H]([C@H](C)/C=C/[C@@H](C)C(C)C)CC[C@H]33)C)C3=CC=C21 DNVPQKQSNYMLRS-SOWFXMKYSA-N 0.000 description 2
- 238000004128 high performance liquid chromatography Methods 0.000 description 2
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- SPSPIUSUWPLVKD-UHFFFAOYSA-N 2,3-dibutyl-6-methylphenol Chemical compound CCCCC1=CC=C(C)C(O)=C1CCCC SPSPIUSUWPLVKD-UHFFFAOYSA-N 0.000 description 1
- 229930024421 Adenine Natural products 0.000 description 1
- GFFGJBXGBJISGV-UHFFFAOYSA-N Adenine Chemical compound NC1=NC=NC2=C1N=CN2 GFFGJBXGBJISGV-UHFFFAOYSA-N 0.000 description 1
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- VKJGBAJNNALVAV-UHFFFAOYSA-M Berberine chloride (TN) Chemical compound [Cl-].C1=C2CC[N+]3=CC4=C(OC)C(OC)=CC=C4C=C3C2=CC2=C1OCO2 VKJGBAJNNALVAV-UHFFFAOYSA-M 0.000 description 1
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- 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
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- AUNGANRZJHBGPY-SCRDCRAPSA-N Riboflavin Chemical compound OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-SCRDCRAPSA-N 0.000 description 1
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- 201000009310 astigmatism Diseases 0.000 description 1
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- 229910021538 borax Inorganic materials 0.000 description 1
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- XOAAWQZATWQOTB-UHFFFAOYSA-N taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 description 1
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- BJORNXNYWNIWEY-UHFFFAOYSA-N tetrahydrozoline hydrochloride Chemical compound Cl.N1CCN=C1C1C2=CC=CC=C2CCC1 BJORNXNYWNIWEY-UHFFFAOYSA-N 0.000 description 1
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- 229940046009 vitamin E Drugs 0.000 description 1
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- 150000003722 vitamin derivatives Chemical class 0.000 description 1
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Abstract
【解決手段】本発明は、以下の(a)、(b)及び(c)を含有することを特徴とする眼科用剤である。
(a)硫酸亜鉛及び乳酸亜鉛の一種以上
(b)脂溶性ビタミン類
(c)ポリオキシエチレン硬化ヒマシ油類、ポリオキシエチレンヒマシ油類及びポリソルベート類から選ばれる1種又は2種以上の非イオン界面活性剤
また、さらに清涼化剤を含有することを特徴とする眼科用剤である。
【選択図】 なし
Description
(a)硫酸亜鉛及び乳酸亜鉛の一種以上
(b)脂溶性ビタミン類
(c)ポリオキシエチレン硬化ヒマシ油類、ポリオキシエチレンヒマシ油類及びポリソルベート類から選ばれる1種又は2種以上の非イオン界面活性剤
実施例1の点眼剤からパルミチン酸レチノールを除去し、他の成分は同量(下記表3に記載、各成分の配合量の単位はmg/100mLである)とした点眼剤を得た。
実施例1の点眼剤からポリオキシエチレン硬化ヒマシ油60を除去し、他の成分は同量(下記表3に記載、各成分の配合量の単位はmg/100mLである)とした点眼剤を得た。
実施例2の点眼剤からポリオキシエチレン硬化ヒマシ油60を除去し、他の成分は同量(下記表3に記載、各成分の配合量の単位はmg/100mLである)とした点眼剤を得た。
実施例1の点眼剤からポリオキシエチレン硬化ヒマシ油60の代わりにポリオキシエチレン200 ポリプロピレン70グリコールを添加し、他の成分は同量(下記表3に記載、各成分の配合量の単位はmg/100mLである)とした点眼剤を得た。
実施例1の点眼剤からポリオキシエチレン硬化ヒマシ油60の代わりにステアリン酸ポリオキシル40を添加し、他の成分は同量(下記表3に記載、各成分の配合量の単位はmg/100mLである)とした点眼剤を得た。
健常者4名に対し、実施例1〜10及び比較例1〜5で得た点眼剤を点眼し、使用時の刺激感と霧視の有無を評価した。なお、点眼剤は1〜2滴ずつ両眼に点眼した。このときの結果を表1〜表3に示した。本発明の点眼剤は、点眼時に眼痛を生じず、かつ霧視を生じないことが示された。
(刺激)
スコア−0:刺激無し。
スコア−1:ほとんど刺激なし。
スコア−2:やや刺激あり。
スコア−3:刺激あり。
スコア−4:強い刺激あり。
スコア−0:霧視なし。
スコア−1:ほとんど霧視なし。
スコア−2:やや霧視あり。
スコア−3:霧視あり。
スコア−4:強い霧視あり。
実施例1、実施例4及び実施例8で得た点眼剤をガラスアンプルに充填し、50℃に保った。10日後のパルミチン酸レチノールの残存量を下記に示した高速液体クロマトグラフ法で測定した。結果を表4に示す。本発明の点眼剤は、パルミチン酸レチノールを安定に保存できることが示された。特に、ポリオキシエチレン硬化ヒマシ油60とポリオキシエチレンヒマシ油35がパルミチン酸レチノールを安定に保存できることが示された。
試料中のパルミチン酸レチノールをプロピオン酸エルゴステロールを内標準物質に用いて高速液体クロマトグラフ法で測定した。即ち、試料水溶液2mLを正確に量り、内標準溶液(プロピオン酸エルゴステロールの2−プロパノール/テトラヒドロフラン(3:2)混液溶液(3→1000))2mLを正確に加え、これに2−プロパノール/テトラヒドロフラン(3:2)混液を加えて10mLとし、試料溶液とした。
カラム:資生堂カプセルパック UG120 4.6mm× 150mm
溶離液:液体クロマトグラフ用アセトニトリル/水/リン酸 = 980/20/1
検出器:紫外吸光光度計(測定波長280nm)
流速:パルミチン酸レチノールのピークが約25分に検出されるように調整した(通例1mL/分)。
Claims (2)
- 以下の(a)、(b)及び(c)を含有することを特徴とする眼科用剤。
(a)硫酸亜鉛及び乳酸亜鉛の一種以上
(b)脂溶性ビタミン類
(c)ポリオキシエチレン硬化ヒマシ油類、ポリオキシエチレンヒマシ油類及びポリソルベート類から選ばれる1種又は2種以上の非イオン界面活性剤 - さらに清涼化剤を含有することを特徴とする請求項1に記載の眼科用剤。
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WO2012090985A1 (ja) * | 2010-12-28 | 2012-07-05 | ロート製薬株式会社 | 水性眼科組成物 |
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KR20150018509A (ko) * | 2012-06-08 | 2015-02-23 | 라이온 가부시키가이샤 | 점막용 조성물 |
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