JPWO2017094508A1 - 眼科組成物 - Google Patents
眼科組成物 Download PDFInfo
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- JPWO2017094508A1 JPWO2017094508A1 JP2017553762A JP2017553762A JPWO2017094508A1 JP WO2017094508 A1 JPWO2017094508 A1 JP WO2017094508A1 JP 2017553762 A JP2017553762 A JP 2017553762A JP 2017553762 A JP2017553762 A JP 2017553762A JP WO2017094508 A1 JPWO2017094508 A1 JP WO2017094508A1
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- 229910052939 potassium sulfate Inorganic materials 0.000 description 1
- 235000011151 potassium sulphates Nutrition 0.000 description 1
- NMMVKSMGBDRONO-UHFFFAOYSA-N potassium;9-methyl-3-(1,2,4-triaza-3-azanidacyclopenta-1,4-dien-5-yl)pyrido[1,2-a]pyrimidin-4-one Chemical compound [K+].CC1=CC=CN(C2=O)C1=NC=C2C1=NN=N[N-]1 NMMVKSMGBDRONO-UHFFFAOYSA-N 0.000 description 1
- JVUYWILPYBCNNG-UHFFFAOYSA-N potassium;oxido(oxo)borane Chemical compound [K+].[O-]B=O JVUYWILPYBCNNG-UHFFFAOYSA-N 0.000 description 1
- 229960003101 pranoprofen Drugs 0.000 description 1
- 229960004919 procaine Drugs 0.000 description 1
- MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 description 1
- 235000013930 proline Nutrition 0.000 description 1
- ULWHHBHJGPPBCO-UHFFFAOYSA-N propane-1,1-diol Chemical compound CCC(O)O ULWHHBHJGPPBCO-UHFFFAOYSA-N 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 description 1
- ZUFQODAHGAHPFQ-UHFFFAOYSA-N pyridoxine hydrochloride Chemical compound Cl.CC1=NC=C(CO)C(CO)=C1O ZUFQODAHGAHPFQ-UHFFFAOYSA-N 0.000 description 1
- 229960004172 pyridoxine hydrochloride Drugs 0.000 description 1
- 235000019171 pyridoxine hydrochloride Nutrition 0.000 description 1
- 239000011764 pyridoxine hydrochloride Substances 0.000 description 1
- MIXMJCQRHVAJIO-TZHJZOAOSA-N qk4dys664x Chemical compound O.C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O.C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O MIXMJCQRHVAJIO-TZHJZOAOSA-N 0.000 description 1
- MCJGNVYPOGVAJF-UHFFFAOYSA-N quinolin-8-ol Chemical compound C1=CN=C2C(O)=CC=CC2=C1 MCJGNVYPOGVAJF-UHFFFAOYSA-N 0.000 description 1
- 229950004535 rebamipide Drugs 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000008439 repair process Effects 0.000 description 1
- 229960000342 retinol acetate Drugs 0.000 description 1
- 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 1
- 235000019173 retinyl acetate Nutrition 0.000 description 1
- 239000011770 retinyl acetate Substances 0.000 description 1
- 229940108325 retinyl palmitate Drugs 0.000 description 1
- 235000019172 retinyl palmitate Nutrition 0.000 description 1
- 239000011769 retinyl palmitate Substances 0.000 description 1
- XWGJFPHUCFXLBL-UHFFFAOYSA-M rongalite Chemical compound [Na+].OCS([O-])=O XWGJFPHUCFXLBL-UHFFFAOYSA-M 0.000 description 1
- 239000010666 rose oil Substances 0.000 description 1
- 235000019719 rose oil Nutrition 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- GQTHJBOWLPZUOI-FJXQXJEOSA-M sodium D-pantothenate Chemical compound [Na+].OCC(C)(C)[C@@H](O)C(=O)NCCC([O-])=O GQTHJBOWLPZUOI-FJXQXJEOSA-M 0.000 description 1
- 239000001632 sodium acetate Substances 0.000 description 1
- 235000017281 sodium acetate Nutrition 0.000 description 1
- 229960004249 sodium acetate Drugs 0.000 description 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
- 235000010234 sodium benzoate Nutrition 0.000 description 1
- 239000004299 sodium benzoate Substances 0.000 description 1
- 229960003885 sodium benzoate Drugs 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 235000017550 sodium carbonate Nutrition 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 235000019259 sodium dehydroacetate Nutrition 0.000 description 1
- 229940079839 sodium dehydroacetate Drugs 0.000 description 1
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
- 235000010262 sodium metabisulphite Nutrition 0.000 description 1
- 229940068459 sodium pantothenate Drugs 0.000 description 1
- 239000001488 sodium phosphate Substances 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- DSOWAKKSGYUMTF-GZOLSCHFSA-M sodium;(1e)-1-(6-methyl-2,4-dioxopyran-3-ylidene)ethanolate Chemical compound [Na+].C\C([O-])=C1/C(=O)OC(C)=CC1=O DSOWAKKSGYUMTF-GZOLSCHFSA-M 0.000 description 1
- XTXYCJOBMKKQOW-UHFFFAOYSA-N sodium;(4-aminophenyl)sulfonyl-(2,6-dimethylpyrimidin-4-yl)azanide Chemical compound [Na+].CC1=NC(C)=CC([N-]S(=O)(=O)C=2C=CC(N)=CC=2)=N1 XTXYCJOBMKKQOW-UHFFFAOYSA-N 0.000 description 1
- GEYJUFBPCGDENK-UHFFFAOYSA-M sodium;3,8-dimethyl-5-propan-2-ylazulene-1-sulfonate Chemical compound [Na+].CC(C)C1=CC=C(C)C2=C(S([O-])(=O)=O)C=C(C)C2=C1 GEYJUFBPCGDENK-UHFFFAOYSA-M 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 235000019721 spearmint oil Nutrition 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 229960000654 sulfafurazole Drugs 0.000 description 1
- 229960005404 sulfamethoxazole Drugs 0.000 description 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
- JLKIGFTWXXRPMT-UHFFFAOYSA-N sulphamethoxazole Chemical compound O1C(C)=CC(NS(=O)(=O)C=2C=CC(N)=CC=2)=N1 JLKIGFTWXXRPMT-UHFFFAOYSA-N 0.000 description 1
- 229940104261 taurate Drugs 0.000 description 1
- 229960003080 taurine Drugs 0.000 description 1
- 229940021790 tetrahydrozoline hydrochloride Drugs 0.000 description 1
- 229960000337 tetryzoline Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- OGIDPMRJRNCKJF-UHFFFAOYSA-N titanium oxide Inorganic materials [Ti]=O OGIDPMRJRNCKJF-UHFFFAOYSA-N 0.000 description 1
- 229940042585 tocopherol acetate Drugs 0.000 description 1
- GYDJEQRTZSCIOI-LJGSYFOKSA-N tranexamic acid Chemical compound NC[C@H]1CC[C@H](C(O)=O)CC1 GYDJEQRTZSCIOI-LJGSYFOKSA-N 0.000 description 1
- 229960000401 tranexamic acid Drugs 0.000 description 1
- 229960005342 tranilast Drugs 0.000 description 1
- NZHGWWWHIYHZNX-CSKARUKUSA-N tranilast Chemical compound C1=C(OC)C(OC)=CC=C1\C=C\C(=O)NC1=CC=CC=C1C(O)=O NZHGWWWHIYHZNX-CSKARUKUSA-N 0.000 description 1
- WYXIGTJNYDDFFH-UHFFFAOYSA-Q triazanium;borate Chemical compound [NH4+].[NH4+].[NH4+].[O-]B([O-])[O-] WYXIGTJNYDDFFH-UHFFFAOYSA-Q 0.000 description 1
- 229910000404 tripotassium phosphate Inorganic materials 0.000 description 1
- 235000019798 tripotassium phosphate Nutrition 0.000 description 1
- IYKMDRMCUIFHRA-UHFFFAOYSA-H tripotassium;trisodium;2-hydroxypropane-1,2,3-tricarboxylate;hydrate Chemical compound O.[Na+].[Na+].[Na+].[K+].[K+].[K+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O IYKMDRMCUIFHRA-UHFFFAOYSA-H 0.000 description 1
- BSVBQGMMJUBVOD-UHFFFAOYSA-N trisodium borate Chemical compound [Na+].[Na+].[Na+].[O-]B([O-])[O-] BSVBQGMMJUBVOD-UHFFFAOYSA-N 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 229910000406 trisodium phosphate Inorganic materials 0.000 description 1
- 235000019801 trisodium phosphate Nutrition 0.000 description 1
- 229960000281 trometamol Drugs 0.000 description 1
- 229960004791 tropicamide Drugs 0.000 description 1
- 239000004474 valine Substances 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000008215 water for injection Substances 0.000 description 1
- 239000003871 white petrolatum Substances 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
- 239000011592 zinc chloride Substances 0.000 description 1
- 235000005074 zinc chloride Nutrition 0.000 description 1
- 229960001939 zinc chloride Drugs 0.000 description 1
- 239000011787 zinc oxide Substances 0.000 description 1
- 235000014692 zinc oxide Nutrition 0.000 description 1
Classifications
-
- 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
- A61K31/13—Amines
- A61K31/133—Amines having hydroxy groups, e.g. sphingosine
-
- 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
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
- A61L12/00—Methods or apparatus for disinfecting or sterilising contact lenses; Accessories therefor
- A61L12/08—Methods or apparatus for disinfecting or sterilising contact lenses; Accessories therefor using chemical substances
- A61L12/10—Halogens or compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
- A61L12/00—Methods or apparatus for disinfecting or sterilising contact lenses; Accessories therefor
- A61L12/08—Methods or apparatus for disinfecting or sterilising contact lenses; Accessories therefor using chemical substances
- A61L12/12—Non-macromolecular oxygen-containing compounds, e.g. hydrogen peroxide or ozone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
- A61L12/00—Methods or apparatus for disinfecting or sterilising contact lenses; Accessories therefor
- A61L12/08—Methods or apparatus for disinfecting or sterilising contact lenses; Accessories therefor using chemical substances
- A61L12/14—Organic compounds not covered by groups A61L12/10 or A61L12/12
-
- G—PHYSICS
- G02—OPTICS
- G02C—SPECTACLES; SUNGLASSES OR GOGGLES INSOFAR AS THEY HAVE THE SAME FEATURES AS SPECTACLES; CONTACT LENSES
- G02C13/00—Assembling; Repairing; Cleaning
-
- G—PHYSICS
- G02—OPTICS
- G02C—SPECTACLES; SUNGLASSES OR GOGGLES INSOFAR AS THEY HAVE THE SAME FEATURES AS SPECTACLES; CONTACT LENSES
- G02C7/00—Optical parts
- G02C7/02—Lenses; Lens systems ; Methods of designing lenses
- G02C7/04—Contact lenses for the eyes
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Physics & Mathematics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Ophthalmology & Optometry (AREA)
- General Physics & Mathematics (AREA)
- Optics & Photonics (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
[2](A)成分がアルギニン及びその塩からなる群より選択される1種以上である、[1]に記載の眼科組成物。
[3](B)成分がムコ多糖類である、[1]又は[2]に記載の眼科組成物。
[4](C)殺菌剤又は防腐剤を更に含有する、[1]〜[3]のいずれか一項に記載の眼科組成物。
[5]眼科組成物がコンタクトレンズ用である、[1]〜[4]のいずれか一項に記載の眼科組成物。
本実施形態に係る眼科組成物は、(A)アルギニン、2−アミノ−2−メチル−1,3−プロパンジオール、トリス(ヒドロキシメチル)アミノメタン(トロメタモールともいう)、2−アミノエタノール(モノエタノールアミンともいう)及びこれらの塩からなる群より選択される1種以上(単に「(A)成分」とも表記する。)と、(B)多糖類(単に「(B)成分」とも表記する。)を含有する。
(A)成分は、アルギニン、2−アミノ−2−メチル−1,3−プロパンジオール、トリス(ヒドロキシメチル)アミノメタン、2−アミノエタノール及びこれらの塩からなる群より選択される1種以上である。(A)成分は、1種を単独で使用してもよく、又は2種以上を組み合わせて使用してもよい。
(B)成分は、多糖類である。(B)成分は、1種を単独で使用してもよく、又は2種以上を組み合わせて使用してもよい。
本実施形態に係る眼科組成物は、更に(C)殺菌剤又は防腐剤(単に「(C)成分」とも表記する。)を含有することが好ましい。眼科組成物が(C)成分を更に含有することで、本発明による効果がより顕著に奏される。
抗ヒスタミン剤:例えば、イプロヘプチン、塩酸ジフェンヒドラミン、マレイン酸クロルフェニラミン、フマル酸ケトチフェン、塩酸オロパタジン、塩酸レボカバスチン等。
抗アレルギー剤:例えば、クロモグリク酸ナトリウム、トラニラスト、ペミロラストカリウム等。
ステロイド剤:例えば、プロピオン酸フルチカゾン、フランカルボン酸フルチカゾン、フランカルボン酸モメタゾン、プロピオン酸ベクロメタゾン、フルニソリド等。
消炎剤:例えば、グリチルレチン酸、グリチルリチン酸二カリウム、プラノプロフェン、サリチル酸メチル、サリチル酸グリコール、アラントイン、トラネキサム酸、ε−アミノカプロン酸、ベルベリン、アズレンスルホン酸ナトリウム、塩化リゾチーム、硫酸亜鉛、乳酸亜鉛、甘草等。
充血除去剤:塩酸テトラヒドロゾリン、硝酸テトラヒドロゾリン、塩酸ナファゾリン、硝酸ナファゾリン、エピネフリン、塩酸エピネフリン、塩酸エフェドリン、塩酸フェニレフリン、dl−塩酸メチルエフェドリン等。
眼筋調節薬剤:例えば、アセチルコリンと類似した活性中心を有するコリンエステラーゼ阻害剤、具体的にはメチル硫酸ネオスチグミン、トロピカミド、ヘレニエン、硫酸アトロピン等。
ビタミン類:例えば、フラビンアデニンジヌクレオチドナトリウム、シアノコバラミン、塩酸ピリドキシン、パンテノール、パントテン酸カルシウム、パントテン酸ナトリウム、パルミチン酸レチノール、酢酸レチノール、酢酸トコフェロール等。
無機塩類:例えば、塩化カルシウム、塩化マグネシウム、塩化ナトリウム、塩化カリウム、塩化アンモニウム等の金属の塩化物、硫酸カルシウム、硫酸マグネシウム、硫酸ナトリウム、硫酸カリウム、硫酸アンモニウム等の金属の硫酸塩等。
収斂剤:例えば、亜鉛華、乳酸亜鉛、硫酸亜鉛等。
局所麻酔剤:例えば、リドカイン、プロカイン等。
その他:レバミピド等。
担体:例えば、水、含水エタノール等の水性溶媒。
基剤:例えば、オクチルドデカノール、酸化チタン、臭化カリウム、プラスチベース、流動パラフィン、軽質流動パラフィン、精製ラノリン、白色ワセリン等。
pH調節剤:塩酸、酢酸、水酸化ナトリウム、水酸化カリウム、水酸化カルシウム、水酸化マグネシウム、トリエタノールアミン、ジイソプロパノールアミン等。
糖類:例えば単糖類、二糖類、具体的にはグルコース、マルトース、トレハロース、スクロース、シクロデキストリン、キシリトール、ソルビトール、マンニトールなど。
安定化剤:ジブチルヒドロキシトルエン、ブチルヒドロキシアニソール、ナトリウムホルムアルデヒドスルホキシレート(ロンガリット)、亜硫酸水素ナトリウム、ピロ亜硫酸ナトリウム、モノステアリン酸アルミニウム、モノステアリン酸グリセリン、シクロデキストリン等。
陰イオン界面活性剤:ポリオキシエチレンアルキルエーテルリン酸塩、ポリオキシエチレンアルキルエーテル硫酸塩、アルキルベンゼンスルホン酸塩、アルキル硫酸塩、N−アシルタウリン塩等。
両性界面活性剤:ラウリルジメチルアミノ酢酸ベタイン等。
ビニル系高分子:ポリビニルピロリドン、ポリビニルアルコール、カルボキシビニルポリマー等。
本実施形態に係る眼科組成物は、低酸素状態によって引き起こされる角膜障害の治療又は予防に有用である。したがって、本発明の一実施形態として、(A)アルギニン、2−アミノ−2−メチル−1,3−プロパンジオール、トリス(ヒドロキシメチル)アミノメタン、2−アミノエタノール及びこれらの塩からなる群より選択される1種以上と、(B)多糖類と、を眼科組成物に含有させることを含む、該眼科組成物に低酸素状態によって引き起こされる角膜障害の治療又は予防作用を付与する方法が提供される。
本実施形態に係る眼科組成物は、角膜細胞を賦活化するという効果を奏する。したがって、本発明の一実施形態として、(A)アルギニン、2−アミノ−2−メチル−1,3−プロパンジオール、トリス(ヒドロキシメチル)アミノメタン、2−アミノエタノール及びこれらの塩からなる群より選択される1種以上と、(B)多糖類と、を眼科組成物に含有させることを含む、該眼科組成物に角膜細胞の賦活化作用を付与する方法が提供される。
本実施形態に係る眼科組成物は、アカントアメーバ角膜感染症の原因となるアカントアメーバを効果的に殺菌するという効果を奏する。
本実施形態に係る眼科組成物は、アカントアメーバ角膜感染症を予防するという効果を奏する。
本実施形態に係る眼科組成物は、角膜ステイニング等の角膜上皮障害を予防するという効果を奏する。
本実施形態に係る眼科組成物は、コンタクトレンズの装用感を改善するという効果を奏する。
表1に記載の処方に従い、各試験液(眼科組成物)を調製した。表1における各成分量の単位はw/v%である。
発現比=2−{(試験液処理による遺伝子のCt値)−(試験液処理による18S rRNAのCt値)}/2−{(比較例1−1処理による遺伝子のCt値)−(比較例1−1処理による18S rRNAのCt値)}
結果を表1に示す。
表2に記載の処方に従い、各試験液(眼科組成物)を調製した。表2における各成分量の単位はw/v%である。
比較例2−1に対する細胞生存率の上昇率(%)=
{(各試験液の細胞生存率−比較例2−1の細胞生存率)/比較例2−1の細胞生存率}×100
結果を表2に示す。
表3に記載の処方に従い、各試験液(コンタクトレンズ消毒・洗浄・保存液)を調製した。表3における各成分量の単位はw/v%である。調製直後の各試験液、及び60℃で3週間保管した後の各試験液について、アカントアメーバのトロホ型、及びシスト型に対する殺菌力を評価した。
アメーバ殺菌力改善率(%)={(各試験例のLog reduction−「比較例3−1」のLog reduction)/「比較例3−1」のLog reduction}×100
算出したアメーバ殺菌力改善率を表3に示す。
表4に記載の処方に従い、各試験液(コンタクトレンズ消毒・洗浄・保存液)を調製した。表4における各成分量の単位はw/v%である。各試験液(3mL)中に、コンタクトレンズ(アキュビューアドバンス(登録商標)、ジョンソンアンドジョンソン社製)を終夜浸漬させた後、健常人4名に装用させた。
<評価基準>
0:ステイニングが全くない
1:わずかなステイニングがある
2:中程度のステイニングがある
3:重篤なステイニングがある
表5に記載の処方に従い、各試験液(コンタクトレンズ消毒・洗浄・保存液)を調製した。表5における各成分量の単位はw/v%である。各試験液(3mL)中に、コンタクトレンズ(アキュビューアドバンス(登録商標)、ジョンソンアンドジョンソン社製)を終夜浸漬させた後、健常人4名に装用させた。
コンタクトレンズ装用直後、装用2時間後、及び装用8時間後に、表5に記載の各症状に関する感じ方をVAS(Visual analog scale:視覚的評価スケール)によって評価した。
VASによる評価は次のように行った。100mmの線が引いてある自覚症状調査シート上に、表5に記載の各症状が全く感じられない場合を0mm、強く感じる場合を100mmとして、被験者が感じた症状の程度のところにチェックしてもらった。この長さ(mm)をVAS値とした。すなわち、VAS値が高いほど、各症状の自覚症状スコアが高いということになる。
また、下記式を用いて比較例5−1に対するスコア変化率(%)を算出した。
スコア変化率(%)={(各試験例のVAS値−「比較例5−1」のVAS値)/「比較例5−1」のVAS値}×100
算出したスコア変化率を表5に示す。
表6に記載の処方に従い、各試験液(眼科組成物)を調製した。表6における各成分量の単位は、表中に記載があるもの以外は全て(w/v%)である。
測定対象の遺伝子をHMOX1のみとしたこと、及び比較例1−1に代えてコントロールを使用したこと以外は試験例1と同じ方法で、コントロールに対するHMOX1遺伝子の相対的発現比を算出した。コントロールは、ヒアルロン酸ナトリウムを含有しないこと以外は比較例6−1と同じ処方である。
各処方の発現比を算出した後、下記式を用いて対応する処方に対する発現比の上昇率を算出した。
発現比の上昇率(%)={(各試験例の発現比−対応する比較例の発現比)/対応する比較例の発現比}×100
ここで、実施例6−1〜6−3の対応する比較例は比較例6−1、実施例6−4及び6−5の対応する比較例は比較例6−2である。
算出した発現比の上昇率を表6に示す。
表7に記載の処方に従い、各試験液(眼科組成物)を調製した。表7における各成分量の単位はw/v%である。
発現比=2−{(試験液処理による遺伝子のCt値)−(試験液処理による18S rRNAのCt値)}/2−{(比較例7−1処理による遺伝子のCt値)−(比較例7−1処理による18S rRNAのCt値)}
結果を表7に示す。
表8及び9に記載の処方で眼科組成物を調製し、製剤例1〜18とした。表中の単位は、表中に記載があるもの以外は全て(w/v%)である。
Claims (5)
- (A)アルギニン、2−アミノ−2−メチル−1,3−プロパンジオール、トリス(ヒドロキシメチル)アミノメタン、2−アミノエタノール及びこれらの塩からなる群より選択される1種以上と、(B)多糖類と、を含有する、眼科組成物。
- (A)成分がアルギニン及びその塩からなる群より選択される1種以上である、請求項1に記載の眼科組成物。
- (B)成分がムコ多糖類である、請求項1又は2に記載の眼科組成物。
- (C)殺菌剤又は防腐剤を更に含有する、請求項1〜3のいずれか一項に記載の眼科組成物。
- 眼科組成物がコンタクトレンズ用である、請求項1〜4のいずれか一項に記載の眼科組成物。
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