JP6917103B1 - 近視抑制用点眼剤 - Google Patents
近視抑制用点眼剤 Download PDFInfo
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- JP6917103B1 JP6917103B1 JP2021082858A JP2021082858A JP6917103B1 JP 6917103 B1 JP6917103 B1 JP 6917103B1 JP 2021082858 A JP2021082858 A JP 2021082858A JP 2021082858 A JP2021082858 A JP 2021082858A JP 6917103 B1 JP6917103 B1 JP 6917103B1
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- myopia
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- 238000010586 diagram Methods 0.000 abstract 1
- 210000001508 eye Anatomy 0.000 description 21
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- 229960002467 bunazosin Drugs 0.000 description 6
- 208000010412 Glaucoma Diseases 0.000 description 5
- 241000699666 Mus <mouse, genus> Species 0.000 description 5
- 239000006196 drop Substances 0.000 description 5
- 239000002997 ophthalmic solution Substances 0.000 description 5
- 229940054534 ophthalmic solution Drugs 0.000 description 5
- 238000005259 measurement Methods 0.000 description 4
- 239000000654 additive Substances 0.000 description 3
- 230000004329 axial myopia Effects 0.000 description 3
- LOKCTEFSRHRXRJ-UHFFFAOYSA-I dipotassium trisodium dihydrogen phosphate hydrogen phosphate dichloride Chemical compound P(=O)(O)(O)[O-].[K+].P(=O)(O)([O-])[O-].[Na+].[Na+].[Cl-].[K+].[Cl-].[Na+] LOKCTEFSRHRXRJ-UHFFFAOYSA-I 0.000 description 3
- XXUPXHKCPIKWLR-JHUOEJJVSA-N isopropyl unoprostone Chemical compound CCCCCCCC(=O)CC[C@H]1[C@H](O)C[C@H](O)[C@@H]1C\C=C/CCCC(=O)OC(C)C XXUPXHKCPIKWLR-JHUOEJJVSA-N 0.000 description 3
- 239000002953 phosphate buffered saline Substances 0.000 description 3
- 230000004515 progressive myopia Effects 0.000 description 3
- 229950008081 unoprostone isopropyl Drugs 0.000 description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
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- 229940124308 alpha-adrenoreceptor antagonist Drugs 0.000 description 2
- 210000005252 bulbus oculi Anatomy 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 230000004305 hyperopia Effects 0.000 description 2
- 201000006318 hyperopia Diseases 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- LSIXBBPOJBJQHN-UHFFFAOYSA-N 2,3-Dimethylbicyclo[2.2.1]hept-2-ene Chemical compound C1CC2C(C)=C(C)C1C2 LSIXBBPOJBJQHN-UHFFFAOYSA-N 0.000 description 1
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- 102100035792 Kininogen-1 Human genes 0.000 description 1
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- QXZGBUJJYSLZLT-FDISYFBBSA-N bradykinin Chemical compound NC(=N)NCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1[C@H](C(=O)NCC(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CO)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)CCC1 QXZGBUJJYSLZLT-FDISYFBBSA-N 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- PANKHBYNKQNAHN-JUMCEFIXSA-N carotenoid dicarboxylic acid Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C(=O)O)C=CC=C(/C)C(=O)O PANKHBYNKQNAHN-JUMCEFIXSA-N 0.000 description 1
- 239000002738 chelating agent Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 239000002826 coolant Substances 0.000 description 1
- PANKHBYNKQNAHN-MQQNZMFNSA-N crocetin Chemical compound OC(=O)C(/C)=C/C=C/C(/C)=C/C=C/C=C(\C)/C=C/C=C(\C)C(O)=O PANKHBYNKQNAHN-MQQNZMFNSA-N 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000036040 emmetropia Effects 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 208000030533 eye disease Diseases 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 230000006698 induction Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000004410 intraocular pressure Effects 0.000 description 1
- 230000007721 medicinal effect Effects 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 210000002464 muscle smooth vascular Anatomy 0.000 description 1
- 238000012014 optical coherence tomography Methods 0.000 description 1
- -1 pH regulators Substances 0.000 description 1
- 230000003950 pathogenic mechanism Effects 0.000 description 1
- 239000002831 pharmacologic agent Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 230000004436 pseudomyopia Effects 0.000 description 1
- 230000004331 refractive myopia Effects 0.000 description 1
- 239000003590 rho kinase inhibitor Substances 0.000 description 1
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- 239000003381 stabilizer Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000024883 vasodilation Effects 0.000 description 1
- 230000004304 visual acuity Effects 0.000 description 1
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/10—Ophthalmic agents for accommodation disorders, e.g. myopia
-
- 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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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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- Health & Medical Sciences (AREA)
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- Chemical & Material Sciences (AREA)
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- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Ophthalmology & Optometry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Rehabilitation Tools (AREA)
Abstract
Description
本発明者らは、緑内障の点眼薬には近視進行抑制に効果的であるものがあることに着目し、既存の緑内障点眼薬から近視進行抑制効果を見つける試みを行った。本願では、緑内障点眼薬をマウス近視モデルに点眼し、眼軸長と屈折率を測定し、軸性近視の進行抑制効果があるか否かを評価した。
図1に示すように、生後3週齢のマウス(C57BL6/J,日本クレア株式会社)に、左眼0D(「D」はDiopterの略で、レンズの屈折力の単位である。)及び右眼−30Dのレンズを装着し、近視を誘導した。点眼は3週間継続し、PBS(Phosphate Buffered Saline)点眼を対照群とし、ブナゾシン点眼を試験群とした。ブナゾシンはデタントール点眼液の主成分であり、ブナゾシンの点眼はデタントール0.01%点眼液(参天製薬株式会社製、1mL中にブナゾシン塩酸塩が0.1mg含まれる)を用いて行った。点眼回数については、1日1回2滴の場合と1日2回(朝、夕各2滴)の場合とした。3週間後のマウス眼球の屈折率及び眼軸長を測定し、その変化量を計算した。なお、図中、*はp<0.05、**はp<0.01であることを示す(本願の図において同じ。)。
屈折値の測定は、マウス用赤外線フォトリフレクター(Infrared photorefractor for mice、Tubingen大学Schaeffel教授作製)を用いた。眼軸長の測定は、スペクトラルドメイン光コヒーレンストモグラフィー(Envisu R4310、Leica社製)を用いた。
図2は屈折率の結果である。屈折率は負数になるほど近視になる。対照群の屈折率の変化では、−30Dレンズの眼は近視となり、0Dの眼と有為差がみられた。一方、点眼群では、−30Dレンズの眼と0Dの眼との有為差はなく、近視抑制に効果があることがわかった。なお、1回点眼の方が2回点眼より近視抑制効果が見られた。
実験1と同様のマウスを使用し、近視を誘導した。点眼は3週間継続し、PBS点眼を対照群とし、ウノプロストン点眼を試験群とした。ウノプロストンはレスキュラ点眼液の主成分であり、ウノプロストンの点眼はレスキュラ点眼液0.12%(日東メディック株式会社、1mL中にイソプロピルウノプロストンが1.2mg含まれる)の点眼(両目、1日1回2滴)で行った。3週間後のマウス眼球の屈折率及び眼軸長を測定し、その変化量を計算した。屈折率測定と眼軸長測定は実験1と同じである。
図4は屈折率の結果である。対照群の屈折率の変化では、−30Dレンズの眼は近視となり、0Dの眼と有為差がみられた。一方、点眼群では、両目が近視となり、点眼での近視抑制効果は見られなかった。
Claims (1)
- ブナゾシンを含む点眼剤である、ことを特徴とする近視抑制用点眼剤。
Priority Applications (8)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2021082858A JP6917103B1 (ja) | 2021-05-17 | 2021-05-17 | 近視抑制用点眼剤 |
AU2022276728A AU2022276728A1 (en) | 2021-05-17 | 2022-05-17 | Eye drop for suppressing myopia |
KR1020237038535A KR20240008848A (ko) | 2021-05-17 | 2022-05-17 | 근시억제용 점안제 |
CA3216748A CA3216748A1 (en) | 2021-05-17 | 2022-05-17 | Ophthalmic preparation for myopia supression |
TW111118406A TW202313058A (zh) | 2021-05-17 | 2022-05-17 | 抑制近視用滴眼劑 |
CN202280035569.4A CN117320726A (zh) | 2021-05-17 | 2022-05-17 | 抑制近视用滴眼剂 |
PCT/JP2022/020514 WO2022244765A1 (ja) | 2021-05-17 | 2022-05-17 | 近視抑制用点眼剤 |
EP22804676.9A EP4342472A1 (en) | 2021-05-17 | 2022-05-17 | Eye drop for suppressing myopia |
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JP2021082858A JP6917103B1 (ja) | 2021-05-17 | 2021-05-17 | 近視抑制用点眼剤 |
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JP6917103B1 true JP6917103B1 (ja) | 2021-08-11 |
JP2022176427A JP2022176427A (ja) | 2022-11-30 |
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JP2021082858A Active JP6917103B1 (ja) | 2021-05-17 | 2021-05-17 | 近視抑制用点眼剤 |
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EP (1) | EP4342472A1 (ja) |
JP (1) | JP6917103B1 (ja) |
KR (1) | KR20240008848A (ja) |
CN (1) | CN117320726A (ja) |
AU (1) | AU2022276728A1 (ja) |
CA (1) | CA3216748A1 (ja) |
TW (1) | TW202313058A (ja) |
WO (1) | WO2022244765A1 (ja) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2024048750A1 (ja) * | 2022-08-31 | 2024-03-07 | 株式会社坪田ラボ | α1ブロッカーを含む近視進行抑制用点眼剤 |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2016132616A (ja) * | 2015-01-15 | 2016-07-25 | 大内新興化学工業株式会社 | 眼疾患治療用ナノ粒子製剤 |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2563336B2 (ja) * | 1987-06-01 | 1996-12-11 | エーザイ株式会社 | 角膜透過促進点眼剤 |
JP4300347B2 (ja) * | 2002-01-29 | 2009-07-22 | 参天製薬株式会社 | ブナゾシンとプロスタグランジン類からなる緑内障治療剤 |
US8629161B2 (en) * | 2005-06-21 | 2014-01-14 | Kowa Co., Ltd. | Preventive or remedy for glaucoma |
EP2319539A4 (en) | 2008-07-24 | 2012-03-28 | Univ Osaka | PROPHYLACTIC OR THERAPEUTIC AGENT FOR AXIAL MYOPIA |
JP2011144111A (ja) | 2010-01-12 | 2011-07-28 | Osaka Univ | 軸性近視の予防または治療剤 |
TWI787268B (zh) | 2017-05-15 | 2022-12-21 | 日商坪田實驗室股份有限公司 | 預防近視用組成物及機能性食品 |
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2021
- 2021-05-17 JP JP2021082858A patent/JP6917103B1/ja active Active
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2022
- 2022-05-17 CA CA3216748A patent/CA3216748A1/en active Pending
- 2022-05-17 WO PCT/JP2022/020514 patent/WO2022244765A1/ja active Application Filing
- 2022-05-17 AU AU2022276728A patent/AU2022276728A1/en active Pending
- 2022-05-17 CN CN202280035569.4A patent/CN117320726A/zh active Pending
- 2022-05-17 EP EP22804676.9A patent/EP4342472A1/en active Pending
- 2022-05-17 KR KR1020237038535A patent/KR20240008848A/ko unknown
- 2022-05-17 TW TW111118406A patent/TW202313058A/zh unknown
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2016132616A (ja) * | 2015-01-15 | 2016-07-25 | 大内新興化学工業株式会社 | 眼疾患治療用ナノ粒子製剤 |
Non-Patent Citations (1)
Title |
---|
あたらしい眼科, vol. 37, no. 5, JPN6021026222, 2020, pages 559 - 574, ISSN: 0004546407 * |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2024048750A1 (ja) * | 2022-08-31 | 2024-03-07 | 株式会社坪田ラボ | α1ブロッカーを含む近視進行抑制用点眼剤 |
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Publication number | Publication date |
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TW202313058A (zh) | 2023-04-01 |
WO2022244765A1 (ja) | 2022-11-24 |
JP2022176427A (ja) | 2022-11-30 |
AU2022276728A1 (en) | 2023-11-09 |
CN117320726A (zh) | 2023-12-29 |
KR20240008848A (ko) | 2024-01-19 |
CA3216748A1 (en) | 2022-11-24 |
EP4342472A1 (en) | 2024-03-27 |
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