CN106456584A - 用于矫正老视的药理学眼科用组合物和其施用 - Google Patents

用于矫正老视的药理学眼科用组合物和其施用 Download PDF

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CN106456584A
CN106456584A CN201480075407.9A CN201480075407A CN106456584A CN 106456584 A CN106456584 A CN 106456584A CN 201480075407 A CN201480075407 A CN 201480075407A CN 106456584 A CN106456584 A CN 106456584A
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presbyopia
ophthalmic composition
pharmacological
correction
administration
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C·G·费宝木
S·帕特尔
F·沙拉蒙
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Aklaghi J Pharmaceuticals
Orasis Pharmaceuticals Ltd
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    • 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
    • A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
    • A61K31/728—Hyaluronic acid
    • 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
    • A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • 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
    • A61K9/0051—Ocular inserts, ocular implants
    • 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
    • A61K9/08—Solutions
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Abstract

本发明的目的是提供用于矫正老视的药理学眼科用组合物，其作为滴液被引入眼睛和周围的软组织(多滴滴液)的表面上或作为植入物通过手术引入结膜下空间用于持续缓释应用。

Description

用于矫正老视的药理学眼科用组合物和其施用
本发明的目的是提供用于矫正老视的药理学眼科用组合物，其作为滴液被引入眼睛和周围的软组织(多滴滴液)的表面上或作为植入物通过手术引入眼睛内用于持续缓释应用。采用滴液或植入物实现瞳孔大小的下降，导致视野深度增加，眼睛高阶光学像差的大小下降和改善的近的和远的裸眼视力。本发明属于国际专利分类的A 61 K45/06、A61 K31/4178和A6 P 27/10类。
当年轻的正视者注视近的物体时，在眼睛中发生两个主要的变化：调视(accommodation)和瞳孔缩小。调视是晶状体折光力的变化。晶状体变得更圆，由此其折光力增加。瞳孔大小中的瞳孔缩小减少，由此焦深增加并且高阶像差减小。
在副交感神经系统的影响下发生瞳孔缩小和调视这两者。结合至毒蕈碱受体的拟副交感神经药乙酰胆碱诱使瞳孔的睫状肌和括约肌的肌肉收缩。
老视是因为调节幅度的逐渐丧失在近距离的物体上聚焦的递减的年龄相关能力。在五十岁之后不久，晶状体丧失经历调节光学变化的全部能力。主观地测量，调节幅度具有渐进的丧失直到大约五十岁，其中保持在大约1折光度。这是由于像差和瞳孔缩小的焦深，定义为假性调视。
已经使用眼镜、接触镜或眼内植入物、和角膜切除或嵌入矫正老视。已经提出的矫正老视的手术方法不会完全恢复已经通过自然老化或其他方式下降的眼睛的天然调节功能。提出药物治疗以恢复导致老视的眼镜的调节功能的天然丧失。根据EP 1 938 839，拟副交感神经药和非甾体抗炎药的结合，其中使用的拟副交感神经药是浓度从1％至2％的毛果芸香碱(或其盐)。这些浓度的拟副交感神经药可导致非期望的副作用。
还已知的是，在眼底附近通过玻璃体内显微注射方式持续释放递送眼科用组合物是有效的和有优势的。在WO 2011/079123 A1文件(在所附的专利文件WO20/079123 A1中阐述了步骤描述)中描述了这种治疗。显微注射的优势是经与引入至眼表面上的流体相关的天然排液通道使保留在眼中的缓慢释放的成分不损失。通过避免常常重复滴入滴液，显微注射节省了使用者(患者)时间和劳动。本发明涉及用于矫正老视而无有害影响的眼科用组合物，如在其他文件中所陈述。
根据本发明的眼科用组合物包含以下：从0.1％至0.9％的透明质酸钠、从0.006％至0.012％的双氯芬酸钠和从0.2％至0.4％的盐酸毛果芸香碱。本发明的组合物延伸至包含可被添加、改变、替代或去除的其他成分以改善舒适度和总体疗效。
本发明的实施方式(modus operandi)如下。
由于滴液的成分对天然虹膜的肌肉纤维的作用的结果，瞳孔的大小下降。诱使瞳孔缩小，焦深增加和高阶像差的大小减小，改善了未矫正的近视和远视视力。
该组合物的优势是i)低剂量ii)抗炎作用iii)舒适。文献检索未显示提及浓度的任何成分对眼睛的任何已知的长期有害效果。这受到申请人基于超过100个病例(62受试者)的观察的支持。
提出将滴液用于短距离光学处方的通常健康良好的人，之前做过角膜的激光眼部手术的那些人(LASIK或PRK)，之前做过常规白内障手术和植入标准单焦点眼内植入晶状体的那些人。将一滴或两滴滴液引入至眼表面上，通常可在几分钟之后报告远视和近视的改善并且该效果可持续高至8小时。
在使用局部滴液刺激试验之后，在已经确定患者将受益于植入物之后通过眼科手术将该缓释植入物手术引入结膜下空间内。其成分被动的到达虹膜，与改变瞳孔大小的虹膜的肌肉纤维相互作用。该作用导致视野深度增加，以及本文所提及的远视和近视的改善。

Claims (3)

1.用于矫正老视的药理学眼科用组合物，其包括从0.1％至0.9％的透明质酸钠，从0.006％至0.012％的双氯芬酸钠和从0.2％至0.4％的盐酸毛果芸香碱。
2.根据权利要求1所述的药理学眼科用组合物的用途，其中在8小时的期间内其以一至两滴滴液的形式被施用至眼表面上。
3.根据权利要求1所述的药理学眼科用组合物的用途，其中其以持续缓释植入物的形式施用，通过手术引入结膜下空间。
CN201480075407.9A 2014-02-11 2014-02-11 用于矫正老视的药理学眼科用组合物和其施用 Withdrawn CN106456584A (zh)

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PCT/SI2014/000008 WO2015122853A1 (en) 2014-02-11 2014-02-11 Pharmacological ophthalmic composition for use in the correction of presbyopia and its administration

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JP (1) JP2017505805A (zh)
CN (1) CN106456584A (zh)
AU (1) AU2014382677A1 (zh)
CA (1) CA2939427A1 (zh)
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AU2017311636B2 (en) 2016-08-19 2023-08-10 Orasis Pharmaceuticals Ltd. Ophthalmic pharmaceutical compositions and uses relating thereto
JP2018035075A (ja) * 2016-08-29 2018-03-08 株式会社Ｌｔｔバイオファーマ ドライアイ治療剤
KR20230079489A (ko) 2018-04-24 2023-06-07 알러간, 인코포레이티드 안구 증상의 치료를 위한 필로카르핀 염산염의 용도
MX2020012116A (es) * 2020-11-12 2022-08-09 Cesar Alejandro Sanchez Galeana Composicion oftalmologica sinergica en dosis de baja concentracion eficaz en la prevencion, control y erradicacion de la presbicia.
WO2023069037A1 (en) * 2021-10-19 2023-04-27 Vsy Biyoteknoloji Ve Ilac Sanayi Anonim Sirketi Ophthalmic formulations for treatment of presbyopia, dry eye disease and computer vision syndrome

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RU2016136333A3 (zh) 2018-03-15
WO2015122853A1 (en) 2015-08-20
JP2017505805A (ja) 2017-02-23
CA2939427A1 (en) 2015-08-20
AU2014382677A1 (en) 2016-09-01
EP3104851A1 (en) 2016-12-21
HK1232159A1 (zh) 2018-01-05
US20170007637A1 (en) 2017-01-12

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Application publication date: 20170222