JP2018520110A - リポ酸および粘膜模倣ポリマーを含んでなる眼科用組成物 - Google Patents
リポ酸および粘膜模倣ポリマーを含んでなる眼科用組成物 Download PDFInfo
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- JP2018520110A JP2018520110A JP2017560808A JP2017560808A JP2018520110A JP 2018520110 A JP2018520110 A JP 2018520110A JP 2017560808 A JP2017560808 A JP 2017560808A JP 2017560808 A JP2017560808 A JP 2017560808A JP 2018520110 A JP2018520110 A JP 2018520110A
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- lipoic acid
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- mucosal
- polymer
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- 239000000203 mixture Substances 0.000 title claims abstract description 91
- 235000019136 lipoic acid Nutrition 0.000 title claims abstract description 38
- 229960002663 thioctic acid Drugs 0.000 title claims abstract description 38
- 229920000642 polymer Polymers 0.000 title claims abstract description 32
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- 238000000034 method Methods 0.000 claims abstract description 11
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 11
- 150000003839 salts Chemical class 0.000 claims description 11
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical group CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims description 10
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- AGBQKNBQESQNJD-UHFFFAOYSA-N lipoic acid Chemical compound OC(=O)CCCCC1CCSS1 AGBQKNBQESQNJD-UHFFFAOYSA-N 0.000 description 32
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
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Abstract
Description
− エマルション安定化剤、特にポリマー安定剤として、例えば、ポリビニルアルコールポリマー、ポリソルベート、およびセルロース系、特にメチルセルロース、エチルセルロース、ヒドロキシプロピルセルロース、カルボキシメチルセルロース、およびそれらの混合物があり、これら安定剤は、組成物の総重量に対し0.05〜0.2%の範囲の量で使用することができる;
− 界面活性剤は、ポリソルベート、ポリエチレングリコールおよびその誘導体、ポリオキシエチレン-40-ステアレート、ソルビタンエステル、ポリオキシエチレン-ポリオキシプロピレン共重合体、ポリビニルアルコール、ポリビニルピロリドンポリマー、およびそれらの混合物が挙げられ、これら界面活性剤の組成物の総重量に対し0.01〜0.5重量%の範囲の量で使用することができる;
− 保存剤は、特に、第四級アンモニウム化合物、特に塩化ベンザルコニウム、アルキルジメチルベンジルアンモニウム、セトリミド、セチルピリジニウムクロライド、ベンゾドデシニウムブロマイド、ベンゾチオニウムクロライド、セタルコニウムクロライド、硝酸/酢酸/ホウ酸フェニル水銀のような水銀保存剤、チメロサール、クロロブタノール、ベンジルアルコール、フェニルエタノール、フェニルエチルアルコールのようなアルコール防腐剤、ソルビン酸のようなカルボン酸、フェノール類、特にメチル/プロピルパラベン、アミジン、例えばグルコン酸クロルヘキシジン、EDTA、少なくとも一つの防腐剤と併用して防腐剤の効力を増強するキレート剤、およびこれらの混合物が挙げられ、これら防腐剤は、組成物の総重量に対し0.001〜0.1%の範囲の量で使用することができる;
−脂質として、ヒマシ油、大豆油、ゴマ油、パラフィン、ラノリン、ワセリン、しかし、グリセリンなどのアシルグリセロールまたはグリセリドのクラスの脂質としてトリグリセリドおよびそれらの誘導体、またはホスホアシルグリセロールとも呼ばれるホスホアシルグリセリド、ホスホ燐スフィンゴ脂質、ホスホノス燐スフィンゴ脂質、ホスホグリコ脂質、ホスホ糖脂質およびホスファチジルコリン、およびそれらの混合物などのリン脂質タイプのモノグリセリド、トリグリセリドのようは油分が挙げられ、これらの脂質は、組成物の総重量に対してい0.1から1.5重量%の範囲の量で使用することができる;
− 緩衝剤は、眼に使用するための許容されるpHを安定化させるためであり、リン酸塩、酢酸塩、クエン酸塩、およびそれらの混合物が挙げられ、これら緩衝剤は、組成物の総重量に対して0.1から1.5重量%の範囲で使用することができる。
最初の実験室的試験のバッチは、リポ酸を含有するエマルジョンが改善された安定性を示すことを実証した。エマルジョン安定性は、特に粒子径を指標とする。小さな粒子サイズを維持するエマルジョンの能力は、安定性のマーカーとなる。粒径測定は、リポ酸を含むか否か以外は同一である剤型について行った。
− BR PI0 800 818
− CN 103 860 625
− DE10 229 995
− JP 2013 241398
− US 5 817 630
− US 6 162 393
− US 2004/265345
− US 2005/192229
− US 2006/188492
− WO 01/93824
− WO 02/098345
− WO 2011/131765
− WO 2012/013736
− WO 2015/150459
− Masami Kojima & col., Japanese Journal of Ophthalmology, January 2007, Volume 51, Issue 1, pp 10-13
Claims (15)
- 粘膜模倣ポリマーとリポ酸とを含む水中油型エマルジョンの形態である、眼科用組成物。
- 前記粘膜模倣ポリマーが、ヒアルロン酸またはその塩である、請求項1に記載の眼科用組成物。
- 前記粘膜模倣ポリマーの含有量が、組成物の全重量に対して0.01から5重量%の範囲である、請求項1または2に記載の組成物。
- 前記リポ酸が、リポ酸ナトリウムである、請求項1〜3のいずれか一項に記載の組成物。
- 前記リポ酸の含有量が、組成物の全重量に対して0.01〜0.02重量%である、請求項1〜4のいずれか一項に記載の組成物。
- 前記リポ酸/前記粘膜模倣ポリマーの重量比が、0.05〜0.15の範囲である、請求項1〜5のいずれか一項に記載の組成物。
- 5000 NTUまたはそれ以下の透明度を有する、請求項1〜6のいずれかに記載の組成物。
- 1000 NTUまたはそれ以下の透明度を有する、請求項7に記載の組成物。
- 約200〜700 NTUの透明度を有する、請求項8に記載の組成物。
- 点眼剤の形態である、請求項1〜9のいずれか一項に記載の組成物。
- 組成物の全重量に対して少なくとも70%の水を含んでなる、請求項10に記載の組成物。
- 組成物の全重量に対して少なくとも80%の水、より好ましくは少なくとも95%の水を含んでなる、請求項11に記載の組成物。
- 請求項1〜12のいずれか一項に記載の粘膜模倣ポリマーを含む水中油型エマルジョンを調製するための方法であって、当該組成物の乳化工程の前またはその間に、リポ酸を添加する工程を含んでなる、方法。
- 粘膜模倣ポリマーを含む水中油型エマルジョンを安定化するための、リポ酸の使用。
- 粘膜模倣ポリマーが、ヒアルロン酸またはその塩である、請求項14に記載の使用。
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FR1554590A FR3036284B1 (fr) | 2015-05-21 | 2015-05-21 | Acide lipoique en tant qu'agent osmoprotecteur |
FR1652042A FR3048613B3 (fr) | 2016-03-11 | 2016-03-11 | Composition ophtalmique comprenant de l'acide lipoique et un polymere muco-mimetique |
FR1652042 | 2016-03-11 | ||
PCT/EP2016/061362 WO2016185000A1 (fr) | 2015-05-21 | 2016-05-20 | Composition ophtalmique comprenant de l'acide lipoique et un polymere muco-mimetique |
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ES2883956T3 (es) | 2021-12-09 |
BR112017024804B1 (pt) | 2024-02-27 |
CA2985014A1 (fr) | 2016-11-24 |
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CN107820422B (zh) | 2022-02-08 |
RU2017142726A3 (ja) | 2019-09-27 |
US10940206B2 (en) | 2021-03-09 |
EP3297626A1 (fr) | 2018-03-28 |
WO2016185000A1 (fr) | 2016-11-24 |
RU2724955C2 (ru) | 2020-06-29 |
RU2017142726A (ru) | 2019-06-21 |
CN107820422A (zh) | 2018-03-20 |
US20180147283A1 (en) | 2018-05-31 |
EP3297626B1 (fr) | 2021-06-16 |
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CA2985014C (fr) | 2024-01-16 |
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