JP2014512387A - 二つの異なる粘性増強剤を有する粘性増強システムを備えた眼科用組成物 - Google Patents
二つの異なる粘性増強剤を有する粘性増強システムを備えた眼科用組成物 Download PDFInfo
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Abstract
Description
本出願は、2011年4月22日に出願された米国特許仮出願第61/478,084号に基づく優先権を主張する。
本発明は、二つの異なる粘性増強剤を含む粘性増強システムを有する眼科用組成物に関連する。より具体的には、本発明は、眼への組成物を投薬(dispensing)する際に増強された粘性を提供する第一の粘性増強剤と、眼への組成物を投薬した後で粘性を増加させる(例えば、ゲル化するか、もしくは部分的にゲル化する)ことによって組成物の延長された粘性増強を提供する第二の粘性剤とを含む眼科用水性組成物に関連する。
Claims (19)
- 局所的眼科用複数回用量水性組成物であって、該組成物が:
粘性増強システム;および水を含み、該粘性増強システムが:
i)消散粘性増強剤であって、該消散粘性増強剤は、ヒトの眼の眼表面への該組成物の投与の際に、増強された粘性を呈するが、次いで、投与の後で、消散し、粘性を徐々に失う、消散粘性増強剤;および
ii)感熱相転移粘性増強剤であって、該感熱相転移粘性増強剤は、該ヒトの眼の該眼表面への該組成物の投与の際に、より低い粘性を呈するが、次いで、該眼の該眼表面への投与の後で、増強された粘性を呈する、感熱相転移粘性増強剤
を含む、局所的眼科用複数回用量水性組成物。 - 治療剤をさらに含む、請求項1に記載の眼科用組成物。
- 前記感熱ポリマーは、エチルヒドロキシエチルセルロース、メチルセルロース、ポロキサマー(例えば、ポリオキシエチレン(ポリ(エチレンオキシド))の二つの親水性鎖が側部についたポリオキシプロピレン(ポリ(プロピレンオキシド))の中央の疎水性鎖から構成される非イオン性トリブロックコポリマー)(例えば、BASFから市販されているPLURONICS(登録商標))、ポリ(ラクチド‐コ‐グリコリド)およびポリエチレングリコールから形成されるブロックコポリマー(例えば、ABAトリブロックコポリマー)、ポリ(N−イソプロピルアクリルアミド)および/もしくはポリ(N,N−ジメチルアクリルアミド)のようなアクリルアミド、エチレンオキシドおよびプロピレンオキシドをベースにした4官能性ブロックコポリマー(例えば、BASFから市販されているTETRONICS(登録商標))、またはこれらの任意の組み合わせから成る群から選択される、請求項1もしくは請求項2に記載の眼科用組成物。
- 前記消散ポリマーは、カルボキシビニルポリマー、HPMC、HEC、PVP、CMC、ポリビニルアルコール、もしくはこれらの任意の組み合わせを含む群から選択される、請求項1、請求項2もしくは請求項3に記載の眼科用組成物。
- 前記消散粘性増強剤は、前記組成物にさらなる粘性を提供し、該さらなる粘性は、少なくとも10cpであるが、100cp以下である、前記請求項のいずれかに記載の眼科用組成物。
- 前記組成物中の前記消散粘性増強剤の濃度が、少なくとも約0.10w/v%であるが、約2.5w/v%以下である、前記請求項のいずれかに記載の眼科用組成物。
- 前記組成物中の前記感熱粘性剤の濃度が、少なくとも約0.80w/v%であるが、10w/v%以下である、前記請求項のいずれかに記載の眼科用組成物。
- 前記感熱粘性剤は、粘性を実質的に増大させ、好ましくは、上昇させられた温度において、ゲル化するか、もしくは少なくとも部分的にゲル化し、該上昇させられた温度は、室温(すなわち、25℃)〜ヒト体温(すなわち、37℃)、より典型的に29℃〜35℃、さらにより典型的に32℃〜34℃にある、前記請求項のいずれかに記載の眼科用組成物。
- 局所的眼科用複数回用量水性組成物であって、該組成物が:
治療的有効量の治療剤;
粘性増強システム;および水を含み、該粘性増強システムが:
i)消散粘性増強剤であって、該消散粘性増強剤は、ヒトの眼の眼表面への該組成物の投与の際に、増強された粘性を呈するが、次いで、投与の後で、消散し、粘性を徐々に失い、該消散粘性増強剤はポリマー性である、消散粘性増強剤;および
ii)感熱相転移粘性増強剤であって、該感熱相転移粘性増強剤は、該ヒトの眼の該眼表面への該組成物の投与の際に、より低い粘性を呈するが、次いで、該眼の該眼表面への投与の後で、増強された粘性を呈し、該消散粘性増強剤はポリマー性である、感熱相転移粘性増強剤
を含む、局所的眼科用複数回用量水性組成物。 - 前記感熱ポリマーは、エチルヒドロキシエチルセルロース、メチルセルロース、ポロキサマー(例えば、ポリオキシエチレン(ポリ(エチレンオキシド))の二つの親水性鎖が側部についたポリオキシプロピレン(ポリ(プロピレンオキシド))の中央の疎水性鎖から構成される非イオン性トリブロックコポリマー)(例えば、BASFから市販されているPLURONICS(登録商標))、ポリ(ラクチド‐コ‐グリコリド)およびポリエチレングリコールから形成されるブロックコポリマー(例えば、ABAトリブロックコポリマー)、ポリ(N−イソプロピルアクリルアミド)および/もしくはポリ(N,N−ジメチルアクリルアミド)のようなアクリルアミド、エチレンオキシドおよびプロピレンオキシドをベースにした4官能性ブロックコポリマー(例えば、BASFから市販されているTETRONICS(登録商標))、またはこれらの任意の組み合わせから成る群から選択される、請求項9に記載の眼科用組成物。
- 前記消散ポリマーは、カルボキシビニルポリマー、HPMC、HEC、CMC、もしくはこれらの任意の組み合わせから成る群から選択される、請求項9もしくは請求項10に記載の眼科用組成物。
- 前記消散粘性増強剤は、前記組成物にさらなる粘性を提供し、該さらなる粘性は、少なくとも10cpであるが、100cp以下である、請求項9から請求項11のいずれかに記載の眼科用組成物。
- 前記組成物中の前記消散粘性増強剤の濃度が、少なくとも約0.10w/v%であるが、約2.5w/v%以下である、請求項9から請求項12のいずれかに記載の眼科用組成物。
- 前記組成物中の前記感熱粘性剤の濃度が、少なくとも約0.80w/v%であるが、10w/v%以下である、請求項9から請求項13のいずれかに記載の眼科用組成物。
- 前記感熱粘性剤は、粘性を実質的に増大させ、好ましくは、上昇させられた温度において、ゲル化するか、もしくは少なくとも部分的にゲル化し、該上昇させられた温度は、室温(すなわち、25℃)〜ヒト体温(すなわち、37℃)、より典型的に29℃〜35℃、さらにより典型的に32℃〜34℃にある、請求項9から請求項14のいずれかに記載の眼科用組成物。
- 前記治療剤は、抗緑内障剤、抗血管新生剤;抗感染剤;抗炎症剤;成長因子;免疫抑制剤;および抗アレルギー剤から成る群から選択される、前記請求項のいずれかに記載の眼科用組成物。
- 前記請求項のいずれかに記載の眼科用組成物を投与する方法であって、該方法は:
該眼科用組成物を哺乳類の眼へ局所的に投与する工程
を含む、前記請求項のいずれかに記載の眼科用組成物を投与する方法。 - 前記哺乳類は、ヒトである、請求項17に記載の方法。
- 前記投与する工程は、前記組成物の点眼物を点眼器から前記眼へ放つ工程を含む、請求項17もしくは請求項18に記載の方法。
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PCT/US2012/034187 WO2012145470A2 (en) | 2011-04-22 | 2012-04-19 | Ophthalmic composition with a viscosity enhancement system having two different viscosity enhancing agents |
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JPH05508154A (ja) * | 1990-06-15 | 1993-11-18 | アラーガン、インコーポレイテッド | 可逆ゲル化組成物および使用方法 |
JP2008195720A (ja) * | 1996-02-07 | 2008-08-28 | Rohto Pharmaceut Co Ltd | 粘度を調節した眼科用組成物 |
JP2004514731A (ja) * | 2000-12-06 | 2004-05-20 | ボシュ・アンド・ロム・インコーポレイテッド | 眼薬送達のための可逆的ゲル化システム |
WO2005042026A1 (ja) * | 2003-10-31 | 2005-05-12 | Wakamoto Pharmaceutical Co., Ltd. | 可逆性熱ゲル化水性組成物 |
CN101073556A (zh) * | 2007-06-25 | 2007-11-21 | 苏州瑞桥医药科技有限公司 | 一种散瞳眼用制剂及其制备方法 |
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RU2601115C2 (ru) | 2016-10-27 |
MX2013012308A (es) | 2014-01-31 |
WO2012145470A3 (en) | 2013-04-25 |
EP2699229A2 (en) | 2014-02-26 |
CA2833596A1 (en) | 2012-10-26 |
RU2013152026A (ru) | 2015-05-27 |
AU2012245454A1 (en) | 2013-10-17 |
WO2012145470A2 (en) | 2012-10-26 |
KR20140022901A (ko) | 2014-02-25 |
US20120270955A1 (en) | 2012-10-25 |
EP3045163A1 (en) | 2016-07-20 |
CN103491944A (zh) | 2014-01-01 |
BR112013026534A2 (pt) | 2016-12-27 |
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