JP6209163B2 - ドライアイ治療用組成物 - Google Patents
ドライアイ治療用組成物 Download PDFInfo
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- JP6209163B2 JP6209163B2 JP2014534753A JP2014534753A JP6209163B2 JP 6209163 B2 JP6209163 B2 JP 6209163B2 JP 2014534753 A JP2014534753 A JP 2014534753A JP 2014534753 A JP2014534753 A JP 2014534753A JP 6209163 B2 JP6209163 B2 JP 6209163B2
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Description
本願は、2011年10月6日出願の米国仮特許出願第61/544,151号の利益を主張するものであり、この開示全体は、本明細書中にこの具体的な参照により援用される。
行われた臨床試験は、ドライアイ疾患の兆候および症状を示す対象における、アラガンの既存のOPTIVE(商標)目薬中の、2つの候補物である製剤Aおよび製剤Bの安全性、効力、および許容性を評価することを目的とした。
Ocular Surface Disease Index(著作権)(OSDI)アンケートを、インテント・トゥ・トリート(intent−to−treat)(ITT)集団において30日目に行うことにより、主要な効力の測定を行った。このOSDIアンケートは、5段階評価(0=全くなし、1=時々、2=半分ほど、3=たいてい、4=常時、であり、質問の一部は、「N/A」(該当せず)の回答となる可能性がある)での12の質問からなる(Schiffmanら、2000)。対象は、5段階評価を使用して、ドライアイの多様な症状の頻度、関連する視覚機能、および環境的な引き金を評価するために質問された。対象は、試験のため来院する前の1週間の症状の頻度に関する評価を基準とするように依頼された。このことは、眼ごとに評価せず、総合的に評価した。
この試験の結果から、製剤Bが、軽度〜重篤なドライアイを伴う対象の乾燥の症状の重症度を低下させるうえでOPTIVE UD製剤よりも劣ってはいないことが示される。
製剤Bは、試験の間良好な耐性を有するようであった。試験にわたり、治療に関連する深刻な有害事象は存在しなかった。この安全性プロファイルは、OPTIVE UD、OPTIVE MD、および製剤Aと一致した。このことは、臨床的な使用において、製剤Bの安全性を支持するものであり、製剤Aの安全性を確認するものである。
二次的な効力の測定を、TBUT(涙破壊時間)、角膜染色、結膜染色、およびシルマー試験により行った。
現在の試験の目的は、ドライアイ疾患の兆候および症状を伴う対象における製剤Bの安全性、効力、および許容性を評価することである。この試験は、既存のOPTIVE UD製剤と製剤Bとの比較、および製剤Aと製剤Bとを比較するために実施された。主要な効力の終点は、この試験と一致した。
製剤Bの目薬を、ドライアイを訴える白色人種の52歳の男性患者の眼に投与した。2日間各眼に1日2回この目薬を投与した後、患者のドライアイの症状が軽減した。
製剤Aの目薬を、ドライアイ患者の各眼に1日1〜3回投与した。2日後、患者はドライアイ症候群が軽減したと感じた。
Claims (18)
- モノオレイン酸ポリオキシエチレン(20)ソルビタン、カルボキシメチルセルロースナトリウム、グリセリン、ホウ酸、アクリレート/C10−30アルキルアクリレート架橋ポリマー、ひまし油、エリスリトール、レボカルニチン、水酸化ナトリウムおよび水を含む点眼用組成物(ただし、前記点眼用組成物は、ひまし油以外の油を含まず、またシクロスポリンAを含まない)。
- 前記モノオレイン酸ポリオキシエチレン(20)ソルビタンが、約0.1%w/w〜約2%w/wの濃度で存在する、請求項1に記載の組成物。
- 前記カルボキシメチルセルロースナトリウムが、約0.1%w/w〜約2%w/wの濃度で存在する、請求項1に記載の組成物。
- 前記グリセリンが、約0.2%w/w〜約5%w/wの濃度で存在する、請求項1に記載の組成物。
- 前記ホウ酸が、約0.02%w/w〜約2%w/wの濃度で存在する、請求項1に記載の組成物。
- 前記アクリレート/C10−30アルキルアクリレート架橋ポリマーが、約0.02%w/w〜約0.5%w/wの濃度で存在する、請求項1に記載の組成物。
- 前記ひまし油が、約0.05%w/w〜約0.5%w/wの濃度で存在する、請求項1に記載の組成物。
- 前記エリスリトールが、約0.05%w/wまたは約3%w/wの濃度で存在する、請求項1に記載の組成物。
- 前記レボカルニチンが、約0.05%w/wまたは約3%w/wの濃度で存在する、請求項1に記載の組成物。
- pHが約7.3である、請求項1に記載の組成物。
- 約0.5%w/wのモノオレイン酸ポリオキシエチレン(20)ソルビタン、約0.5%w/wのカルボキシメチルセルロースナトリウム、約1.0%w/wのグリセリン、約0.6%w/wのホウ酸、約0.1%w/wのアクリレート/C10−30アルキルアクリレート架橋ポリマー、約0.25%w/wのひまし油、約0.25%w/wのエリスリトール、約0.25%w/wのレボカルニチン、水酸化ナトリウム、pHが約7.3および水を含む、請求項1に記載の組成物。
- ドライアイ症候群を治療、診断、治癒、緩和、または予防するための、請求項1に記載の組成物。
- 前記点眼用組成物が、約0.5%w/wのモノオレイン酸ポリオキシエチレン(20)ソルビタン、約0.5%w/wのカルボキシメチルセルロースナトリウム、約1.0%w/wのグリセリン、約0.6%w/wのホウ酸、約0.1%w/wのアクリレート/C10−30アルキルアクリレート架橋ポリマー、約0.25%w/wのひまし油、約0.25%w/wのエリスリトール、約0.25%w/wのレボカルニチン、水酸化ナトリウム、pHが約7.3および水を含む、請求項12に記載の組成物。
- 安定化オキシクロロ錯体をさらに含む、請求項1に記載の組成物。
- 前記安定化オキシクロロ錯体が、約0.002%w/w〜約0.05%w/wの濃度で存在する、請求項14に記載の組成物。
- 約0.01%w/wの安定化オキシクロロ錯体をさらに含む、請求項11に記載の組成物。
- ドライアイ症候群を治療、診断、治癒、緩和、または予防するための、請求項14に記載の組組成物。
- 前記点眼用組成物が、約0.5%w/wのモノオレイン酸ポリオキシエチレン(20)ソルビタン、約0.5%w/wのカルボキシメチルセルロースナトリウム、約1.0%w/wのグリセリン、約0.01%w/wの安定化オキシクロロ錯体、約0.6%w/wのホウ酸、約0.1%w/wのアクリレート/C10−30アルキルアクリレート架橋ポリマー、約0.25%w/wのひまし油、約0.25%w/wのエリスリトール、約0.25%w/wのレボカルニチン、pHを約7.3にするための水酸化ナトリウム、および水を含む、請求項17に記載の組成物。
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US201161544151P | 2011-10-06 | 2011-10-06 | |
US61/544,151 | 2011-10-06 | ||
PCT/US2012/058893 WO2013052760A1 (en) | 2011-10-06 | 2012-10-05 | Compositions for the treatment of dry eye |
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JP2014528452A JP2014528452A (ja) | 2014-10-27 |
JP6209163B2 true JP6209163B2 (ja) | 2017-10-04 |
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EP (1) | EP2765987A1 (ja) |
JP (1) | JP6209163B2 (ja) |
CN (2) | CN108175778A (ja) |
AU (1) | AU2012318556B2 (ja) |
BR (1) | BR112014008314B1 (ja) |
CA (1) | CA2851398C (ja) |
CL (1) | CL2014000863A1 (ja) |
HK (1) | HK1201042A1 (ja) |
IL (1) | IL231970A (ja) |
MX (1) | MX2014004203A (ja) |
MY (1) | MY169328A (ja) |
RU (1) | RU2651046C2 (ja) |
SG (1) | SG11201401323PA (ja) |
TW (1) | TWI642432B (ja) |
WO (1) | WO2013052760A1 (ja) |
ZA (1) | ZA201404121B (ja) |
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US8957048B2 (en) * | 2011-10-06 | 2015-02-17 | Allergan, Inc. | Compositions for the treatment of dry eye |
KR102017922B1 (ko) * | 2011-12-07 | 2019-09-03 | 알러간, 인코포레이티드 | 염-민감성 유액 시스템을 사용한 사람 눈물막으로의 효율적인 지질 전달 방법 |
US9907826B2 (en) | 2011-12-07 | 2018-03-06 | Allergan, Inc. | Efficient lipid delivery to human tear film using a salt-sensitive emulsion system |
US9278132B2 (en) | 2012-02-13 | 2016-03-08 | Bausch & Lomb Incorporated | Ophthalmic pharmaceutical compositions and methods of making and using same |
US20140377210A1 (en) * | 2013-06-21 | 2014-12-25 | Gnt, Llc | Artificial tear compositions |
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