JP2015531374A - 局所ケトプロフェン組成物 - Google Patents
局所ケトプロフェン組成物 Download PDFInfo
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- JP2015531374A JP2015531374A JP2015534599A JP2015534599A JP2015531374A JP 2015531374 A JP2015531374 A JP 2015531374A JP 2015534599 A JP2015534599 A JP 2015534599A JP 2015534599 A JP2015534599 A JP 2015534599A JP 2015531374 A JP2015531374 A JP 2015531374A
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- percent
- ketoprofen
- composition
- polyacrylic acid
- topical composition
- Prior art date
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Abstract
Description
本出願は、全体が参照により本明細書に組み込まれる、2012年9月27日に出願された米国特許仮出願第61/706,163号の優先権を主張する。
1.実験材料
ケトプロフェンはBoehinger−Ingelheimから入手した。
クロマトグラフィ条件:
無勾配逆相HPLCシステムを用いてケトプロフェン製剤の安定性および光安定性を測定した。HPLC装置はAgilent 1100であった。WatersからのNovaPak(登録商標)4.6×300mm C18カラムを使用した。移動相は、塩酸でpH2.3に調整したギ酸緩衝液(0.025M)とアセトニトリルの混合物(50:50)から成った。流量は1.0ml/分であった。検出は220nmと254nmで実施した。注入量は25μlに設定した。これらの条件下で、ケトプロフェンおよびオキシベンゾンの保持時間はそれぞれ約5分および13分であった。ケトプロフェンおよびオキシベンゾンの検量線の濃度範囲は、それぞれ7−210μg/mlおよび120−480μg/mlであった。試料の実行時間は20分であった。
安定性試験のために、それぞれ5%および10%のケトプロフェンを含有する組成物についての試料約75または50mgを25mlメスフラスコに直接量り取った。移動相約20mlを各フラスコに添加し、この後3分間ボルテックスして、移動相を容積まで満たし、十分に振とうした。
デルマトームで採皮した死体皮膚(Science Care,Aurora,CO)を、さらなる処理を行わずに使用した。ブタ皮膚(Lampire Biological Laboratories,Pipersville,PA)をデルマトームで標準的な厚さに採皮した。改変フランツセルを用いて37℃で約1.3cm2の露出皮膚膜表面積で透過試験を実施し、2、4および22時間目に試料を採取して、HPLCによって検定した。各々のフランツセルに約100mgのクリーム試料の1つの小さなアリコートを添加し、ガラス棒を用いて皮膚膜表面に軽く広げて、水分の喪失を防ぐためにカバーディスクで覆った。レセプタ相はpH7.4のリン酸緩衝液を含んだ。
調製物を超高強度UV光源(300ルクスまで)に5分間または10分間暴露した。この暴露レベルでヒト皮膚は容易に熱傷する。暴露したクリームのアリコートを、前述したHPLC手順を用いてケトプロフェンおよびオキシベンゾンに関して検定した。
試料を0℃で24時間保存し、次いで25℃で24時間解凍した。試料を各サイクル後に相分離に関して観測した。各々の試料について、5回のサイクルを評価した。
1.許容される安定化ポリマー増粘剤を見出すためおよび凍結/融解の失敗を最小限に抑えるこれらのポリマーの最適レベルを見出すために一連の試験を実施した。これらの試験を以下に示す。
1.種々の比率のCarbopol(登録商標)980とCarbopol(登録商標)Ultrez 10を含有する組成物に関して凍結/融解安定性試験を実施した。
1.3か月の安定性−5重量%のケトプロフェン−1kgバッチ
Claims (10)
- 水中油型エマルションである局所組成物であって、重量ベースで
約0.5から約15パーセントのケトプロフェン、約0.01から約1パーセントのキレート剤、約0.15から約1.5パーセントの架橋ポリアクリル酸共重合体、約0.15から約1.5パーセントの架橋ポリアクリル酸ホモポリマー、約2.5から約6パーセントのオキシベンゾン、約0.25から約2.5パーセントの乳化剤、約5から約15パーセントの水混和性アルキレングリコール、約10から約30パーセントのC2−C3アルカノール、約0.5から約2.5パーセントの化粧品防腐剤、約0.02から約2パーセントの抗酸化剤、約0.001から約0.1パーセントの皮膚軟化薬、該組成物のpH値を約4.5から約6の範囲内に維持するのに十分な量のpH調整剤、および残りは水
を含有する、局所組成物。 - 水中油型エマルションがクリーム状の粘度を有する、請求項1に記載の局所組成物。
- 請求項1に記載の局所組成物であって、
約10パーセントのケトプロフェン、約0.05パーセントのエチレンジアミン四酢酸の二ナトリウム塩、約1.25パーセントの架橋ポリアクリル酸共重合体、約0.5パーセントの架橋ポリアクリル酸ホモポリマー、約5パーセントのオキシベンゾン、約0.5パーセントのPEG−40硬化ヒマシ油、約10パーセントのプロピレングリコール、約10パーセントの無水エタノール、約9パーセントのイソプロパノール、約1パーセントのベンジルアルコール、約0.05パーセントのビタミンE、約1パーセントのブチル化ヒドロキシトルエン、約3パーセントのミリスチン酸イソプロピル、約1.5パーセントのトリエタノールアミン、および残りは水
を含有する、局所組成物。 - 請求項1に記載の局所組成物であって、
約5パーセントのケトプロフェン、約0.05パーセントのエチレンジアミン四酢酸の二ナトリウム塩、約1.25パーセントの架橋ポリアクリル酸共重合体、約0.5パーセントの架橋ポリアクリル酸ホモポリマー、約5パーセントのオキシベンゾン、約0.5パーセントのPEG−40硬化ヒマシ油、約10パーセントのプロピレングリコール、約10パーセントの無水エタノール、約9パーセントのイソプロパノール、約1パーセントのベンジルアルコール、約0.05パーセントのビタミンE、約1パーセントのブチル化ヒドロキシトルエン、約3パーセントのミリスチン酸イソプロピル、約1.5パーセントのトリエタノールアミン、および残りは水
を含有する、局所組成物。 - 請求項1に記載の局所組成物であって、
約0.5パーセントのケトプロフェン、約0.05パーセントのエチレンジアミン四酢酸の二ナトリウム塩、約1.25パーセントの架橋ポリアクリル酸共重合体、約0.5パーセントの架橋ポリアクリル酸ホモポリマー、約5パーセントのオキシベンゾン、約0.5パーセントのPEG−40硬化ヒマシ油、約10パーセントのプロピレングリコール、約10パーセントの無水エタノール、約9パーセントのイソプロパノール、約1パーセントのベンジルアルコール、約0.05パーセントのビタミンE、約1パーセントのブチル化ヒドロキシトルエン、約3パーセントのミリスチン酸イソプロピル、約1.5パーセントのトリエタノールアミン、および残りは水
を含有する、局所組成物。 - 疼痛を患っている患者に治療有効量の請求項1に記載の組成物を局所適用することを含む、疼痛を治療する方法。
- 組成物を、1回適用当たり約500ミリグラムまでのケトプロフェンを提供する量で適用する、請求項6に記載の方法。
- 組成物を毎日適用する、請求項6に記載の方法。
- 片頭痛を患っている患者の前頭に治療有効量の請求項1に記載の組成物を局所適用することを含む、片頭痛を治療する方法。
- 組成物を毎日適用する、請求項9に記載の方法。
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PCT/US2013/061403 WO2014052313A1 (en) | 2012-09-27 | 2013-09-24 | Topical ketoprofen composition |
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Publication number | Priority date | Publication date | Assignee | Title |
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JP2018537503A (ja) * | 2015-12-16 | 2018-12-20 | アケリオス セラピューティクス,インコーポレーテッド | 末梢神経障害を治療するための方法及び組成物 |
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CA2885619A1 (en) | 2014-04-03 |
MX2015004006A (es) | 2015-10-29 |
EP2900231B1 (en) | 2021-11-03 |
US8822537B2 (en) | 2014-09-02 |
CA2885619C (en) | 2020-09-08 |
HK1212898A1 (zh) | 2016-06-24 |
IL237810B (en) | 2018-06-28 |
EP2900231A4 (en) | 2016-03-02 |
NZ706108A (en) | 2018-03-23 |
BR112015006790B1 (pt) | 2022-05-31 |
BR112015006790A2 (pt) | 2017-07-04 |
JP6238991B2 (ja) | 2017-11-29 |
EP2900231A1 (en) | 2015-08-05 |
AU2013323766A1 (en) | 2015-04-09 |
KR102184245B1 (ko) | 2020-11-30 |
RU2652345C2 (ru) | 2018-04-25 |
WO2014052313A1 (en) | 2014-04-03 |
US20140088195A1 (en) | 2014-03-27 |
ES2902850T3 (es) | 2022-03-30 |
KR20150074009A (ko) | 2015-07-01 |
RU2015115723A (ru) | 2016-11-20 |
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