JP2004115525A - 抗炎症性化合物の局所搬送用搬送剤 - Google Patents
抗炎症性化合物の局所搬送用搬送剤 Download PDFInfo
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- JP2004115525A JP2004115525A JP2003338818A JP2003338818A JP2004115525A JP 2004115525 A JP2004115525 A JP 2004115525A JP 2003338818 A JP2003338818 A JP 2003338818A JP 2003338818 A JP2003338818 A JP 2003338818A JP 2004115525 A JP2004115525 A JP 2004115525A
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- menthol
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- camphor
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Abstract
【解決手段】複数の疎水性化合物から成る液体状共融混合物を含む搬送剤、具体的には、当該共晶化合物は樟脳とメントールを含むことを特徴とし、更にはグリセリンエステル類、シリコーン類、あるいはトコフェロール類を含むことが出来、活性成分としてはインドメタシン等が挙げられる。
【選択図】なし
Description
(±)樟脳とL−メントールとを、透明な液体になるまで、40℃〜50℃で加熱しながら混合した。
油相調製
大豆レシチン、MCT油およびTPGSを、均一な溶液になるまで45℃で混合した。次に、Tween−80(商標)を加え、その後、前記共融混合搬送剤を加えた。この混合物を完全に溶解するまで攪拌した。この加温混合物にインドメタシン(USPグレード)を加え、完全に溶解するまで45℃で10分攪拌した。
EDTA二ナトリウム塩、グリセリンおよびTween−80(商標)を水(計算量の90%)に加え、完全に溶解するまで攪拌した。
この溶液を、前記油相と合わせ、適当なミキサーを用いて十分に混合し、8,000−12,000 psi (600−800 bar)で高圧ホモゲナイザー(Avestin(登録商標) C−5)を用いて均一にした。この混合物を、2から3回ホモゲナイザーに通過させた。
別の容器において、カルボポル(登録商標)971Pを、計算量の水10%と混合し、2から6時間浸水させた。カルボポル(登録商標)ペーストを、ホモゲナイズし均一化した乳化物と、高いせん断力を持つ回転・静止型ミキサー(Omni GLHミキサー)を18,000−24,000 rpm(1分当たりの回転数)で用いて混合した。混合している間、トリエタノールアミンを、所望のpHと粘度が得られるまで徐々に加えた。
本組成物は、実施例1の方法に倣って調製した。
1%ジクロフェナッククリームの組成を表3に示す。このクリームは、MCT:樟脳:メントール比6:3:4による油相を約14%含んでいる。
水相は、ジクロフェナックナトリウムとTween−80(商標)を、85℃の純水に溶解して調製した。
5%イブプロフェンクリームを、実施例2に記載したように調製した。5%ジクロフェナッククリーム用の乳剤の組成を表4に示す。このクリームは、約4.25:1:1の比で表されるMCT:樟脳:メントールから成る油相を約26%含む。
本組成物は実施例4に記載する方法によって調製した。ただし、L−(−)−メントールは、チモール(2−イソプロピル−5−メチルフェノール)と置換した。このクリームは、約2:5:5:2の比で表されるMCT:樟脳:チモール:トコフェロールアセテートから成る油相を約28%含んでいた。
インドメタシンによる乳剤を米国特許第6,113,921号に従って調製した。
動物(ラット、カラゲナン誘発性前肢浮腫モデル)について調べたところ、共融搬送剤を含む局所塗布組成においてかなりの抗炎症作用が示された。
Claims (20)
- 局所搬送用搬送剤であって、複数の疎水性化合物の液体状共融混合物を含む搬送剤。
- 前記共融混合物は樟脳とメントールを含むことを特徴とする、請求項1に記載の搬送剤。
- 前記樟脳は、D−異性体、L−異性体、樟脳ラセミ体、または、複数の樟脳異性体の混合物から成るグループから選ばれることを特徴とする、請求項2に記載の搬送剤。
- 前記メントールは、D−異性体、L−異性体、メントールラセミ体、または、複数のメントール異性体の混合物から成るグループから選ばれることを特徴とする、請求項2に記載の搬送剤。
- 前記樟脳と前記メントールとは、4:1と1:4の間の比として存在することを特徴とする、請求項2に記載の搬送剤。
- 前記樟脳と前記メントールとは、2:1と1:2の間の比として存在することを特徴とする、請求項2に記載の搬送剤。
- さらにチモールを含むことを特徴とする、請求項2に記載の搬送剤。
- 前記共融混合物は樟脳とチモールを含むことを特徴とする、請求項1に記載の搬送剤。
- さらに液体状疎水成分を含むことを特徴とする、請求項1に記載の搬送剤。
- 前記疎水性成分は、薬学的に受容可能なグリセリンエステル類、脂肪族エステル類、芳香族エステル類、ワックス類、脂質類、油脂類、脂質可溶性ビタミン類、炭化水素類、シリコンポリマー類、トコフェロール類、トコトリエノール類、および、関連化合物、または、それらの混合物から成るグループから選ばれることを特徴とする、請求項9に記載の搬送剤。
- 前記疎水成分と液体状共融混合物とは、1:10と10:1の間の比として存在することを特徴とする、請求項9に記載の搬送剤。
- 前記疎水成分と液体状共融混合物とは、1:3と3:1の間の比として存在することを特徴とする、請求項9に記載の搬送剤。
- 水中油成分、または、油中水成分としての乳剤または微細乳剤を含む局所搬送用組成物であって、前記乳剤の前記油相は、請求項11に記載の搬送剤を含むことを特徴とする組成物。
- 活性成分が、前記乳剤または微細乳剤の前記油相に溶解していることを特徴とする、請求項13に記載の組成物。
- 前記油相は、前記組成物を5%から80%含むことを特徴とする、請求項13に記載の組成物。
- 界面活性剤をさらに含むことを特徴とする、請求項13に記載の組成物。
- 前記活性成分は抗炎症薬剤類の内から選ばれることを特徴とする、請求項14に記載の組成物。
- 請求項17に記載の組成物であって、前記複数の抗炎症剤は、インドメタシン、ジクロフェナック、ケトロラック、ピロキシカム、テノキシカム、ケトプロフェン、フルルビプロフェン、イブプロフェン、ナプロキセン、および、サリチル酸から成るグループから選ばれることを特徴とする組成物。
- 請求項13に記載の組成物であって、追加の薬剤、製薬的に受容可能な界面活性剤、粘度調整剤、抗菌性防腐剤、皮膚浸透促進剤、芳香剤および着色剤をさらに含むことを特徴とする組成物。
- 前記抗炎症剤は、非ステロイド抗炎症剤を含むことを特徴とする、請求項17に記載の組成物。
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US10/255,951 US7138394B2 (en) | 2002-09-27 | 2002-09-27 | Vehicle for topical delivery of anti-inflammatory compounds |
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JP2004115525A true JP2004115525A (ja) | 2004-04-15 |
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US (3) | US7138394B2 (ja) |
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Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2008013449A (ja) * | 2006-07-04 | 2008-01-24 | Taisho Pharmaceut Co Ltd | ユビデカレノン含有自己乳化組成物 |
JP2012523408A (ja) * | 2009-04-08 | 2012-10-04 | カディラ・ヘルスケア・リミテッド | ジクロフェナクの安定な医薬組成物 |
WO2015151990A1 (ja) * | 2014-03-30 | 2015-10-08 | 小林製薬株式会社 | 外用医薬組成物 |
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JP2008013449A (ja) * | 2006-07-04 | 2008-01-24 | Taisho Pharmaceut Co Ltd | ユビデカレノン含有自己乳化組成物 |
JP2012523408A (ja) * | 2009-04-08 | 2012-10-04 | カディラ・ヘルスケア・リミテッド | ジクロフェナクの安定な医薬組成物 |
WO2015151990A1 (ja) * | 2014-03-30 | 2015-10-08 | 小林製薬株式会社 | 外用医薬組成物 |
JP2015189760A (ja) * | 2014-03-30 | 2015-11-02 | 小林製薬株式会社 | 外用医薬組成物 |
JP2015189759A (ja) * | 2014-03-30 | 2015-11-02 | 小林製薬株式会社 | 外用医薬組成物 |
JP2022500446A (ja) * | 2018-09-17 | 2022-01-04 | ソシエテ・デクスプロワタシオン・デ・プロデュイ・プール・レ・アンデュストリー・シミック・セピックSociete D’Exploitation De Produits Pour Les Industries Chimiques Seppic | 少なくとも1つの抗炎症物質を含む局所使用のための医薬組成物 |
Also Published As
Publication number | Publication date |
---|---|
US7138394B2 (en) | 2006-11-21 |
US20060211688A1 (en) | 2006-09-21 |
US20040063794A1 (en) | 2004-04-01 |
CN100534530C (zh) | 2009-09-02 |
US20050158348A1 (en) | 2005-07-21 |
MXPA03008947A (es) | 2005-04-19 |
CN1500524A (zh) | 2004-06-02 |
US7781429B2 (en) | 2010-08-24 |
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