JP2005289879A - 抗真菌性外用組成物 - Google Patents
抗真菌性外用組成物 Download PDFInfo
- Publication number
- JP2005289879A JP2005289879A JP2004107093A JP2004107093A JP2005289879A JP 2005289879 A JP2005289879 A JP 2005289879A JP 2004107093 A JP2004107093 A JP 2004107093A JP 2004107093 A JP2004107093 A JP 2004107093A JP 2005289879 A JP2005289879 A JP 2005289879A
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- Prior art keywords
- antifungal
- weight
- composition
- starch
- external use
- Prior art date
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- Granted
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Abstract
【解決手段】 (C)粉末成分として、デンプン、撥水性粉末及び酸化チタンを組み合わせて用いて、(A)抗真菌剤、(B)付着補助剤及び(C)粉末成分を含有する抗真菌性外用組成物を調製する。
【選択図】なし
Description
項1. (A)抗真菌剤、(B)付着補助剤及び(C)粉末成分を含み、(C)粉末成分として、デンプン、撥水性粉末及び酸化チタンを含有することを特徴とする、抗真菌性外用組成物。
項2. デンプン、撥水性粉末及び酸化チタンの総重量100重量部当たり、デンプンが19.2〜79.7重量部、撥水性粉末が14.7〜59.3重量部、酸化チタンが0.4〜51.9重量部の割合で含有される、項1に記載の抗真菌性外用組成物。
項3. デンプンが、バレイショデンプン、トウモロコシデンプン及びコムギデンプンよりなる群から選択される少なくとも1種である、項1又は2に記載の抗真菌性外用組成物。
項4. 撥水性粉末が、タルク、ステアリン酸マグネシウム、ステアリン酸アルミニウム及びステアリン酸亜鉛よりなる群から選択される少なくとも1種である、項1乃至3のいずれかに記載の抗真菌性外用組成物。
項5. 付着補助剤が、クロタミトン、炭酸プロピレン及び脂肪酸エステルよりなる群から選択される少なくとも1種である、項1乃至4のいずれかに記載の抗真菌性外用組成物。
項6. 抗真菌剤が、オキシコナゾール、ビフォナゾール、スルコナゾール、ネチコナゾール、テルビナフィン、ブテナフィン、アモロルフィン、ラノコナゾール及びこれらの塩よりなる群から選択される少なくとも1種である、項1乃至5のいずれかに記載の抗真菌性外用組成物。
項7. 更に、鎮痒剤を含む、項1乃至6のいずれかに記載の抗真菌性外用組成物。
項8. 更に、低級アルコール、水及びこれらの混合物よりなる群から選択される少なくとも1種を含む、項1乃至7のいずれかに記載の抗真菌性外用組成物。
項9. 抗真菌剤を0.3〜3重量%、付着補助剤を1〜15重量%、粉末成分を10〜65重量%、及び鎮痒剤を0.05〜10重量%の割合で含有する、項7に記載の抗真菌性外用組成物。
項10. 抗真菌剤を0.3〜3重量%、付着補助剤を1〜15重量%、粉末成分を10〜65重量%、鎮痒剤を0.05〜10重量%、並びに低級アルコール、水及びこれらの混合物よりなる群から選択される少なくとも1種を7〜88.65重量%の割合で含有する、項8に記載の抗真菌性外用組成物。
項11. 硝酸オキシコナゾールを0.3〜3重量%;クロタミトンを1〜15重量%;トウモロコシデンプン、タルク及び酸化チタンを総量で10〜65重量%;リドカインを0.05〜10重量%;並びにエタノール、水及びこれらの混合物よりなる群から選択される少なくとも1種を7〜88.65重量%の割合で含有する、項10に記載の抗真菌性外用組成物。
項12. 項1乃至11のいずれかに記載の抗真菌性外用組成物と、噴射剤を含有することを特徴とする、抗真菌性外用エアゾール製剤。
表1−4に示す処方の組成物(実施例1−14及び比較例1−17)を調製し、下記試験を行い、使用感及び塗布面の均一性について評価した。
(1)使用感の評価方法
使用感を評価するために、下記方法に従って動摩擦計数(MIU)を計測した。
1.人工皮革(5cm×13cm)のMIUをKES-SE表面特性試験機(カトーテック社製)で測定した。
2.同じ人工皮革に1gの各組成物(実施例1−14及び比較例1−17)を3cm×6cmの範囲に、指で均一に塗り広げ、その塗布面のMIUをKES-SE表面特性試験機(カトーテック社製)で測定した。本使用感の評価試験は、n=3で行った。
3.下記評価基準に従って、測定したMIUの平均値から使用感を評価した。
<使用感の評価基準>
○ 塗布後のMIUの平均値が、塗布前のMIUの平均値よりも小さい
× 塗布後のMIUの平均値が、塗布前のMIUの平均値よりも大きい
#:MIUは、すべりの特性と相関する値であり、MIU値の減少はすべりの改善、MIU値の増加はすべりの改悪を意味する。
人工皮革(5cm×13cm)に1gの各組成物(実施例1−14及び比較例1−17)を3cm×6cmの範囲に、指で均一に塗布し、塗布面の性状を下記評価基準に基づいて評価した。
<塗布面の均一性の評価基準>
○ 斑状や切片状の塗布面が形成されることのない均一な塗布面である
△ 斑状の塗布面は形成されないが、少量の切片状の塗布面が形成される
× 斑状や切片状の塗布面が形成される
得られた結果を表1−4に併せて示す。この結果から、クロタミトンと共に、粉末成分として、デンプン、撥水性粉末及び酸化チタンを組み合わせて使用すると塗布面に優れた使用感と均一性が付与されることが明らかとなった。これに対して、デンプン、撥水性粉末及び酸化チタンの内、いずれか一つでも掛けていると、使用感と均一性の双方において優れた塗布面を形成できないことが確認された。
表5に示す組成の抗真菌性外用組成物(実施例15−18及び比較例18−19)を調製した。この抗真菌性外用組成物を使用して、以下の試験を行い、鎮痒効果の評価及び官能評価を行った。また、併せて、上記試験例と同様の方法で、MIU値の測定による使用感の評価を行った。
1.ddY系クリーンマウス(雄、6週齢)を1週間飼育して、馴化させた。
2.マウスの体重を計測し、後背部をバリカンにて毛剃りした。
3.毛剃り部分に抗真菌性外用組成物(実施例15−18及び比較例18−19)200mgを満遍なく塗布し、指で擦り込んだ。
4.抗真菌性外用組成物塗布30分後に、エーテル麻酔を行い、かゆみ惹起物質(4.8mgのCompound48/80(ICN Biomedicals,Inc製)を1mLの生理食塩水に溶解したもの)を体重40g当たり20μLの割合でマウスに皮内投与した。
5.皮内投与5分後から25分後までの間に、マウスのスクラッチ(マウスが口で皮内投与物質を投与した部分を直接掻く行動)回数をカウントした。
6.陽性コントロールとして、抗真菌性外用組成物を塗布せずにかゆみ惹起物質を投与したものについても、同様に試験を行い、スクラッチ回数をカウントした。なお、かかる鎮痒効果の評価試験はn=6で行った。
7.下記基準に従って、各抗真菌性外用組成物の鎮痒効果を評価した。
○:平均スクラッチ回数が、陽性コントロールの平均スクラッチ回数の1/4未満
△:平均スクラッチ回数が、陽性コントロールの平均スクラッチ回数の1/4以上1/2未満
×:平均スクラッチ回数が、陽性コントロールの平均スクラッチ回数の1/2以上
官能評価
被験者(湿潤型水虫患者2人及び健常者3人の合計5人)に足指間に抗真菌性外用組成物を適当量塗布した。塗布後、靴下及び靴を履いて1日通常の生活をおくった後に、各被験者が、付着性、均一性、さらさら感、実感、総合的使用感のそれぞれについて、下記5段階の評点で評価を行った。
5点:極めて良好である
4点:良好である
3点:普通である
2点:良くない
1点:悪い
得られた各被験者の評点を合計して、下記基準に従って、各抗真菌性外用組成物の官能評価について判定した。
<官能評価の評価基準>
◎:評点の合計20以上25以下
○:評点の合計15以上19以下
△:評点の合計10以上14以下
×:評点の合計5以上9以下
得られた結果を表5に併せて示す。この結果、本発明の抗真菌性外用組成物は、抗真菌作用に加えて、極めて良好な使用感が得られることが明らかとなった。
表6に示す処方の抗真菌性外用組成物(実施例19−25)を調製した。該抗真菌性外用組成物(実施例19−25)を噴射剤(ジメチルエーテル)と共に、該抗真菌性外用組成物:噴射剤=1:4の重量比で、エアゾール容器に充填して、抗真菌性外用エアゾール製剤を製した。また、同様に、該抗真菌性外用組成物(実施例19−25)を噴射剤(液化石油ガス)と共に、該抗真菌性外用組成物:噴射剤=1:4の重量比で、エアゾール容器に充填して、抗真菌性外用エアゾール製剤を製した。
表7に示す処方の軟膏を常法に従って調製した。
Claims (10)
- (A)抗真菌剤、(B)付着補助剤及び(C)粉末成分を含み、(C)粉末成分として、デンプン、撥水性粉末及び酸化チタンを含有することを特徴とする、抗真菌性外用組成物。
- デンプン、撥水性粉末及び酸化チタンの総重量100重量部当たり、デンプンが19.2〜79.7重量部、撥水性粉末が14.7〜59.3重量部、酸化チタンが0.4〜51.9重量部の割合で含有される、請求項1に記載の抗真菌性外用組成物。
- デンプンが、バレイショデンプン、トウモロコシデンプン及びコムギデンプンよりなる群から選択される少なくとも1種である、請求項1又は2に記載の抗真菌性外用組成物。
- 撥水性粉末が、タルク、ステアリン酸マグネシウム、ステアリン酸アルミニウム及びステアリン酸亜鉛よりなる群から選択される少なくとも1種である、請求項1乃至3のいずれかに記載の抗真菌性外用組成物。
- 付着補助剤がクロタミトン、炭酸プロピレン及び脂肪酸エステルよりなる群から選択される少なくとも1種である、請求項1乃至4のいずれかに記載の抗真菌性外用組成物。
- 抗真菌剤が、オキシコナゾール、ビフォナゾール、スルコナゾール、ネチコナゾール、テルビナフィン、ブテナフィン、アモロルフィン、ラノコナゾール及びこれらの塩よりなる群から選択される少なくとも1種である、請求項1乃至5のいずれかに記載の抗真菌性外用組成物。
- 更に、鎮痒剤を含む、請求項1乃至6のいずれかに記載の抗真菌性外用組成物。
- 更に、低級アルコール、水及びこれらの混合物よりなる群から選択される少なくとも1種を含む、請求項1乃至7のいずれかに記載の抗真菌性外用組成物。
- 硝酸オキシコナゾールを0.3〜3重量%;クロタミトンを1〜15重量%;トウモロコシデンプン、タルク及び酸化チタンの混合物を10〜65重量%;リドカインを0.05〜10重量%;並びにエタノール、水及びこれらの混合物よりなる群から選択される少なくとも1種を7〜88.65重量%の割合で含有する、請求項8に記載の抗真菌性外用組成物。
- 請求項1乃至9のいずれかに記載の抗真菌性外用組成物と、噴射剤を含有することを特徴とする、抗真菌性外用エアゾール製剤。
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| JP2004107093A JP3783104B2 (ja) | 2004-03-31 | 2004-03-31 | 抗真菌性外用組成物 |
| PCT/JP2004/013363 WO2005099764A1 (ja) | 2004-03-31 | 2004-09-14 | 抗真菌性外用組成物 |
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| JP2004107093A JP3783104B2 (ja) | 2004-03-31 | 2004-03-31 | 抗真菌性外用組成物 |
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| JP2005289879A true JP2005289879A (ja) | 2005-10-20 |
| JP3783104B2 JP3783104B2 (ja) | 2006-06-07 |
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Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8058303B2 (en) | 2006-03-08 | 2011-11-15 | Nihon Nohyaku Co, Ltd | Pharmaceutical composition for external use |
| US8268876B2 (en) | 2006-03-08 | 2012-09-18 | Nihon Nohyaku Co., Ltd. | Pharmaceutical composition for external use |
| US8349882B2 (en) | 2006-03-08 | 2013-01-08 | Nihon Nohyaku Co., Ltd. | Pharmaceutical composition for external use |
| US8513296B2 (en) | 2007-09-05 | 2013-08-20 | Pola Pharma Inc. | Pharmaceutical composition |
| US8952044B2 (en) | 2009-08-25 | 2015-02-10 | Pola Pharma Inc. | Antimycotic pharmaceutical composition |
| US9050271B2 (en) | 2009-04-09 | 2015-06-09 | Pola Pharma Inc. | Antimycotic pharmaceutical composition |
| US9480678B2 (en) | 2007-09-05 | 2016-11-01 | Pola Pharma Inc. | Antifungal pharmaceutical composition |
| US9968591B2 (en) | 2007-09-05 | 2018-05-15 | Pola Pharma Inc. | Antifungal composition |
| US10130610B2 (en) | 2009-04-09 | 2018-11-20 | Pola Pharma Inc. | Antimycotic pharmaceutical composition |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2395839B1 (en) | 2009-02-13 | 2014-05-07 | Topica Pharmaceuticals, Inc | Anti-fungal formulation |
| JP5538297B2 (ja) * | 2011-04-25 | 2014-07-02 | 小林製薬株式会社 | 外用剤キット |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ220364A (en) * | 1986-05-30 | 1990-04-26 | Garry D Fields | A liquid body powder composition and method of preparation |
| FR2666962B1 (fr) * | 1990-09-26 | 1996-06-14 | Oreal | Composition antifongique sous forme de spray sec. |
| CA2052193A1 (en) * | 1990-09-28 | 1992-03-29 | Norio Takasugi | Topical powder composition containing cyclic amp derivative |
| JP3124106B2 (ja) * | 1992-04-13 | 2001-01-15 | 久光製薬株式会社 | 複合粉体抗菌剤 |
| JPH0840899A (ja) * | 1994-07-29 | 1996-02-13 | Tokyo Tanabe Co Ltd | 硝酸オキシコナゾールのエアゾール剤 |
| JPH11106332A (ja) * | 1997-08-07 | 1999-04-20 | Taisho Pharmaceut Co Ltd | 粉末エアゾール製剤 |
| JPH11302126A (ja) * | 1998-04-24 | 1999-11-02 | Kose Corp | 液状アイライナー化粧料 |
| JP2000119134A (ja) * | 1998-10-16 | 2000-04-25 | Kose Corp | 油性固型化粧料 |
| JP4438147B2 (ja) * | 1998-12-10 | 2010-03-24 | 大正製薬株式会社 | 抗真菌剤含有粉末エアゾール製剤 |
| JP2001097848A (ja) * | 1999-09-30 | 2001-04-10 | Kobayashi Pharmaceut Co Ltd | 外用剤組成物 |
| JP2002284702A (ja) * | 2001-01-19 | 2002-10-03 | Teika Seiyaku Kk | 外用抗真菌製剤 |
| JP2003073259A (ja) * | 2002-08-21 | 2003-03-12 | Daizo:Kk | 人体用エヤゾール製品 |
-
2004
- 2004-03-31 JP JP2004107093A patent/JP3783104B2/ja not_active Expired - Lifetime
- 2004-09-14 WO PCT/JP2004/013363 patent/WO2005099764A1/ja not_active Ceased
Cited By (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8058303B2 (en) | 2006-03-08 | 2011-11-15 | Nihon Nohyaku Co, Ltd | Pharmaceutical composition for external use |
| US8268876B2 (en) | 2006-03-08 | 2012-09-18 | Nihon Nohyaku Co., Ltd. | Pharmaceutical composition for external use |
| US8349882B2 (en) | 2006-03-08 | 2013-01-08 | Nihon Nohyaku Co., Ltd. | Pharmaceutical composition for external use |
| KR101343291B1 (ko) | 2006-03-08 | 2013-12-18 | 가부시키가이샤 폴라 파마 | 외용의 의약 조성물 |
| US8513296B2 (en) | 2007-09-05 | 2013-08-20 | Pola Pharma Inc. | Pharmaceutical composition |
| US9480678B2 (en) | 2007-09-05 | 2016-11-01 | Pola Pharma Inc. | Antifungal pharmaceutical composition |
| US9968591B2 (en) | 2007-09-05 | 2018-05-15 | Pola Pharma Inc. | Antifungal composition |
| US9050271B2 (en) | 2009-04-09 | 2015-06-09 | Pola Pharma Inc. | Antimycotic pharmaceutical composition |
| US10130610B2 (en) | 2009-04-09 | 2018-11-20 | Pola Pharma Inc. | Antimycotic pharmaceutical composition |
| US8952044B2 (en) | 2009-08-25 | 2015-02-10 | Pola Pharma Inc. | Antimycotic pharmaceutical composition |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2005099764A1 (ja) | 2005-10-27 |
| JP3783104B2 (ja) | 2006-06-07 |
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