JP2018525318A - 爪甲真菌症の予防用または治療用の医薬組成物およびその製造方法 - Google Patents
爪甲真菌症の予防用または治療用の医薬組成物およびその製造方法 Download PDFInfo
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/00—Medicinal preparations containing organic active ingredients
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- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
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- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
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Abstract
Description
表1に示した成分および量にしたがってハイドロゲルを製造した。表1の量は、ハイドロゲル中の各成分のwt%を表す。ポリビニルピロリドンおよびポリビニルアルコールを水(使用する全重量の約60%)に加えた後、得られた混合物を50℃で加熱しながら撹拌して溶液を得た(溶液A)。尿素およびフマル酸(製剤例4の場合、酒石酸)を残りの水に加えた後、得られた混合物を80℃で加熱しながら撹拌して溶液を得た(溶液B)。1,3−ブチレングリコール、ポリアクリル酸(AC−10LHPK)、アクリル酸とアクリル酸ナトリウムとの共重合体(AP−40F)、アルミニウムグリシネート、グリセリン、カルボキシメチルセルロースナトリウム、SpanTM80、TweenTM80、エチレンジアミン四酢酸二ナトリウム、メチルパラベンおよびプロピルパラベンを均一に混合し、これに溶液Aおよび溶液Bを加えて、約15分間均一に混合した。得られた溶液をエンボスポリプロピレンフィルム(embossed polypropylene film)上に塗布した後;支持膜として、ポリウレタンでコーティングした不織布をその上に積層して、パッチ剤形態を有するハイドロゲル含有製剤を製造した。
製剤例1〜4で得られたパッチ剤およびラッカー剤(EmtrixTM、Ozhealth pharma社製)をそれぞれブタ足指爪に5時間適用して、角質溶解能および水分保持能を評価した。水分保持能の評価は、水分の保持による膨潤の程度を測定することによって行った。すなわち、水分保持能の評価は、それぞれの製剤の適用前後の足指爪の厚さ変化を測定することによって行った。角質溶解能の評価は、製剤の適用前後の足指爪の硬度変化をテクスチャーアナライザー(texture analyzer)で測定することによって行った。各製剤の適用前の厚さおよび硬度を100%としたときの、各製剤の適用後の厚さおよび硬度の変化を、下記表2および表3に示す。
製剤例1で得られたパッチ剤を用いて、爪甲真菌症の患者を対象とする臨床試験を行った。
Claims (16)
- 尿素;フマル酸;1,3−ブチレングリコール;ゲル形成性重合体;架橋剤;および45〜60wt%の水を含み、ハイドロゲル形態であり、角質溶解能および水分保持能を有する爪甲真菌症の予防用または治療用の医薬組成物。
- 前記尿素が、前記組成物の全重量に対して、15〜25wt%の範囲の量で存在することを特徴とする請求項1に記載の医薬組成物。
- 前記フマル酸が、前記組成物の全重量に対して、0.5〜2.5wt%の範囲の量で存在することを特徴とする請求項1に記載の医薬組成物。
- 前記1,3−ブチレングリコールが、前記組成物の全重量に対して、8〜18wt%の範囲の量で存在することを特徴とする請求項1に記載の医薬組成物。
- 前記ゲル形成性重合体が、ポリアクリル酸、アクリル酸とアクリル酸ナトリウムとの共重合体、またはその混合物であることを特徴とする請求項1に記載の医薬組成物。
- 前記ゲル形成性重合体が、前記組成物の全重量に対して、5〜10wt%の範囲の量で存在することを特徴とする請求項1に記載の医薬組成物。
- 前記架橋剤が、アルミニウムグリシネートであることを特徴とする請求項1に記載の医薬組成物。
- 前記架橋剤が、前記組成物の全重量に対して、0.1〜0.5wt%の範囲の量で存在することを特徴とする請求項1に記載の医薬組成物。
- 15〜25wt%の尿素;0.5〜2.5wt%のフマル酸;8〜18wt%の1,3−ブチレングリコール;5〜10wt%のゲル形成性重合体;0.1〜0.5wt%の架橋剤;および45〜60wt%の水を含むことを特徴とする請求項1に記載の医薬組成物。
- 可塑剤、増粘剤、界面活性剤、キレート化剤および保存剤からなる群から選択される1種以上の添加剤をさらに含むことを特徴とする請求項1〜9のいずれかに記載の医薬組成物。
- 前記可塑剤が、グリセリンであり、前記組成物の全重量に対して、3〜8wt%の範囲の量で存在することを特徴とする請求項10に記載の医薬組成物。
- 前記増粘剤が、カルボキシメチルセルロースまたはその塩、ポリビニルピロリドンおよびポリビニルアルコールからなる群から選択される1種以上であり;前記組成物の全重量に対して、5〜10wt%の範囲の量で存在することを特徴とする請求項10に記載の医薬組成物。
- 前記界面活性剤が、ソルビタンモノオレートおよびポリオキシエチレンソルビタン脂肪酸エステルからなる群から選択される1種以上であり;前記組成物の全重量に対して、0.3〜1wt%の範囲の量で存在することを特徴とする請求項10に記載の医薬組成物。
- 前記キレート化剤が、エチレンジアミン四酢酸またはその塩であり;前記保存剤が、メチルパラベンおよびプロピルパラベンからなる群から選択される1種以上であることを特徴とする請求項10に記載の医薬組成物。
- 尿素;フマル酸;1,3−ブチレングリコール;ゲル形成性重合体;架橋剤;45〜60wt%の水;ならびに、任意選択の成分として可塑剤、増粘剤、界面活性剤、キレート化剤および保存剤からなる群から選択される1種以上の添加剤を混合してハイドロゲルを形成することを含む、角質溶解能および水分保持能を有する爪甲真菌症の予防用または治療用の医薬組成物の製造方法。
- 前記組成物の全重量に対して、前記尿素が15〜25wt%の範囲の量で用いられ;前記フマル酸が0.5〜2.5wt%の範囲の量で用いられ;前記1,3−ブチレングリコールが8〜18wt%の範囲の量で用いられ;前記ゲル形成性重合体が5〜10wt%の範囲の量で用いられ;前記架橋剤が0.1〜0.5wt%の範囲の量で用いられ;水が45〜60wt%の範囲の量で用いられることを特徴とする請求項15に記載の方法。
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