JPWO2012057220A1 - 経皮吸収型製剤 - Google Patents
経皮吸収型製剤 Download PDFInfo
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- JPWO2012057220A1 JPWO2012057220A1 JP2012540913A JP2012540913A JPWO2012057220A1 JP WO2012057220 A1 JPWO2012057220 A1 JP WO2012057220A1 JP 2012540913 A JP2012540913 A JP 2012540913A JP 2012540913 A JP2012540913 A JP 2012540913A JP WO2012057220 A1 JPWO2012057220 A1 JP WO2012057220A1
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- transdermal
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- skin
- fatty acid
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Abstract
Description
また、経皮投与法の利点として、徐放化することにより一定の血中濃度を維持することで副作用を軽減することが期待される。なかでも、長期間(1日〜7日)にわたって投与できる経皮投与型製剤が患者のコンプライアンスの点から望まれる傾向にある。
イミダフェナシンは現在臨床の場において経口投与剤として用いられているところ、肝障害などの副作用の軽減および長期間にわたる血中濃度の安定化および効果の持続性の観点から、経口投与よりも、むしろ貼付剤等による経皮投与型製剤の開発が望まれている。
特許文献1および2には、4−(2−メチル−1H−イミダゾール−1−イル)−2,2−ジフェニルブタンアミド(イミダフェナシン)を含有する経皮吸収型製剤が記載されるが、イミダフェナシンは皮膚透過性が低く、皮膚を介して薬物を効率よく吸収させる皮膚吸収型製剤において用いるためには、皮膚透過性を増加させ、かつ結晶を生じさせないようにする必要があるが、特許文献1および2はともに、かかる課題を解決する手段を提供するものではない。
特許文献3には、遊離塩基性薬物と炭素数が8〜22の脂肪族炭化水素基を有する脂肪酸と粘着剤を含有する膏体層と支持体とを備えた貼付剤が記載されているが、頻尿・尿失禁の治療薬であるイミダフェナシンを含有する経皮吸収型製剤において、結晶を生じさせないようにすると同時に皮膚透過性を低下させないという課題を解決する手段を提供するものではない。
(a) イミダフェナシンおよび/またはその塩、イソステアリン酸および脂肪酸エステルを含有する経皮吸収型製剤。
(b) イソステアリン酸が結晶析出防止剤である、(a)に記載の経皮吸収型製剤。
(c) 経皮吸収型製剤におけるイソステアリン酸の含有量が2〜20質量%である、(a)または(b)に記載の経皮吸収型製剤。
(d) 脂肪酸エステルがモノラウリン酸ソルビタンである、(a)〜(c)のいずれかに記載の経皮吸収型製剤。
(e) 経皮吸収促進剤としてトリアセチンをさらに含有する、(a)〜(d)のいずれかに記載の経皮吸収型製剤。
(f) 適用から15時間後の皮膚透過速度が2.0μg/cm2/hrよりも大きく、累積透過量が30μg/cm2よりも大きい、(a)〜(e)のいずれかに記載の経皮吸収型製剤。
(g) 粘着基剤を含有する粘着剤組成物を含む皮膚外用貼付剤である、(a)〜(f)のいずれかに記載の経皮吸収製剤。
(h) 粘着基剤として(メタ)アクリル酸エステル共重合体を含む、(g)に記載の経皮吸収型製剤。
(i) 粘着剤組成物を支持体に積層し、ライナーを被覆してなる構造を有する皮膚外用貼付剤である、(g)または(h)に記載の経皮吸収型製剤。
(j) イミダフェナシンおよび/またはその塩を含有する経皮吸収製剤において、結晶防止剤としてのイソステアリン酸と脂肪酸エステルをさらに含有させる、経皮吸収型製剤の製造方法。
本発明の経皮吸収型製剤におけるイソステアリン酸の含有量は、とくに制限はされないが、好ましくは1〜20質量%、より好ましくは2〜7質量%である。
本発明の経皮吸収型製剤におけるモノラウリン酸ソルビタンの含有量は、とくに制限はされないが、好ましくは1〜20質量%、より好ましくは3〜10質量%である。
本発明の経皮吸収型製剤におけるミリスチン酸イソプロピルの含有量は、とくに制限はされないが、好ましくは1〜15質量%、より好ましくは3〜10質量%である。
本発明の経皮吸収型製剤におけるオレイルアルコール、オクチルドデカノールまたはステアリルアルコールの含有量は、とくに制限はされないが、好ましくは1〜15質量%、より好ましくは3〜10質量%である。
皮膚外用貼付剤は、好ましくは、粘着剤組成物を支持体に積層し、ライナーを被覆してなる構造を有する。
この親水性基剤に用いられる水溶性高分子として、ゼラチン、カゼイン、プルラン、デキストラン、アルギン酸ナトリウム、可溶性デンプン、カルボキシデンプン、デキストリン、カルボキシメチルセルロース、カルボキシメチルセルロースナトリウム、メチルセルロース、エチルセルロース、ヒドロキシエチルセルロース、ポリビニルアルコール、ポリエチレンオキサイド、ポリアクリル酸、ポリアクリルアミド、ポリアクリル酸ナトリウム、ポリビニルピロリドン、カルボキシビニルポリマー、ポリビニルエーテル、メトキシエチレン無水マレイン酸共重合体、イソブチレン無水マレイン酸共重合体、N−ビニルアセトアミド、N−ビニルアセトアミドとアクリル酸および/またはアクリル酸塩共重合体等から1種または2種以上のものが適宜選ばれる。この場合、水溶性高分子の配合量は製剤全体の1〜30質量%、好ましくは1〜20質量%、より好ましくは1〜15質量%である。配合量が少ななすぎると粘度が低くなって保型性低下し、多すぎると逆に粘度が高くなって練合時や塗工時の作業性が低下する。
この硬膏剤は、従来公知の製造法によって容易に製造できるものであり、例えば、合成ゴム系のテープの場合、ニーダー、ミキサー等の混合機を用い、120〜160℃で粘着性基剤と軟化剤および粘着付与剤を加熱混合し、次いで薬効成分を添加混合し、直接ポリプロピレンまたはポリエステル等のフィルムに展延するか、あるいは一旦、離型処理の施された紙、もしくはフィルムに展延した後所望の支持体を覆い、圧着転写させてもよい。
次に、その他の経皮吸収型製剤である軟膏剤、ゲル剤、クリーム剤、ゲル状クリーム剤、ローション剤、リザーバー型パッチ剤、リニメント剤、エアゾール剤の配合処方について簡単に説明する。
この軟膏剤の製剤処方は、例えば高級脂肪酸またはそのエステル5〜15質量%、界面活性剤1〜10質量%、薬効成分0.5〜10質量%を室温または加温下で混合し、ロウ類4〜10質量%、炭化水素50〜90質量%を加え加温または加熱融解し、50〜100℃に保ち、全成分が透明溶解液になった後、ホモミキサーで均一に混和する。その後、撹拌しながら室温まで下げることによって軟膏剤とするものである。
このゲル剤の製剤処方は、例えば水55質量%以下にゲル化剤0.5〜5質量%を加えて膨張させる。一方、薬効成分0.5〜10質量%をグリコール類40質量%以下と低級アルコール60質量%以下の混合物に溶解する。これら両者を混合し、さらに中和剤を加えてpH4〜7となるように調整し、ゲル剤が得られる。
このクリーム剤の配合処方は、上記した薬効成分、高級脂肪酸エステル、水、炭化水素類、乳化剤を適量加え混合、撹拌することにより得られる。
このゲル状クリーム剤の配合処方は、例えば薬効成分0.5〜10質量%を高級脂肪酸エステル25質量%以下と低級アルコール40質量%以下の混合物に溶解し、さらに乳化剤5質量%以下を加える。一方、水にゲル化剤0.5〜5質量%を加えて膨張させる。次に、両者を混合しホモミキサーで均一に乳化させ、乳化後、中和剤を添加し、pHを4〜8に調整する。
このローション剤の配合処方は、上記した薬効成分、低級アルコール、水および/またはグリコール類を適量加えて混合、撹拌することにより得られる。
リニメント剤の配合処方は、薬効成分0.5〜10質量%をアルコール10〜70質量%、水55質量%以下、脂肪酸エステル60質量%以下と混合、撹拌することにより得られる。
エアゾール剤の具体的な処方は、薬効成分0.5〜10質量%を低級アルコール、水に配合し、エアゾール容器に充填し、さらに噴射剤としてジメチルエーテルおよび/または液化石油ガスを圧入することにより得られる。
ヘアレスマウスより摘出した皮膚(体側部)の角質層側に上記経皮吸収型製剤を貼付し、即ち上記経皮吸収型製剤を適用し、真皮側をレセプター層側にしてフロースルー型拡散セルに装着した。レセプター層はpH7.4のリン酸緩衝生理食塩水を皮膚表面温度が32±1℃となるように循環させ、一定時間毎にサンプリングを行い、高速液体クロマトグラフ法により薬物濃度を測定し、さらに皮膚透過速度(Flux(μg/cm2/hr))を算出した。
さらに、イソステアリン酸に加え、モノラウリン酸ソルビタンおよび/またはトリアセチンを含有する経皮吸収型製剤においては、結晶が析出されないだけでなく、適用から15時間後の時点で2.0μg/cm2/hrより大きな皮膚透過速度を測定し、さらに高いJmax値が短い時間(Tmax)で得られ、30μg/cm2を超える大きな累積透過量を有する、良好なヘアレスマウス皮膚透過性を呈し、よって、製剤安定性に加え、十分な皮膚浸透性を有する経皮吸収型製剤であることが実証された。
Claims (10)
- イミダフェナシンおよび/またはその塩、イソステアリン酸および脂肪酸エステルを含有する経皮吸収型製剤。
- イソステアリン酸が結晶析出防止剤である、請求項1に記載の経皮吸収型製剤。
- 経皮吸収型製剤におけるイソステアリン酸の含有量が2〜20質量%である、請求項1または2に記載の経皮吸収型製剤。
- 脂肪酸エステルがモノラウリン酸ソルビタンである、請求項1〜3のいずれか一項に記載の経皮吸収型製剤。
- 経皮吸収促進剤としてトリアセチンをさらに含有する、請求項1〜4のいずれか一項に記載の経皮吸収型製剤。
- 適用から15時間後の皮膚透過速度が2.0μg/cm2/hrよりも大きく、累積透過量が30μg/cm2よりも大きい、請求項1〜5のいずれか一項に記載の経皮吸収型製剤。
- 粘着基剤を含有する粘着剤組成物を含む皮膚外用貼付剤である、請求項1〜6のいずれか一項に記載の経皮吸収製剤。
- 粘着基剤として(メタ)アクリル酸エステル共重合体を含む、請求項7に記載の経皮吸収型製剤。
- 粘着剤組成物を支持体に積層し、ライナーを被覆してなる構造を有する皮膚外用貼付剤である、請求項7または8に記載の経皮吸収型製剤。
- イミダフェナシンおよび/またはその塩を含有する経皮吸収製剤において、結晶防止剤としてのイソステアリン酸と脂肪酸エステルをさらに含有させる、経皮吸収型製剤の製造方法。
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