JP6138168B2 - 多孔質微粒子を含む経皮デバイス - Google Patents
多孔質微粒子を含む経皮デバイス Download PDFInfo
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- JP6138168B2 JP6138168B2 JP2014559218A JP2014559218A JP6138168B2 JP 6138168 B2 JP6138168 B2 JP 6138168B2 JP 2014559218 A JP2014559218 A JP 2014559218A JP 2014559218 A JP2014559218 A JP 2014559218A JP 6138168 B2 JP6138168 B2 JP 6138168B2
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Description
・接着性マトリックス中にニコチンが均質分布することを特徴とするパッチを得、それにより、例外的な場合にはパッチをあるサイズに切断することを可能にすること;
・ニコチンの存在によって誘導される可塑化を制御し、それにより、接着性マトリックスの凝集性が保たれることを可能にすること;
・より薄く、より柔軟なパッチにすることにより快適さを改善し、その結果として、パッチを使用しやすくすること
の解決を試みた。
・新規マトリックス支持体を用いてニコチンの放出を制御する(最小限に制御し、速過ぎる放出(心臓および皮膚系に起こり得る副作用、とりわけ、中毒と同じ意味)を避ける)こと;
・接着および皮膚忍容性に関して良質であること;
・製品の初期物理化学的特徴にとってそのエージングが全く重大ではないパッチを得ること;
・ニコチン適合成分を選択すること;
・透明なパッチを得ること(起こり得る刺激または局所感作の現象の観察が可能になる)
を、優先的に考慮すべきである。
a.65〜93重量%の、アクリルまたはアクリレート系ポリマー、シリコーン系ポリマー、酢酸ビニル系ポリマー、天然または合成ゴム、それらのコポリマー、およびそれらの混合物を含んでなる群から選択される少なくとも1種類の自己接着性ポリマーと;
b.2〜15重量%の、スチレン、ジビニルベンゼン、メタクリル酸メチル、ジメタクリル酸エチレングリコール、4−ビニルピリジン、メタクリル酸ラウリル、メタクリル酸アリル、ジメタクリル酸グリコール、およびそれらの混合物を含んでなるモノマー群から選択されるモノマー単位を含んでなる、有効成分含有可能な少なくとも1種類のマイクロポーラス固体ポリマーと;
c.5〜20重量%の有効成分と
を含むことを特徴とする、前記自己接着性経皮デバイスに関する。
a.65〜93重量%の、アクリル系ポリマー、シリコーン系ポリマー、酢酸ビニル系ポリマー、天然または合成ゴム、それらのコポリマー、およびそれらの混合物を含んでなる群から選択される少なくとも1種類の自己接着性ポリマーと;
b.2〜15重量%の、スチレン、ジビニルベンゼン、メタクリル酸メチル、ジメタクリル酸エチレングリコール、4−ビニルピリジン、メタクリル酸ラウリル、メタクリル酸アリル、ジメタクリル酸グリコール、およびそれらの混合物を含んでなるモノマー群から選択されるモノマー単位を含んでなる、有効成分含有可能な少なくとも1種類のマイクロポーラス固体ポリマーと;
c.5〜20重量%の、有効成分としてのニコチンと;
d.所望により、0.1〜1%の酸化防止剤と;
からなることを特徴とする。
a.自己接着性ポリマーと、マイクロポーラス固体ポリマーと、有効成分、優先的には、ニコチンと、所望により酸化剤とを、均質混合物が得られるまで混合する工程;
b.工程aにおいて得られた均質混合物を、剥離可能な保護フィルム上にコーティングする工程;
c.コーティングした混合物を徐々に乾燥させる工程;
d.工程cにおいて得られた産物を支持体層上へ積層する工程;および
e.所望により、工程dにおいて得られた産物を、望ましいサイズの経皮デバイスまたはパッチが得られるような方法で切断する工程
を含むまたはそれらからなることを特徴とする方法に関する。
実施例1A:吸着能力試験(表1):
様々なマイクロポーラス固体によるニコチンの吸着能力を測定するための比較試験を行った。それらの試験は、以下の手順に従って、それらのマイクロポーラス支持体に吸着され得るニコチンの最大量を測定することであった。
・約0.1gを量り分けることにより繰返しニコチンを加える。
・ニコチンを添加するたびにスパチュラを用いてマイクロポーラス支持体にニコチンを充満させる。その際、その混合物の外観に注意する。
吸着支持体に、事前に決定したそれらの最大吸着能力(上記の表1を参照のこと)の50%または80%でニコチンを充填した。その後、洗浄試験を行って、それらの放出能力を決定する。その能力はニコチン添加量に対するニコチン放出の割合%で表される。
マイクロポーラス支持体の分散試験を、コーティング前に接着性混合物の多数相を構成する溶媒中で行う。これらの分散試験により接着性混合物の技術的な実現可能性を実証することが可能になる。
・9mLガラスバイアルに、マイクロポーラス支持体をその密度に応じて0.2〜1.25g秤量する。
・マイクロポーラス支持体に対する溶媒の質量比が約3となるように、溶媒(酢酸エチルまたはヘプタン)を加える。
・スパチュラを用いて混ぜ、混合物をすぐに観察する;48時間静置後にも混合物を観察する。
本発明による調製物を以下の方法により調製する:
接着剤、次いで、ニコチンと、マイクロポーラスポリマーと、所望によりBHTとを混合容器に入れる。撹拌パラメーター(時間および速度)は、塊形成が起こらず、かつ、均質混合物が得られるように設定し、特に、容器のサイズに応じたものとする。24時間静置した後、接着性混合物を150±5g/m2の割合でシリコーンフィルム上にコーティングし、その後、接着剤の溶媒を蒸発させるために45℃で乾燥処理を行い、続いて、そのマトリックスを透明なポリエステル支持体上へ積層する。このようにして得られた産物を望ましいサイズに切断する。
以下の実施例により、本発明による組成物の調製のために、ニコチン放出に対する接着剤の影響を説明する。
Claims (18)
- 自己接着性経皮デバイスであって、
前記自己接着性経皮デバイスが、支持体層および自己接着性マトリックス層の結合体と、剥離可能な保護フィルムとを含み、
前記自己接着性マトリックス層が、前記自己接着性マトリックス層の全重量に対して、
a.65〜93重量%の、アクリルまたはアクリレート系ポリマー、シリコーン系ポリマー、酢酸ビニル系ポリマー、天然または合成ゴム、それらのコポリマー、およびそれらの混合物を含んでなる群から選択される少なくとも1種類の自己接着性ポリマーと;
b.2〜15重量%の、メタクリル酸メチル、ジメタクリル酸エチレングリコール、メタクリル酸ラウリル、ジメタクリル酸グリコール、およびそれらの混合物を含んでなるモノマー群から選択されるモノマー単位を含んでなる、有効成分含有可能な少なくとも1種類のマイクロポーラス固体ポリマーと;
c.5〜20重量%の有効成分としてのニコチンと
を含むことを特徴とする、前記自己接着性経皮デバイス。 - 前記自己接着性ポリマーが、アクリルまたはアクリレート系のものであり、酢酸ビニル、アクリル酸2−エチルヘキシル、アクリル酸ブチル、アクリル酸、メタクリル酸メチル、アクリル酸メチル、tert−オクチルアクリルアミド、アクリル酸2−ヒドロキシエチル、メタクリル酸グリシジル、またはそれらの混合物を含んでなる群から選択されるモノマーを含んでなることを特徴とする、請求項1に記載のデバイス。
- 前記モノマーが、アクリル酸、アクリル酸ブチル、アクリル酸2−エチルヘキシル、酢酸ビニル、またはそれらの混合物を含んでなる群から選択されることを特徴とする、請求項2に記載のデバイス。
- 前記マイクロポーラス固体ポリマーが、ジメタクリル酸エチレングリコールのモノマー単位と、メタクリル酸メチルのモノマー単位とを含んでなることを特徴とする、請求項1〜3のいずれか一項に記載のデバイス。
- 前記マイクロポーラス固体ポリマーが、1μm〜100μmの間、優先的には、5μm〜50μmの間、より優先的には、15μm〜30μmの間に含まれる平均サイズの微粒子の形態で提供されることを特徴とする、請求項1〜4のいずれか一項に記載のデバイス。
- 前記マイクロポーラス固体ポリマーが、0.5mL/g〜3.0mL/gの間、優先的には、1mL/g〜2mL/gの間に含まれる全細孔容積を有することを特徴とする、請求項1〜5のいずれか一項に記載のデバイス。
- 前記マイクロポーラス固体ポリマーが、0.2mL/g〜3.0mL/gの間、優先的には、0.5mL/g〜1.5mL/gの間に含まれる粒子内部細孔容積を有することを特徴とする、請求項1〜6のいずれか一項に記載のデバイス。
- 前記マイクロポーラス固体ポリマーが、前記自己接着性ポリマー塊内に均質に分布していることを特徴とする、請求項1〜7のいずれか一項に記載のデバイス。
- 前記有効成分が、前記マイクロポーラス固体ポリマー塊中に均質に吸着されていることを特徴とする、請求項1〜8のいずれか一項に記載のデバイス。
- 前記自己接着性マトリックス層の坪量が50〜300g/m2の間、優先的には、100〜200g/m2の間に含まれることを特徴とする、請求項1〜9のいずれか一項に記載のデバイス。
- 前記自己接着性マトリックス層が、ブチルヒドロキシトルエン(BHT)、ブチルヒドロキシアニソール(BHA)、パルミチン酸アスコルビル、αトコフェロールおよびそれらのエステル、クエン酸、没食子酸プロピル、ならびにそれらの混合物を含んでなる群から選択される少なくとも1種類の酸化防止剤を含むことを特徴とする、請求項1〜10のいずれか一項に記載のデバイス。
- 前記酸化防止剤が、前記自己接着性マトリックス層中に、前記自己接着性マトリックス層の全重量に対して、0.01〜1重量%の間に含まれる割合で存在することを特徴とする、請求項11に記載のデバイス。
- 前記マイクロポーラス固体ポリマーが請求項5に記載のとおりであること、および前記坪量が100g/m2〜200g/m2の間に含まれることを特徴とする、請求項1〜12のいずれか一項に記載のデバイス。
- 1〜24時間の間に含まれるある期間中前記マトリックス層からの平均ニコチン送達速度が、10μg/cm2/時〜50μg/cm2/時の間に含まれることを特徴とする、請求項1〜13のいずれか一項に記載のデバイス。
- 請求項1〜14のいずれか一項に記載の経皮デバイスを製造するための方法であって、 以下の工程:
a.前記自己接着性ポリマーと、前記マイクロポーラス固体ポリマーと、ニコチンと、所望により酸化剤とを、均質混合物が得られるまで混合する工程;
b.工程aにおいて得られた均質混合物を、剥離可能な保護フィルム上にコーティングする工程;
c.コーティングした混合物を徐々に乾燥させる工程;
d.工程cにおいて得られた産物を支持体層上へ積層する工程;および
e.所望により、工程dにおいて得られた産物を、望ましいサイズの経皮デバイスまたはパッチが得られるような方法で切断する工程
を含むことを特徴とする、前記方法。 - 薬物として使用するための、請求項1〜14のいずれか一項に記載のデバイス。
- ニコチン中毒の治療において使用するための、請求項16に記載のデバイス。
- 神経変性疾患の治療において使用するための、請求項16に記載のデバイス。
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FR1251940 | 2012-03-02 | ||
FR1251940A FR2987561B1 (fr) | 2012-03-02 | 2012-03-02 | Dispositif transdermique comprenant des micro-particules poreuses |
PCT/EP2013/054047 WO2013127929A1 (fr) | 2012-03-02 | 2013-02-28 | Dispositif transdermique comprenant des micro-particules poreuses |
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KR20170045225A (ko) * | 2014-08-25 | 2017-04-26 | 헨켈 아이피 앤드 홀딩 게엠베하 | 아크릴 중합체 및 그의 경피 약물 전달에서의 용도 |
ITUB20150555A1 (it) * | 2015-02-12 | 2016-08-12 | Tecres Spa | Miscela ternaria per cemento osseo e metodo per la sua realizzazione |
FR3092838A1 (fr) | 2019-02-14 | 2020-08-21 | Jean-Marc BRUNET | Gel de silicone auto-adherent chargé de microparticules particules à adhésion améliorée |
KR20230068877A (ko) * | 2021-11-11 | 2023-05-18 | 주식회사 아울바이오 | 고용량 바레니클린을 포함하는 미립구 및 이의 제조방법 및 이를 포함하는 약학적 조성물 |
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