JP5695562B2 - 安定化された経皮薬物送達システム - Google Patents
安定化された経皮薬物送達システム Download PDFInfo
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- JP5695562B2 JP5695562B2 JP2011511876A JP2011511876A JP5695562B2 JP 5695562 B2 JP5695562 B2 JP 5695562B2 JP 2011511876 A JP2011511876 A JP 2011511876A JP 2011511876 A JP2011511876 A JP 2011511876A JP 5695562 B2 JP5695562 B2 JP 5695562B2
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Description
以下に、出願時の特許請求の範囲の記載を示す。
[請求項1]
経皮薬物送達デバイスであって、
(a)支持フィルムと;
(b)第一の接着剤、
第一のアモルファス形の治療薬、及び
水素結合形成官能基を含む第一の兼用(combination)ポリマー性安定及び分散
剤
を含む固体分散物を含む第一の接着剤層と;
(c)保護用剥離ライナーと
を含む経皮薬物送達デバイス。
[請求項2]
前記ポリマー性安定/分散剤対前記アモルファス形の治療薬の重量比が少なくとも0.5である、請求項1に記載の薬物送達デバイス。
[請求項3]
前記治療薬の少なくとも95%が、室温で少なくとも6ヶ月間の貯蔵後にアモルファス形である、請求項1に記載の薬物送達デバイス。
[請求項4]
前記治療薬の少なくとも99%が、室温で少なくとも6ヶ月間の貯蔵後にアモルファス形である、請求項3に記載の薬物送達デバイス。
[請求項5]
前記治療薬の少なくとも99%が、室温で少なくとも18ヶ月間の貯蔵後にアモルファス形である、請求項4に記載の薬物送達デバイス。
[請求項6]
前記治療薬が、前記ポリマー性安定/分散剤を含まない同一の経皮薬物送達物中の前記治療薬の皮膚吸収速度に比べて、少なくとも50%増大した皮膚吸収速度を有する、請求項1に記載の薬物送達デバイス。
[請求項7]
前記治療薬が、(i)スコポラミン、オキシブチニン、ナルトレキソン、テストステロン、エストラジオール、ロチゴチン、フェンタニル、エチニルエストラジオール、又はノルエルゲストラール(norelgestral)、(ii)(i)のいずれかのものの製薬学的に許容しうる塩、又は(i)、(ii)、又は(i)及び(ii)のいずれかのものの組合せからなる群から選ばれる、請求項1に記載の薬物送達デバイス。
[請求項8]
(d)前記第一の接着剤層と前記保護用剥離ライナーとの間に第二の接着剤層をさらに含み、前記第二の接着剤層は、
前記第一の接着剤と同じでも異なっていてもよい第二の接着剤、前記第一の治療薬と同じでも異なっていてもよい第二のアモルファス形の治療薬、及び
水素結合形成官能基を含む、前記第一の兼用ポリマー性安定及び分散剤と同じでも異なっていてもよい第二の兼用ポリマー性安定及び分散剤
を含む、請求項1に記載の経皮薬物送達デバイス。
[請求項9]
(e)前記第一及び第二の接着剤層の間に膜
をさらに含む、請求項8に記載の薬物送達デバイス。
[請求項10]
前記第一の接着剤層が、皮膚浸透増強剤、粘着付与剤、凝集促進剤、及び前述のいずれかのものの組合せからなる群から選ばれるメンバーをさらに含む、請求項1に記載の薬物送達デバイス。
[請求項11]
前記第一、第二、又は第一及び第二の接着剤層が、独立して、皮膚浸透増強剤、粘着付
与剤、凝集促進剤、及び前述のいずれかのものの組合せからなる群から選ばれるメンバーをさらに含む、請求項8に記載の薬物送達デバイス。
[請求項12]
前記アモルファス形の治療薬が少なくとも一つの水素結合形成基を含有する、請求項1に記載の薬物送達デバイス。
[請求項13]
前記アモルファス形の治療薬と前記ポリマー性安定/分散剤との間に一つ又は複数の水素結合があり、前記薬物送達デバイスは、前記ポリマー性安定/分散剤を含まない同一の経皮薬物送達デバイスと比べてより大きい分散能力を有する、請求項12に記載の薬物送達デバイス。
[請求項14]
ポリマー性安定/分散剤対アモルファス形の治療薬の重量比が0.5以上である、請求項1に記載の薬物送達デバイス。
[請求項15]
前記ポリマー性安定剤対前記アモルファス形の治療薬の重量比が2以上であり、前記アモルファス形の治療薬が50℃未満のガラス転移温度を有する、請求項1に記載の薬物送達デバイス。
[請求項16]
ポリマー性安定剤対アモルファス形の治療薬の重量比が2〜10であり、前記アモルファス形の治療薬が40℃未満のガラス転移温度を有する、請求項15に記載の薬物送達デバイス。
[請求項17]
前記ポリマー性安定剤対前記アモルファス形の治療薬の重量比が0.5以上であり、前記アモルファス形の治療薬が少なくとも60℃のガラス転移温度を有する、請求項1に記載の薬物送達デバイス。
[請求項18]
前記ポリマー性安定剤対前記アモルファス形の治療薬の重量比が0.5〜10であり、前記アモルファス形の治療薬が少なくとも70℃のガラス転移温度を有する、請求項17に記載の薬物送達デバイス。
[請求項19]
前記ポリマー性安定剤対前記アモルファス形の治療薬の重量比が0.5〜2である、請求項18に記載の薬物送達デバイス。
[請求項20]
前記アモルファス形の治療薬が1.0%未満の結晶化度を含有する、請求項1に記載の薬物送達デバイス。
[請求項21]
前記接着剤層が約0.05〜約40重量%の前記治療薬を含む、請求項1に記載の薬物送達デバイス。
[請求項22]
前記接着剤層が約1〜約20重量%の前記アモルファス形の治療薬を含む、請求項1に記載の薬物送達デバイス。
[請求項23]
前記接着剤が、ポリシロキサン、ポリイソブチレン、アクリル系接着剤、又は前述のいずれかのものの組合せからなる群から選ばれる、請求項1に記載の薬物送達デバイス。
[請求項24]
経皮薬物送達デバイスの製造法であって、前記方法は、
(a)(i)第一のアモルファス形の治療薬、及び水素結合形成官能基を含む第一の兼用ポリマー性安定及び分散剤を含む第一の均一溶液を、
(ii)第一の接着剤又は接着剤溶液と
混合して、第二の溶液又は懸濁液を形成し、
(b)剥離ライナーを前記第二の溶液又は懸濁液でコーティングして第一の被覆剥離ライナーを形成し、そして
(c)前記第一の被覆剥離ライナーを乾燥させる
ことを含む方法。
[請求項25]
(d)前記乾燥被覆剥離ライナーを支持フィルム上にラミネートする
ステップをさらに含む、請求項24に記載の方法。
[請求項26]
(e)前記ラミネートから一つ又は複数の単位剤形を打ち抜く
ステップをさらに含む、請求項24に記載の方法。
[請求項27]
前記均一溶液、接着剤、接着剤溶液、第二の溶液又は懸濁液の一つ又は複数が、独立して、皮膚浸透増強剤、粘着付与剤、凝集促進剤、又は前述のいずれかのものの組合せからなる群から選ばれるメンバーをさらに含む、請求項24に記載の方法。
[請求項28]
(a’)(i)前記第一の治療薬と同じでも異なっていてもよい第二のアモルファス形の治療薬、及び水素結合形成官能基を含む、前記第一の兼用安定及び分散剤と同じでも異なっていてもよい第二の兼用ポリマー性安定及び分散剤を含む第二の均一溶液を、
(ii)前記第一の接着剤又は接着剤溶液と同じでも異なっていてもよい第二の接着剤又は接着剤溶液と
混合して、第三の溶液又は懸濁液を形成し、
(b’)前記第一の剥離ライナーと同じでも異なっていてもよい第二の剥離ライナーを前記第三の溶液又は懸濁液でコーティングし、
(c’)第二の被覆剥離ライナーを乾燥させ、
(d)第一の乾燥被覆剥離ライナーを支持フィルム上にラミネートし、
(e)前記第一の剥離ライナーを前記第一の被覆剥離ライナーから除去して第一の乾燥コーティング層を形成し、そして
(f)第二の乾燥被覆剥離ライナーを前記第一の乾燥コーティング層にラミネートすることをさらに含む、請求項24に記載の方法。
[請求項29]
前記第一の均一溶液、第一の接着剤又は接着剤溶液、第二の溶液又は懸濁液、第二の均一溶液、第二の接着剤又は接着剤溶液、又は第三の溶液又は懸濁液の一つ又は複数が、独立して、皮膚浸透増強剤、粘着付与剤、凝集促進剤、及び前述のいずれかのものの組合せからなる群から選ばれるメンバーをさらに含む、請求項28に記載の方法。
[請求項30]
(a’)(i)前記第一の治療薬と同じでも異なっていてもよい第二のアモルファス形の治療薬、及び水素結合形成官能基を含む、前記第一の兼用安定及び分散剤と同じでも異なっていてもよい第二の兼用ポリマー性安定及び分散剤を含む第二の均一溶液を、
(ii)前記第一の接着剤又は接着剤溶液と同じでも異なっていてもよい第二の接着剤又は接着剤溶液と
混合して、第三の溶液又は懸濁液を形成し、
(b’)前記第一の剥離ライナーと同じでも異なっていてもよい第二の剥離ライナーを前記第三の溶液又は懸濁液でコーティングし、
(c’)第二の被覆剥離ライナーを乾燥させ、
(d)第一の乾燥被覆剥離ライナーを、膜、織りメッシュ、又は不織メッシュの一つの側にラミネートし、そして
(e)第二の乾燥被覆剥離ライナーを、前記膜、織りメッシュ、又は不織メッシュの第二の側にラミネートする
ことをさらに含む、請求項24に記載の方法。
[請求項31]
ステップ(d)及び(e)が同時に行われる、請求項30に記載の方法。
[請求項32]
ステップ(d)がステップ(e)の前に行われる、請求項30に記載の方法。
[請求項33]
前記第一の均一溶液、第一の接着剤又は接着剤溶液、第二の溶液又は懸濁液、第二の均一溶液、第二の接着剤又は接着剤溶液、又は第三の溶液又は懸濁液の一つ又は複数が、独立して、皮膚浸透増強剤、粘着付与剤、凝集促進剤、及び前述のいずれかのものの組合せからなる群から選ばれるメンバーをさらに含む、請求項30に記載の方法。
11 支持層
12 接着剤層
13 保護用剥離ライナー
20 四層の経皮送達デバイス
21 支持層
22 薬物レザバー層
23 皮膚接触層
24 保護用剥離ライナー
30 五層の経皮送達デバイス
31 支持層
32 薬物レザバー層
33 膜
34 皮膚接触層
35 保護用剥離ライナー
Claims (14)
- 経皮薬物送達デバイスであって、
(a)支持フィルムと;
(b)第一の接着剤層であって、
第一の接着剤、
第一のアモルファス形の治療薬、及び
水素結合形成官能基を含む第一の兼用(combination)ポリマー性安定及び分散剤からなる固体分散物である、当該第一の接着剤層と;
(c)保護用剥離ライナーと
からなり、
当該第一の兼用ポリマー性安定及び分散剤がポリビニルピロリドンであり、
ここで、
(i)当該第一のアモルファス形の治療薬が少なくとも70℃のガラス転移温度を有し、当該ポリマー性安定及び分散剤対当該第一のアモルファス形の治療薬の重量比が0.5〜2である;又は、
(ii)当該第一のアモルファス形の治療薬が40℃未満のガラス転移温度を有し、当該ポリマー性安定及び分散剤対当該第一の治療薬の重量比が2〜10であり、
ここで、
当該少なくとも70℃のガラス転移温度を有する第一のアモルファス形の治療薬がナルトレキソンであり、
当該40℃未満のガラス転移温度を有する第一のアモルファス形の治療薬がスコポラミンである、
前記経皮薬物送達デバイス。 - 前記治療薬の少なくとも95%が、室温で少なくとも6ヶ月間の貯蔵後にアモルファス形である、請求項1に記載の薬物送達デバイス。
- 前記治療薬の少なくとも99%が、室温で少なくとも6ヶ月間の貯蔵後にアモルファス形である、請求項2に記載の薬物送達デバイス。
- 前記治療薬の少なくとも99%が、室温で少なくとも18ヶ月間の貯蔵後にアモルファス形である、請求項3に記載の薬物送達デバイス。
- 前記治療薬が、前記ポリマー性安定及び分散剤を含まない同一の経皮薬物送達物中の前記治療薬の皮膚吸収速度に比べて、少なくとも50%増大した皮膚吸収速度を有する、請求項1に記載の薬物送達デバイス。
- 前記アモルファス形の治療薬が少なくとも一つの水素結合形成基を含有する、請求項1に記載の薬物送達デバイス。
- 前記アモルファス形の治療薬と前記ポリマー性安定及び分散剤との間に一つ又は複数の水素結合があり、前記薬物送達デバイスは、前記ポリマー性安定及び分散剤を含まない同一の経皮薬物送達デバイスと比べてより大きい分散能力を有する、請求項6に記載の薬物送達デバイス。
- 前記アモルファス形の治療薬が1.0%未満の結晶化度を含有する、請求項1に記載の薬物送達デバイス。
- 前記接着剤層が0.05〜40重量%の前記治療薬を含む、請求項1に記載の薬物送達デバイス。
- 前記接着剤層が1〜20重量%の前記アモルファス形の治療薬を含む、請求項1に記載の薬物送達デバイス。
- 前記接着剤が、ポリシロキサン、ポリイソブチレン、アクリル系接着剤、又は前述のいずれかのものの組合せからなる群から選ばれる、請求項1に記載の薬物送達デバイス。
- 請求項1に記載の経皮薬物送達デバイスの製造法であって、前記方法は、
(a)(i)第一のアモルファス形の治療薬、及び水素結合形成官能基を含む第一の兼用ポリマー性安定及び分散剤を含む第一の均一溶液を、
(ii)第一の接着剤又は接着剤溶液と
混合して、第二の溶液又は懸濁液を形成し、
(b)剥離ライナーを前記第二の溶液又は懸濁液でコーティングして第一の被覆剥離ライナーを形成し、そして
(c)前記第一の被覆剥離ライナーを乾燥させる
ことを含み、
当該第一の兼用ポリマー性安定及び分散剤がポリビニルピロリドンであり、
ここで、
(i)当該第一のアモルファス形の治療薬が少なくとも70℃のガラス転移温度を有し、及び、当該ポリマー性安定及び分散剤対当該第一のアモルファス形の治療薬の重量比が0.5〜2である;又は、
(ii)当該第一のアモルファス形の治療薬が40℃未満のガラス転移温度を有し、及び、当該ポリマー性安定及び分散剤対当該第一の治療薬の重量比が2〜10であり、
ここで、
当該少なくとも70℃のガラス転移温度を有する第一のアモルファス形の治療薬がナルトレキソンであり、
当該40℃未満のガラス転移温度を有する第一のアモルファス形の治療薬がスコポラミンである、
前記方法。 - (d)前記乾燥被覆剥離ライナーを支持フィルム上にラミネートする
ステップをさらに含む、請求項12に記載の方法。 - (e)前記ラミネートから一つ又は複数の単位剤形を打ち抜く
ステップをさらに含む、請求項12に記載の方法。
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2015083569A (ja) * | 2008-05-30 | 2015-04-30 | マイラン・インコーポレーテッド | 安定化された経皮薬物送達システム |
WO2020189323A1 (ja) | 2019-03-19 | 2020-09-24 | ノーベルファーマ株式会社 | 薬物の生体への吸収性に優れ、且つ、化学的安定性にも優れる医薬組成物 |
Also Published As
Publication number | Publication date |
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CA2726136C (en) | 2016-11-01 |
KR101590209B1 (ko) | 2016-02-01 |
BRPI0913214A2 (pt) | 2016-01-19 |
WO2009158120A3 (en) | 2010-03-04 |
CN102099020B (zh) | 2013-09-18 |
EP2299989A4 (en) | 2013-11-13 |
MX2010012989A (es) | 2011-04-27 |
AU2016202212B2 (en) | 2018-05-10 |
AU2009262871A1 (en) | 2009-12-30 |
WO2009158120A2 (en) | 2009-12-30 |
CN102099020A (zh) | 2011-06-15 |
US20090299304A1 (en) | 2009-12-03 |
EP2299989A2 (en) | 2011-03-30 |
JP2011521974A (ja) | 2011-07-28 |
JP2015083569A (ja) | 2015-04-30 |
US9226902B2 (en) | 2016-01-05 |
EP2299989B1 (en) | 2019-01-02 |
BRPI0913214B1 (pt) | 2022-05-17 |
US20110182949A1 (en) | 2011-07-28 |
AU2016202212A1 (en) | 2016-05-12 |
KR20110025931A (ko) | 2011-03-14 |
NZ589542A (en) | 2012-10-26 |
AU2009262871B2 (en) | 2016-04-14 |
CA2726136A1 (en) | 2009-12-30 |
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