JP2005511653A - ストリキニーネ、ブルシン、セキュリニン、及びそれらの塩の経皮薬物送達システム - Google Patents
ストリキニーネ、ブルシン、セキュリニン、及びそれらの塩の経皮薬物送達システム Download PDFInfo
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Abstract
Description
本発明は、ストリキニーネ、ブルシン、及びセキュリニンの薬理学に関する。
中枢神経麻痺又は末梢神経麻痺、及び神経機能障害に対する治療の為の特効薬が不足している。伝統的な中国人の見地からは、「あらゆる種類の薬物には一定の毒性が有る。」と言われている。伝統的な中国の医学では、難解で複雑な複数の症例に対して治療を行う為に、有毒な植物性薬物(plant drugs)又は鉱物性薬物(mineral drugs)が度々使用され、顕著な治癒効果を挙げている。例えば、馬銭子(Nuxvomica)やヒトツバハギ(securinega suffruticosa)には、上記の疾患を治療する能力が有る。
1.ストリキニーネ、ブルシン、及びセキュリニンの薬理学
本発明に含まれる天然産物は、ストリキニーネ、ブルシン、及びセキュリニンであり、化学構造は、以下の通りである。
過多のストリキニーネ、ブルシン、及びセキュリニンは全て、脊髄反射興奮を有意に亢進させ、それによって強直性痙攣を引き起こし、呼吸筋の強直性収縮に起因する窒息によって死をもたらすことさえ有る。
経皮薬物送達システム(transdermal drug delivery system)は、上記薬物の有毒性の副作用を回避する助けとなるが、問題は、経皮薬物送達システムが同様の治癒効果を奏するように使用できるかどうかである。経皮薬物送達システムの治癒効果と疾患の型との間には、直接的な相関関係が有る。神経学的疾患はウイルス疾患とは異なって、局所神経を刺激することによって治療することができ、前記刺激は、伝統的な中国医学において神経学的疾患に対する治療に用いられる鍼療法や灸療法と同様に、神経伝達を通じて病巣に対して作用する。ストリキニーネ、ブルシン、及びセキュリニンは、神経学的疾患の治療の為の薬物であると共に、人体の局所神経に作用することによって、丁度中国の鍼療法及び灸療法における「艾治療」の様な薬物送達効果を奏することもできる。
中枢性及び末梢性の顔面麻痺に罹患した顔面神経を覆う皮膚で、関係の有る鍼療法のツボ(acupancture points)に、1%ストリキニーネ軟膏を一日一回塗布する。1日から90日継続的にベル麻痺に罹患すると、1日から20日の治療期間を要する。卒中によって引き起こされた顔面麻痺に罹患すると、治療に大体20から40日の継続期間を要する。鍼療法及び灸療法、又は西洋医学を用いるよりも、総有効率(total effective rate)、治癒比(curative ratio)、及び有効率(effective rate)は全て高くなる。疾病期間が7年よりも長い場合でさえ、大変良好な治癒効果を奏した。志願者を伴った外用塗布(external applicatio)試験によって、皮膚のアレルギー反応又は他の副作用が無いことが示された。従って、経皮薬物は安全且つ有効な薬物である。
ストリキニーネ、ブルシン、及びセキュリニンは、それらの塩よりも容易に体内に浸透する。ストリキニーネ、ブルシン、及びセキュリニンは全て、ワセリンに対して一定の溶解性がある。皮膚の水分保持において一定の助長作用があるワセリンは、皮膚に浸透する速度を増大させる助けとなる。ストリキニーネ、ブルシン、及びセキュリニンを軟膏(ointments)又は膏薬(patches)にするのは容易である。
経皮薬物送達システムがより良好な効果を奏する為に、中国の鍼療法や灸療法の技術で選出された鍼療法のツボ(acupuncture point)は推奨に値する。前記の技術では、様々な疾患に基づいて人体の様々な部位又は鍼療法のツボを選択する必要が有る。例えば、顔面麻痺を治療する為には、前記の経皮薬物は風池(Fengchi)、下関(Xiaguan)、太陽(Taiyang)、頬車(Jiache)、及び他の関係の有る鍼療法のツボに外用するべきである。性的障害(sexual disorder)、及び周辺部湿潤不全疾患(peripheral non-cream disease)を治療する為には、前記の経皮薬物は命門(Mingmen)、腎兪(Shenyu)、関元(Guanyuan)、百会(Baihui)、及び他の関係の有る鍼療法のツボに外用するべきである。
前記の経皮薬物は、顔面麻痺、片麻痺、全身麻痺、呼吸筋麻痺、脊髄不完全麻痺、不完全括約筋弛緩(incomplete sphincter relaxation)、陰茎脱、グリーンバーレー症候群(Green-Barley syndrome)、脱肛、周辺部湿潤不全疾患、性的障害(sexual disorder)、灰白髄炎の続発症、重症性筋無力症、及び弱視、乳児障害貧血(postnatal balk anemia)等の中枢又は抹消神経麻痺及び神経機能障害を治療する為に使用することができる。
1.軟膏の調製
[実験1] 2から30mgのストリキニーネと3gのワセリンとを50℃で10分間攪拌し、包装した。
[実験2]ストリキニーネ、ブルシン、又はセキュリニンを含有したワセリンを、周縁部に粘液状接着剤を塗った布片の中心に塗布する。
[産業への利用]
外用製剤は、経口投与又は注射投与よりも有効で、安全で、快適であり、産業製品に利用できる。
Claims (7)
- ストリキニーネ、ブルシン、セキュリニン、及びそれらの塩又はそれらの化合物を個々に含有することを特徴とする経皮薬物送達システム。
- 上記の経皮薬物送達システムは、軟膏、絆創膏、膏薬、エアロゾル、チンキ剤、及び皮膚を介して投与される他の全ての製剤を含むことを特徴とする。
- 上記の経皮薬物送達システムは、ストリキニーネ、ブルシン、セキュリニン、或いはそれらの塩、さらに或いはそれらの混合物を個々に含有することを特徴とする。
- 上記のストリキニーネ、ブルシン、セキュリニンの塩とは、ストリキニーネ、ブルシン、セキュリニンの有機酸塩及び無機酸塩をも含み、前記有機酸及び無機酸は、塩酸、臭化水素酸、硫酸、硝酸、酢酸、酒石酸、マレイン酸、メタンスルホン酸、ベンゼンスルホン酸、アスパラギン酸、及びコレスタノイン酸等を含むことを特徴とする。
- 上記の経皮薬物送達システムには、1−ドデシルアザシクロヘプタン−2−オン、チロン、及びジャコウ等を浸透促進剤として加えてもよいことを特徴とする。
- 上記の経皮薬物送達システムには、抗生物質、抗真菌薬、ビタミン、及び他の薬物を加えてもよいことを特徴とする。
- 上記の塩の経皮薬物送達システムは、顔面麻痺、片麻痺、全身麻痺、呼吸筋麻痺、脊髄不完全麻痺(飽き、不完全括約筋弛緩、陰茎脱、四肢の筋無力症等)、グリーンバーレー症候群、脱肛、周辺部湿潤不全疾患、湿潤不全疾患、性的障害、灰白髄炎の続発症、重症性筋無力症、弱視、及び乳児障害貧血等の神経麻痺又は神経機能異常と、
関節炎、三叉神経痛、眼上神経痛、肩甲骨周辺関節炎、腰部椎間板のプロプラプス、腰部筋肉の繊維組織炎、坐骨神経炎、腰部筋肉の歪み、及び急性腰部捻挫と、
癲癇、統合失調症、眩暈、耳鳴り、及び聾と、
手足の白癬と、の治療に有効であることを特徴とする。
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CN01139894A CN100594027C (zh) | 2001-12-05 | 2001-12-05 | 番木鳖碱、马钱子碱和一叶秋碱及其盐的透皮剂 |
CN01139894.9 | 2001-12-05 | ||
PCT/CN2002/000731 WO2003047554A1 (en) | 2001-12-05 | 2002-10-18 | Transdermal drug delivery system of strychnine, brucine, securinine and their salts |
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JP2005511653A6 JP2005511653A6 (ja) | 2005-09-02 |
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EP (1) | EP1461021A4 (ja) |
JP (1) | JP4445263B2 (ja) |
KR (1) | KR100819220B1 (ja) |
CN (1) | CN100594027C (ja) |
AU (1) | AU2002336886C1 (ja) |
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DE60203726T2 (de) * | 2001-09-20 | 2006-02-09 | Boyle, Frank | Topische zusammensetzung enthaltend brucin und ihre verwendung zur behandlung von hautschäden |
US8835506B2 (en) * | 2008-06-05 | 2014-09-16 | Stc.Unm | Methods and related compositions for the treatment of cancer |
CN101810597B (zh) * | 2010-04-26 | 2012-04-18 | 南京中医药大学 | 一种含马钱子碱的透皮贴剂及其制备方法和其应用 |
CN103059034B (zh) * | 2012-11-19 | 2015-03-25 | 北京大学深圳研究生院 | 一叶萩碱类天然产物flueggine A、norsecurinine、virosaine B及allonorsecurinine的合成方法 |
CN106692113A (zh) * | 2017-02-24 | 2017-05-24 | 湘潭大学 | 一种治疗偏瘫的士的宁经皮贴剂及其制备方法 |
CN114533701B (zh) * | 2020-11-20 | 2023-12-22 | 赛灵药业科技集团股份有限公司 | 一种马钱子碱凝胶贴膏剂及其制备方法和用途 |
CN113599375B (zh) * | 2021-06-21 | 2023-08-18 | 李萍 | 一种治疗口腔疾病的经口给药药物及用途 |
KR20230036054A (ko) * | 2021-09-06 | 2023-03-14 | 서울대학교산학협력단 | 브루신을 포함하는 신경질환 또는 정신질환의 예방 또는 치료용 약학적 조성물 |
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GB845841A (en) * | 1957-12-19 | 1960-08-24 | Friedrich Meyer | Percutaneous administration of physiologically active agents |
US5656286A (en) * | 1988-03-04 | 1997-08-12 | Noven Pharmaceuticals, Inc. | Solubility parameter based drug delivery system and method for altering drug saturation concentration |
US5446070A (en) * | 1991-02-27 | 1995-08-29 | Nover Pharmaceuticals, Inc. | Compositions and methods for topical administration of pharmaceutically active agents |
US5747021A (en) * | 1997-01-10 | 1998-05-05 | Mckenzie; Therman | After shave treatment composition |
US6277884B1 (en) * | 1998-06-01 | 2001-08-21 | Nitromed, Inc. | Treatment of sexual dysfunction with N-hydroxyguanidine compounds |
DE60203726T2 (de) * | 2001-09-20 | 2006-02-09 | Boyle, Frank | Topische zusammensetzung enthaltend brucin und ihre verwendung zur behandlung von hautschäden |
DE60330698D1 (de) * | 2002-08-28 | 2010-02-04 | Lupin Ltd | Kräuterextrakt aus sapindus trifoliatus, enthaltend eine mischung aus saponinen mit krampflösender wirkung |
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2001
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- 2002-10-18 US US10/496,309 patent/US20050019378A1/en not_active Abandoned
- 2002-10-18 WO PCT/CN2002/000731 patent/WO2003047554A1/en active Application Filing
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JP2014094942A (ja) * | 2008-03-14 | 2014-05-22 | Basf Beauty Care Solutions France Sas | 免疫細胞の活性化閾値を上昇させる物質 |
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AU2002336886C1 (en) | 2011-03-17 |
EP1461021A4 (en) | 2009-10-21 |
KR100819220B1 (ko) | 2008-04-02 |
CN1355021A (zh) | 2002-06-26 |
CA2465349A1 (en) | 2003-06-12 |
CN100594027C (zh) | 2010-03-17 |
JP4445263B2 (ja) | 2010-04-07 |
WO2003047554A1 (en) | 2003-06-12 |
CA2465349C (en) | 2009-12-29 |
AU2002336886A1 (en) | 2003-06-17 |
KR20040062982A (ko) | 2004-07-09 |
EP1461021A1 (en) | 2004-09-29 |
AU2002336886B2 (en) | 2009-02-05 |
US20050019378A1 (en) | 2005-01-27 |
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