JP4315687B2 - カプサイシンを含有する乱用防止薬学的組成物 - Google Patents
カプサイシンを含有する乱用防止薬学的組成物 Download PDFInfo
- Publication number
- JP4315687B2 JP4315687B2 JP2002590972A JP2002590972A JP4315687B2 JP 4315687 B2 JP4315687 B2 JP 4315687B2 JP 2002590972 A JP2002590972 A JP 2002590972A JP 2002590972 A JP2002590972 A JP 2002590972A JP 4315687 B2 JP4315687 B2 JP 4315687B2
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- JP
- Japan
- Prior art keywords
- capsaicin
- composition
- present
- opioid
- abuse
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- YKPUWZUDDOIDPM-SOFGYWHQSA-N capsaicin Chemical compound COC1=CC(CNC(=O)CCCC\C=C\C(C)C)=CC=C1O YKPUWZUDDOIDPM-SOFGYWHQSA-N 0.000 title claims abstract description 258
- 229960002504 capsaicin Drugs 0.000 title claims abstract description 111
- 235000017663 capsaicin Nutrition 0.000 title claims abstract description 111
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- UQCNKQCJZOAFTQ-ISWURRPUSA-N Oxymorphone Chemical compound O([C@H]1C(CC[C@]23O)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O UQCNKQCJZOAFTQ-ISWURRPUSA-N 0.000 claims description 14
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- VQEONGKQWIFHMN-UHFFFAOYSA-N Nordihydrocapsaicin Chemical compound COC1=CC(CNC(=O)CCCCCC(C)C)=CC=C1O VQEONGKQWIFHMN-UHFFFAOYSA-N 0.000 description 4
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Classifications
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- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
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Description
本発明は、乱用を防止するための系を含む薬学的組成物に関する。より具体的には、本発明は、有効量の薬学的化合物およびカプサイシンまたはカプサイシノイド化合物を含む組成物に関する。最も具体的には、本発明は、有効量の薬学的化合物および一定量のカプサイシン化合物を含む組成物であって、所望される場合、経口または皮下により投与される場合に、刺激効果をほとんどまたは全く有さないが、鼻腔内、経口および静脈内の乱用を防止するための組成物に関する。
多くの薬学的化合物の医療的な利益(麻酔薬およびオピオイドならびに非麻酔薬および非オピオイドを含む)は、周知であり、そして明白である。不幸にも、多くのこれらの薬物の乱用および依存性も等しく、明白である。このことは、特に、オピオイドに当てはまる。乱用者は、最も大きな効果を得るために、しばしば、薬物の粉末形態または希釈形態を鼻から吸い込むか、または薬物の溶液を調製し、そしてそれを注射する。いずれにしても、乱用者は、錠剤またはカプセルを簡単に粉砕することによって、処方された錠剤およびカプセル中に依存性物質の容易な供給源を見出し得る。オピオイドは、恐らく、これらの化合物の中で、最も依存性が高く、そして最も乱用される。オピオイドは、本明細書中で使用される場合、任意のオピウム生成物もしくはそのアナログ、または他の薬物を意味し、これらは、医薬として使用することが意図される場合、オピオイドレセプターに作用し、この医薬としては、以下が挙げられるが、これらに限定されない:コデイン、ジヒドロコデイン、ブプレノルフィン、フェンタニル、ヒドロコデン、ヒドロモルホン、レボルファノール、メペリジン、メタドン、モルフィン、ナルブフィン、オキシコデン、オキシモルホン、ペンタゾシン、およびプロポキシフェン、トラマゾール。さらに、乱用される他の医薬としては、以下のクラスの薬物中の医薬が挙げられる:ベンゾアジアザピン(例えば、Valium)、およびNMDA−アンタゴニスト(例えば、ケタミン)。
経口使用が企図される薬学的組成物は、有効成分、カプサイシン、および投薬処方物のために使用される他の物質を含む。この組成物は、好ましくは、固体の経口投薬形態、一般に、錠剤またはカプセルのいずれかの形態である。皮下投与される組成物はまた、本発明の範囲内である。有効な薬学的成分とは別に、この組成物は、組成物の鼻腔内使用、経口使用または静脈内使用に対する防止剤(deterrent)として役立つ量のカプサイシンを含む。このような組成物は、鼻から吸い込むことおよび/または注入による乱用のために処方物の薬学的錠剤を粉砕することによる乱用を防止する。このカプサイシンは、投薬形態に直接的に取り込まれ得るか、またはこのカプサイシンは、その放出を減少または排除するために隔離され得る。さらに、カプサイシンの効果を増強させるさらなる物質が、この錠剤中に含まれ得る。
本発明の組成物は、潜在的に乱用され得る物質の医療的に有効な経口投薬を可能にする一方で、鼻腔内、経口、または静脈内でのそれらの乱用を防止し得る。刺激成分は、鼻から吸入した場合または注入した場合に特に刺激するので、本発明は、固体経口投薬形態(例えば、丸剤、錠剤、カプセルなど)を、当然に含む。本発明はまた、液体充填固体経口投薬形態も含む。なぜならば、これらの形態は、同様に乱用され得るからである。本発明は、錠剤およびカプセルに関する。なぜなら、これらの投薬形態は、後者の使用のために、患者に投与されることが企図されるからである。従って、これらの形態は、乱用のための錠剤となる可能性がより高い。皮下適用がまた、企図される。本質的に、粘膜または他のカプサイシン感受性膜との接触が企図されない全ての投薬形態は、本発明の実施形態に従って作製され得る。静脈内または鼻腔内にこの系を入れるように設計された投薬形態は、本発明に従って処方されるべきではない。
R1は、−NHC(O)−、−NHC(O)O−、−NHC(O)NH−、NHC(S)NH−、−NHS(O2)−、または−C(O)NH−であり;
R2は、直鎖または分枝鎖のC5〜C11アルキル、C11〜C23アルケニル、C11〜C23アルキニル、またはC11〜C23アルカジエニルであり;
R3は、OHまたはC1〜C4エステルであり;そして
R4は、OHまたはOCH3である。
Claims (17)
- オピオイドの乱用を防止するための組成物であって、該組成物は、以下:
該オピオイド;および
カプサイシノイドまたはカプサイシン;
を含み、
該組成物は、固体経口投薬形態または経皮投薬形態として処方されており;そして
該カプサイシノイドまたはカプサイシンは、該組成物が、粘膜または血管膜と接触したとき、咳、くしゃみ、分泌、および疼痛から選択される、少なくとも1つの応答を引き起こすために有効な量で存在する、
組成物。 - 固体経口投薬形態として処方された、請求項1に記載の組成物。
- 前記オピオイドが、オキシコドン、ヒドロモルホン、およびオキシモルホンからなる群より選択される、請求項1または2に記載の組成物。
- 前記オピオイドが、2.5mgで存在し、そして前記カプサイシンが、0.125mg未満で存在する、請求項3に記載の組成物。
- 前記オピオイドが、5.0mgで存在し、そして前記カプサイシンが、0.250mg未満で存在する、請求項3に記載の組成物。
- 前記オピオイドが、10mgで存在し、そして前記カプサイシンが、0.5mg未満で存在する、請求項3に記載の組成物。
- 前記オピオイドが、20mgで存在し、そして前記カプサイシンが、1.0mg未満で存在する、請求項3に記載の組成物。
- 前記オピオイドが、40mgで存在し、そして前記カプサイシンが、2.0mg未満で存在する、請求項3に記載の組成物。
- 前記オキシモルホンが、80mgで存在し、そして前記カプサイシンが、4.0mg未満で存在する、請求項3に記載の組成物。
- 前記組成物が、制御放出処方物である、請求項1に記載の組成物。
- 前記オピオイドが、オキシモルホンである、請求項1に記載の組成物。
- 前記オキシモルホンが、10mgで存在し、そして前記カプサイシンが、0.5mg未満で存在する、請求項11に記載の組成物。
- 前記オキシモルホンが、20mgで存在し、そして前記カプサイシンが、1.0mg未満で存在する、請求項11に記載の組成物。
- 前記オキシモルホンが、40mgで存在し、そして前記カプサイシンが、2.0mg未満で存在する、請求項11に記載の組成物。
- 前記オキシモルホンが、80mgで存在し、そして前記カプサイシンが、4.0mg未満で存在する、請求項11に記載の組成物。
- 前記カプサイシンが、前記オピオイドを含むマトリクス中に直接組み込まれている、請求項1に記載の組成物。
- 前記カプサイシンが、前記オピオイドのマトリクスとは別個の第2のマトリクス中に組み込まれている、請求項1に記載の組成物。
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JP6466417B2 (ja) | 2013-05-29 | 2019-02-06 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | 二峰性放出プロファイルを有する改変防止(tamper−resistant)剤形 |
EA032465B1 (ru) | 2013-07-12 | 2019-05-31 | Грюненталь Гмбх | Защищенная от применения не по назначению пероральная фармацевтическая лекарственная форма, содержащая этиленвинилацетатный полимер, и способ ее изготовления |
AU2014356581C1 (en) | 2013-11-26 | 2020-05-28 | Grunenthal Gmbh | Preparation of a powdery pharmaceutical composition by means of cryo-milling |
JP6510628B2 (ja) | 2014-03-26 | 2019-05-15 | サン・ファーマ・アドバンスト・リサーチ・カンパニー・リミテッド | 乱用防止即時放出性被覆リザーバ固体剤形 |
CN106572980A (zh) | 2014-05-12 | 2017-04-19 | 格吕伦塔尔有限公司 | 包含他喷他多的防篡改即释胶囊制剂 |
CN106456550A (zh) | 2014-05-26 | 2017-02-22 | 格吕伦塔尔有限公司 | 避免乙醇剂量倾泻的多颗粒 |
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AU2016251854A1 (en) | 2015-04-24 | 2017-10-19 | Grunenthal Gmbh | Tamper-resistant dosage form with immediate release and resistance against solvent extraction |
WO2017040607A1 (en) | 2015-08-31 | 2017-03-09 | Acura Pharmaceuticals, Inc. | Methods and compositions for self-regulated release of active pharmaceutical ingredient |
JP2018526414A (ja) | 2015-09-10 | 2018-09-13 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | 乱用抑止性の即放性製剤を用いた経口過剰摂取に対する保護 |
WO2017222575A1 (en) | 2016-06-23 | 2017-12-28 | Collegium Pharmaceutical, Inc. | Process of making more stable abuse-deterrent oral formulations |
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US4599342A (en) * | 1984-01-16 | 1986-07-08 | The Procter & Gamble Company | Pharmaceutical products providing enhanced analgesia |
US4681897A (en) * | 1984-01-16 | 1987-07-21 | The Procter & Gamble Company | Pharmaceutical products providing enhanced analgesia |
US4898887A (en) * | 1984-12-20 | 1990-02-06 | The Procter & Gamble Company | Compounds and compositions having anti-inflammatory and analgesic activity |
US5383848A (en) * | 1990-04-12 | 1995-01-24 | Gensia, Inc. | Iontophoretic administration of drugs |
US5478577A (en) * | 1993-11-23 | 1995-12-26 | Euroceltique, S.A. | Method of treating pain by administering 24 hour oral opioid formulations exhibiting rapid rate of initial rise of plasma drug level |
US5762963A (en) * | 1995-06-07 | 1998-06-09 | Emory University | Method and compositions for controlling oral and pharyngeal pain using capsaicinoids |
US5766623A (en) * | 1996-03-25 | 1998-06-16 | State Of Oregon Acting By And Through The Oregon State Board Of Higher Education On Behalf Of Oregon State University | Compactable self-sealing drug delivery agents |
US7141250B2 (en) * | 2001-08-06 | 2006-11-28 | Euro-Celtique S.A. | Pharmaceutical formulation containing bittering agent |
US7332182B2 (en) * | 2001-08-06 | 2008-02-19 | Purdue Pharma L.P. | Pharmaceutical formulation containing opioid agonist, opioid antagonist and irritant |
US7157103B2 (en) * | 2001-08-06 | 2007-01-02 | Euro-Celtique S.A. | Pharmaceutical formulation containing irritant |
US20030068276A1 (en) * | 2001-09-17 | 2003-04-10 | Lyn Hughes | Dosage forms |
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2002
- 2002-04-08 US US10/118,110 patent/US20030064122A1/en not_active Abandoned
- 2002-05-16 ES ES02736910T patent/ES2321589T3/es not_active Expired - Lifetime
- 2002-05-16 WO PCT/US2002/015553 patent/WO2002094254A2/en active Application Filing
- 2002-05-16 AU AU2002309885A patent/AU2002309885B2/en not_active Ceased
- 2002-05-16 EP EP02736910A patent/EP1392270B1/en not_active Expired - Lifetime
- 2002-05-16 AT AT02736910T patent/ATE423556T1/de not_active IP Right Cessation
- 2002-05-16 CA CA002447807A patent/CA2447807C/en not_active Expired - Fee Related
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- 2002-05-16 JP JP2002590972A patent/JP4315687B2/ja not_active Expired - Fee Related
- 2002-05-16 DE DE60231298T patent/DE60231298D1/de not_active Expired - Fee Related
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EP1392270B1 (en) | 2009-02-25 |
JP2005515153A (ja) | 2005-05-26 |
EP1392270A2 (en) | 2004-03-03 |
JP2009149696A (ja) | 2009-07-09 |
WO2002094254A3 (en) | 2003-03-27 |
CA2447807A1 (en) | 2002-11-28 |
ATE423556T1 (de) | 2009-03-15 |
DE60231298D1 (de) | 2009-04-09 |
AU2002309885B2 (en) | 2007-11-01 |
CA2447807C (en) | 2009-10-13 |
WO2002094254A2 (en) | 2002-11-28 |
US20030064122A1 (en) | 2003-04-03 |
ES2321589T3 (es) | 2009-06-09 |
CN1511030A (zh) | 2004-07-07 |
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