JP2007510655A - バイオアベイラビリティーエンハンサを含む第四級アンモニウム化合物の組成物 - Google Patents
バイオアベイラビリティーエンハンサを含む第四級アンモニウム化合物の組成物 Download PDFInfo
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
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- A61K31/00—Medicinal preparations containing organic active ingredients
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
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- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
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- A61K9/5078—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings with drug-free core
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5084—Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
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Abstract
Description
本発明は、バイオアベイラビリティーエンハンサ(bioavailability enhancer)を含む第四級アンモニウム化合物の組成物に関する。
胃腸管の管腔からの第四級アンモニウム化合物の比較的乏しい吸収は、実際、治療におけるそれらの有用性を制限する。高用量が与えられることまたは代替的な投与経路が探求されることがしばしば要求される。当然、高用量は、ほぼいつも所望されない副作用を伴う。
本発明は、薬理学的に活性な第四級アンモニウムまたは他の制限された透過性/バイオアベイラビリティーを有する恒久的に荷電した分子の透過性/バイオアベイラビリティー増強を提供する。胃腸管(消化管(gut)としても知られている)の上皮層を通る透過性は、薬物吸収において重要なステップである。他のステップとしては消化管表面に並ぶ粘膜層を通る透過、消化管腔及び消化管壁における代謝が挙げられる。バイオアベイラビリティーは、生理学的システムにおける薬物のアベイラビリティーとして定性的に規定される。第四級アンモニウム化合物のような薬物に関して、薬物吸収のプロセスにおいて最も重要なステップは、上皮障壁を通る薬物の透過である。従って、そのような薬物の透過性を増強することは直接的にこれらのバイオアベイラビリティーを増加することと言い換えることができる。
透過性増強賦形剤のCaco-2細胞スクリーニング
1%濃度までの透過性増強賦形剤溶液を、ハンクス平衡塩類溶液(HBSS)、pH7.4中に調製し、そして一晩攪拌した。これらの溶液を、0.45mm Teflon (登録商標)Acrodisc filterを用いて濾過した。塩化トロスピウム(16mg/ml)のストック溶液をHBSS中に調製し、賦形剤溶液中へ160ug/mlまで希釈し、一晩攪拌した。Caco-2細胞株の透過性試験を3連で実施した。Caco-2モノレイヤーの完全性を、細胞毒性アッセイを用いる実験後にモニターした。図1に示されるように、有機酸を含む複数の製剤が、トロスピウムの透過性を予想外に有意に増強させた。
薬物(単数または複数)及び増強賦形剤を含む製剤の調製ならびに溶解媒体中での薬物及び増強賦形剤の放出パターン
商業的供給者から購入した不規則なクエン酸顆粒を、流動層コーター造粒機において、1:5の薬物:クエン酸比で、トロスピウムを用いてコートした。第一に不規則な形状のクエン酸顆粒を、Eudragit(登録商標)L30-55を用いて5%の重量増加までコートし、引き続きOpadry(登録商標)whiteを用いて2%の重量増加までコートした。次いで、得られる顆粒を、結合剤としてHPMC E5(1.15%)を含む塩化トロスピウム(17.7%)溶液から塩化トロスピウムでコートした。次いで、これらの顆粒を、Eudragit(登録商標)L30D55、引き続きOpadry(登録商標)Whiteを用いて、夫々、40%及び2%の重量増加までコートした。これらの顆粒は、最後のコーティングが適用された後、これらの不規則な形状を維持していた。図2は、最初の2時間について希HCl、pH1.1、引き続きリン酸緩衝液(pH6.8)中で得られる平均溶解プロフィールを提供する。
トロスピウムコートされたクエン酸顆粒を、実施例2と同一の方法で製造した。次いで、これらの顆粒を、Eudragit(登録商標)FS30D、引き続きOpadry(登録商標)whiteで、夫々40%及び2%の重量増加までコートした。図3は、平均溶解プロフィールを提供する。
腸溶性ポリマーで40%の重量増加までコートされた別個の活性ペレット及びエンハンサペレット
クエン酸顆粒及び活性剤ペレット(トロスピウム層形成されたシュガースフィア)を、別個に、Eudragit(登録商標)L30D-55L、引き続きOpadryを用いて、夫々、40%及び2%重量増加までコートした。トロスピウム層形成されたシュガースフィア(活性剤ペレット)を、Glatt’s流動層プロセッサにおいて、市販の糖球体を塩化トロスピウム溶液でコートすることによって製造する。コートされた活性剤及びエンハンサのペレットを、カプセル中で合わせ、そしてクエン酸及びトロスピウム両方の溶解について試験した。図4は、クエン酸及びトロスピウムについての平均溶解プロフィールを示す。
Claims (11)
- 有機酸と共に治療用第四級アンモニウム化合物を含む、増強された胃腸透過性を有する経口医薬剤形。
- 前記有機酸が短鎖有機酸である、請求項1に記載の剤形。
- 前記短鎖有機酸がクエン酸である、請求項2に記載の剤形。
- 前記第四級アンモニウム化合物がクリジニウム、グリコピロレート、プロパンテリン、またはトロスピウムである、請求項1に記載の剤形。
- 前記第四級アンモニウム化合物が塩化トロスピウムである、請求項4に記載の剤形。
- その分子中に電気陰性エレメントを有する少なくとも1つのポリマーをさらに含む、請求項1に記載の剤形。
- 前記少なくとも1つのポリマーがセルロース系ポリマー(cellulosic polymer)、アルギネート、ガム類、ポリアクリル酸誘導体、ポビドン及びその誘導体、ポリエチレンオキシド、またはポリビニルアルコールから選択される、請求項6に記載の剤形。
- 前記少なくとも1つのポリマーが、グアーガム、キサンタンがム、カルボマー、カラギーナン、またはクロスポビドン(crospovidone)から選択される、請求項7に記載の剤形。
- 前記少なくとも1つのポリマーが、ヒドロキシプロピルメチルセルロース(HPMC)、ヒドロキシプロピルセルロース(HPC)、ヒドロキシエチルセルロース(HEC)、メチルセルロース(MC)、粉末セルロース、セルロースアセテート、カルボキシメチルセルロースナトリウム、カルボキシメチルセルロースのカルシウム塩、またはエチルセルロースから選択される、請求項7に記載の剤形。
- 前記少なくとも1つのポリマーがHPMCである、請求項9に記載の剤形。
- 治療用第四級アンモニウム化合物の層により包まれた透過性増強剤の顆粒状コアを含み、その全体が腸溶性または非腸溶性ポリマーコーティングにより包まれている、剤形。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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US51719603P | 2003-11-04 | 2003-11-04 | |
US60/517,196 | 2003-11-04 | ||
PCT/US2004/036393 WO2005046663A1 (en) | 2003-11-04 | 2004-11-04 | Compositions of quaternary ammonium containing bioavailability enhancers |
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JP2007510655A true JP2007510655A (ja) | 2007-04-26 |
JP4771956B2 JP4771956B2 (ja) | 2011-09-14 |
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JP2006538424A Expired - Fee Related JP4771956B2 (ja) | 2003-11-04 | 2004-11-04 | バイオアベイラビリティーエンハンサを含む第四級アンモニウム化合物の組成物 |
Country Status (6)
Country | Link |
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US (1) | US8709476B2 (ja) |
EP (1) | EP1680100A4 (ja) |
JP (1) | JP4771956B2 (ja) |
AU (1) | AU2004289222B2 (ja) |
CA (1) | CA2536401C (ja) |
WO (1) | WO2005046663A1 (ja) |
Cited By (1)
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- 2004-11-04 US US10/980,819 patent/US8709476B2/en not_active Expired - Fee Related
- 2004-11-04 CA CA2536401A patent/CA2536401C/en not_active Expired - Fee Related
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JP2015511241A (ja) * | 2012-02-21 | 2015-04-16 | ラボラトリオス・デル・ドクトル・エステベ・ソシエダッド・アノニマ | ダビガトランエテキシラートの経口医薬組成物 |
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Also Published As
Publication number | Publication date |
---|---|
CA2536401A1 (en) | 2005-05-26 |
EP1680100A4 (en) | 2012-08-08 |
WO2005046663A1 (en) | 2005-05-26 |
AU2004289222A1 (en) | 2005-05-26 |
JP4771956B2 (ja) | 2011-09-14 |
EP1680100A1 (en) | 2006-07-19 |
US20050123606A1 (en) | 2005-06-09 |
US8709476B2 (en) | 2014-04-29 |
AU2004289222B2 (en) | 2010-01-21 |
CA2536401C (en) | 2011-08-30 |
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