JP2021166744A - 化学療法剤の多段階放出のための組成物、装置、および方法 - Google Patents
化学療法剤の多段階放出のための組成物、装置、および方法 Download PDFInfo
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Abstract
【解決手段】一態様において、本願は、第一期間にわたって第一薬剤を放出するとともに、第二期間にわたって第二薬剤を放出するように構成された微粒子であって、第一期間と第二期間との間に、薬剤を実質的に放出しない遅延期間が生じる微粒子を提供する。別の態様において、本願は、送達システムおよび治療方法における、このような微粒子の使用に関する。別の態様において、本願は、折り込みと、その折り込み内に配置された微粒子とを含む、折り込まれた膨張性薬剤送達用のバルーンを含む薬剤送達システムに関する。
【選択図】 なし
Description
上記態様および実施形態のいずれかと組み合わせ可能な特定の実施形態において、遅延期間は2〜6週間の範囲であってもよい。
上記態様および実施形態のいずれかと組み合わせ可能な特定の実施形態において、微粒子からの総累積薬剤放出の30〜70%が第一期間にわたって生じること、微粒子からの総累積薬剤放出の30〜70%が第二期間にわたって生じること、および総累積薬剤放出の5%未満、より好適には1%未満が遅延期間にわたって生じることの少なくとも一つが生じる。
本願の態様は、同様の参照番号が同様の要素を参照する以下の図面を参照して説明される。
本明細書で使用される「AおよびBの少なくとも一方(and/or)」という語句は、そのように組み合わされた要素、すなわち、ある場合には組み合わされて存在し、他の場合には離接的に存在する要素の「一方または両方」を意味するものと理解されるべきである。「AおよびBの少なくとも一方(and/or)」という語句によって具体的に特定される要素以外の要素は、明確に反対の指示がされない限り、具体的に特定される要素と関連しているか否かにかかわらず、必要に応じて存在していてもよい。従って、非限定的な例として、「AおよびBの少なくとも一方(and/or)」という語句は、「〜を含む(comprising)」等の非限定的な語句と併せて使用される場合、一実施形態において、Aを含むがBを含まない(必要に応じてB以外の要素を含む)ということを表し、別の実施形態において、Bを含むがAを含まない(必要に応じてA以外の要素を含む)ということを表し、さらに別の実施形態において、AおよびBの両方を含む(必要に応じて他の要素を含む)ということを表すこと等が可能である。
抗癌剤の例には、(a)ドキソルビシン、ダウノルビシン、エピルビシン、イダルビシン、ピラルビシン、アクラルビシン、およびミトキサントロン、ならびにアクチノマイシン、ブレオマイシン、プリカマイシン、マイトマイシン等のアントラサイクリンを含む抗悪性腫瘍性抗生物質、(b)ナイトロジェンマスタード(例えば、メクロレタミン、シクロホスファミド、メルファラン、クロラムブシル、イホスファミド、ブスルファン等)、ニトロソウレア(例えば、N−ニトロソ−N−メチル尿素、カルムスチン、ロムスチネム、セムスチン、フォテムスチン、ストレプトゾトシン等)、テトラジン(例えば、ダカルバジン、ミトゾロミド、テモゾロマイド等)、アジリジン(例えば、チオテパ、マイトマイシン、ジアジノン等)、シスプラチンおよび誘導体(例えば、シスプラチン、カルボプラチン、オキサリプラチン等を含む)、および非古典的アルキル化剤(例えば、プロカルバジンおよびヘキサメチルメラミン等)を含むアルキル化剤、(c)葉酸代謝拮抗剤(例えば、メトトレキセート、ペメトレキセド等)、フルオロピリミジン(例えば、5−フルオロウラシル、カペシタビン等)、デオキシヌクレオシド類似体(例えば、シタラビン、ゲムシタビン、デシタビン、ビダザ、フルダラビン、ネララビン、クラドリビン、クロファラビン、ペントスタチン等)、およびチオプリン(例えば、チオグアニン、メルカプトプリン等)を含む代謝拮抗物質、(d)トポイソメラーゼI阻害剤(例えば、イリノテカン、トポテカン、カンプトテシン等)、およびトポイソメラーゼII阻害剤(例えば、エトポシド、ドキソルビシン、ミトキサントロン、テニポシド、ノボビオシン、メルバロン、アクラルビシン等)を含むトポイソメラーゼ阻害剤、および(e)ビンカアルカロイド(例えば、ビンクリスチン、ビンブラスチン、ビノレルビン、ビンデシン、ビンフルニン等)、およびタキサン(例えば、パクリタキセル、ドセタキセル等)を含む微小管阻害剤、ポドフィロトキシン、エトポシド、およびテニポシドが含まれる。
第一期間、第二期間、および遅延期間は、実施形態によって大幅に変わる場合がある。いくつかの実施形態では、第一薬剤が放出される第一期間は、5日以内である。いくつかの実施形態では、第二薬剤が放出される第二期間は、5日以内である。いくつかの実施形態では、第一期間と第二期間との間の遅延期間は、2〜6週間、より典型的には3〜5週間、さらにより典型的には約4週間の範囲である。
バルーンを形成するのに適した材料には、例えばポリエーテルブロックアミド(例えば、PEBAX(登録商標))、ポリエチレンテレフタレート、ナイロン、およびポリウレタン等が含まれる。
Claims (1)
- 対象の体内の栄養動脈に微粒子を放出するように構成された送達装置と、
第一期間にわたって第一薬剤を放出するとともに、第二期間にわたって第二薬剤を放出するように構成された微粒子と、を含み、
前記第一期間と前記第二期間との間に、薬剤を実質的に放出しない遅延期間が生じ、
前記第一薬剤および前記第二薬剤は同一であっても異なっていてもよい送達システム。
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