JP2007513960A - 作用薬及び逆作用薬を含有する不正使用防止共押出剤型、及びその製造方法 - Google Patents
作用薬及び逆作用薬を含有する不正使用防止共押出剤型、及びその製造方法 Download PDFInfo
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- JP2007513960A JP2007513960A JP2006543959A JP2006543959A JP2007513960A JP 2007513960 A JP2007513960 A JP 2007513960A JP 2006543959 A JP2006543959 A JP 2006543959A JP 2006543959 A JP2006543959 A JP 2006543959A JP 2007513960 A JP2007513960 A JP 2007513960A
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- A—HUMAN NECESSITIES
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Abstract
【選択図】図1
Description
定義
何らかの薬剤、例えば作用薬、逆作用薬、オピオイドアゴニスト又はオピオイドアンタゴニストへのここでの言及は、特に異なる記述がない限り、そのような薬剤の製薬上許容されうる形態、例えば遊離形態、製薬上許容されうる塩形態、製薬上許容されうる塩基形態、製薬上許容されうる水和物、製薬上許容されうる溶媒和物、立体異性体、光学異性体、更にそのような薬剤のプロドラッグとそのような薬剤の製薬上活性な類似体、及び前記のいずれか2つ以上の混合物を包含するものとする。
作用薬と逆作用薬とを含有する共押出剤型
作用薬
逆作用薬
コア
シース
シェル
共押出工程
投与方法
投与単位当たりの量
膣又は直腸投与のための方法
キット
実施例
実施例1は、オピオイドアンタゴニストを含有するコア、シース、及びオピオイドアゴニストを含有するシェルを含む粒子の溶融共押出による製造に適するはずである工程の机上の実施例を説明する。作用薬は塩酸ヒドロモルフォンであり、隔離されたオピオイドアンタゴニストは塩酸ナルトレキソンである。コアの上部と底部は、いかなるヒドロモルフォン又はナルトレキソンも含まないシースによって覆われる。コア押出機、シース押出機及びシェル押出機への供給材料の製剤を表1に示す。
Claims (65)
- 逆作用薬を含有するコア、及び作用薬を含有するシェルを含み、前記シェルが前記コアを少なくとも部分的に取り囲んでなる、共押出剤型。
- 前記コアがさらに疎水性物質を含有する、請求項1記載の共押出剤型。
- 前記シェルが前記コアの大部分を取り囲んでなる、請求項2記載の共押出剤型。
- 前記シェルがさらに疎水性物質を含有する、請求項3記載の共押出剤型。
- 前記作用薬がオピオイドアゴニストであり、前記逆作用薬がオピオイドアンタゴニストである、請求項1記載の共押出剤型。
- 前記剤型が経口投与剤型である、請求項1記載の共押出剤型。
- 前記剤型が錠剤又はカプレットである、請求項6記載の共押出剤型。
- 前記剤型が複数の粒子を含有するカプセルである、請求項6記載の共押出剤型。
- 前記粒子が、全ての寸法において約0.1mm〜約3.0mmの範囲内の大きさである、請求項8記載の共押出剤型。
- 前記作用薬がオピオイドアゴニストであり、前記逆作用薬がオピオイドアンタゴニストである、請求項9記載の共押出剤型。
- 前記剤型が、患者への投与後に前記オピオイドアゴニストの制御放出を提供する、請求項10記載の共押出剤型。
- 逆作用薬を含有するコア、
疎水性物質を含有し前記コアの少なくとも一部を取り囲むシース、及び
作用薬を含有し前記シースの少なくとも一部を取り囲むシェル
を含む共押出剤型。 - 前記コアがさらに疎水性物質を含有する、請求項12記載の共押出剤型。
- 前記シースが前記コアの大部分を取り囲み、前記シェルが前記シースの大部分を取り囲んでなる、請求項12記載の共押出剤型。
- 前記シェルがさらに疎水性物質を含有する、請求項12記載の共押出剤型。
- 前記疎水性物質が、アクリル酸及びメタクリル酸ポリマー及びコポリマー、アルキルセルロース、天然及び合成ロウ、水不溶性ロウ、脂肪アルコール、脂肪酸、水添脂肪、脂肪酸エステル、脂肪酸グリセリド、炭化水素、炭化水素骨格を有する疎水性及び親水性ポリマー、並びに上記したもののいずれか2つ又はそれ以上の混合物から成る群より選択される物質を含む、請求項12記載の共押出剤型。
- 前記疎水性物質がアンモニオメタクリレートコポリマーを含む、請求項16記載の共押出剤型。
- 前記剤型が経口投与剤型である、請求項12記載の共押出剤型。
- 前記経口投与剤型が錠剤又はカプレットである、請求項18記載の共押出剤型。
- 前記経口投与剤型が複数の粒子を含有するカプセルである、請求項18記載の共押出剤型。
- 前記作用薬がオピオイドアゴニストであり、前記逆作用薬がオピオイドアンタゴニストである、請求項12記載の共押出剤型。
- 前記オピオイドアゴニストが、アルフェンタニル、アリルプロジン、アルファプロジン、アニレリジン、ベンジルモルフィン、ベジトラミド、ブプレノルフィン、ブトルファノール、クロニタゼン、コデイン、デソモルフィン、デキストロモラミド、デゾシン、ジアンプロミド、ジヒドロコデイン、ジヒドロモルフィン、ジメノキサドール、ジメフェプタノール、ジメチルチアンブテン、ジオキサフェチルブチレート、ジピパノン、エプタゾシン、エトヘプタジン、エチルメチルチアンブテン、エチルモルフィン、エトニタゼン、フェンタニル、ヘロイン、ヒドロコドン、ヒドロモルフォン、ヒドロキシペチジン、イソメタドン、ケトベミドン、レバロルファン、レボルファノール、レボフェナシルモルファン、ロフェンタニル、メペリジン、メプタジノール、メタゾシン、メタドン、メトフォン、モルフィン、ミロフィン、ナルブフィン、ナルセイン、ニコモルフィン、ノルレボルファノール、ノルメタドン、ナロルフィン、ノルモルフィン、ノルピパノン、アヘン、オキシコドン、オキシモルフォン、パパベレタム、ペンタゾシン、フェナドキソン、フェノモルファン、フェナゾシン、フェノペリジン、ピミノジン、ピリトラミド、プロヘプタジン、プロメドール、プロペリジン、プロピラム、プロポキシフェン、スフェンタニル、トラマドール、チリジン、これらの製薬上許容されうる塩、及び上記したもののいずれか2つ又はそれ以上の混合物から成る群より選択される、請求項21記載の共押出剤型。
- 前記オピオイドアゴニストが、モルフィン、コデイン、ヒドロモルフォン、ヒドロコドン、オキシコドン、オキシモルフォン、ジヒドロコデイン、ヒジドロモルフィン、これらの製薬上許容されうる塩、及び上記したもののいずれか2つ又はそれ以上の混合物から成る群より選択される、請求項21記載の共押出剤型。
- 前記オピオイドアンタゴニストが、シクラゾシン、ナロキソン、ナルトレキソン、ナルメフェン、ナルブフィン、ナロルフィン、シクラザシン、レバロルファン、これらの製薬上許容されうる塩、及び上記したもののいずれか2つ又はそれ以上の混合物から成る群より選択される、請求項21記載の共押出剤型。
- 前記オピオイドアンタゴニストが、ナロキソン、ナルトレキソン、ナルメフェン、これらの製薬上許容されうる塩、及び上記したもののいずれか2つ又はそれ以上の混合物から成る群より選択される、請求項21記載の共押出剤型。
- 前記剤型が、患者への投与後に前記オピオイドアゴニストの制御放出を提供する、請求項21記載の共押出剤型。
- 前記剤型が、患者への投与後にインビボで約0.5mg以下のオピオイドアンタゴニストを放出する、請求項21記載の共押出剤型。
- 前記剤型が、患者への投与後にインビボで約0.05mg以下のオピオイドアンタゴニストを放出する、請求項21記載の共押出剤型。
- 請求項12記載の共押出剤型を患者に投与することを含み、作用薬がオピオイドアゴニストであり、逆作用薬がオピオイドアンタゴニストである、患者の疼痛を治療するための方法。
- a)作用薬がオピオイドアゴニストであり、逆作用薬がオピオイドアンタゴニストである、請求項13記載の共押出剤型、及び
b)患者の疼痛を治療するための剤型の使用法を指示する印刷されたセットの指示書
を含む、患者の疼痛を治療するためのキット。 - a)逆作用薬を含有するコアと、作用薬を含有し前記コアを少なくとも部分的に取り囲むシェルとを共押出することによって多層押出物を形成すること、並びに
b)前記多層押出物から少なくとも1個の粒子を形成すること
を含む、不正使用防止剤型を製造する方法。 - 前記剤型が、患者への投与後に前記作用薬の制御放出を提供する、請求項31記載の方法。
- 前記作用薬がオピオイドアゴニストであり、前記逆作用薬がオピオイドアンタゴニストである、請求項31記載の方法。
- 前記オピオイドアゴニストが、アルフェンタニル、アリルプロジン、アルファプロジン、アニレリジン、ベンジルモルフィン、ベジトラミド、ブプレノルフィン、ブトルファノール、クロニタゼン、コデイン、デソモルフィン、デキストロモラミド、デゾシン、ジアンプロミド、ジヒドロコデイン、ジヒドロモルフィン、ジメノキサドール、ジメフェプタノール、ジメチルチアンブテン、ジオキサフェチルブチレート、ジピパノン、エプタゾシン、エトヘプタジン、エチルメチルチアンブテン、エチルモルフィン、エトニタゼン、フェンタニル、ヘロイン、ヒドロコドン、ヒドロモルフォン、ヒドロキシペチジン、イソメタドン、ケトベミドン、レバロルファン、レボルファノール、レボフェナシルモルファン、ロフェンタニル、メペリジン、メプタジノール、メタゾシン、メタドン、メトフォン、モルフィン、ミロフィン、ナルブフィン、ナルセイン、ニコモルフィン、ノルレボルファノール、ノルメタドン、ナロルフィン、ノルモルフィン、ノルピパノン、アヘン、オキシコドン、オキシモルフォン、パパベレタム、ペンタゾシン、フェナドキソン、フェノモルファン、フェナゾシン、フェノペリジン、ピミノジン、ピリトラミド、プロヘプタジン、プロメドール、プロペリジン、プロピラム、プロポキシフェン、スフェンタニル、トラマドール、チリジン、これらの製薬上許容されうる塩、及び上記したものの2又はそれ以上の混合物から成る群より選択される、請求項33記載の方法。
- 前記オピオイドアゴニストが、モルフィン、コデイン、ヒドロモルフォン、ヒドロコドン、オキシコドン、オキシモルフォン、ジヒドロコデイン、ヒジドロモルフィン、これらの製薬上許容されうる塩、及び上記したものの2又はそれ以上の混合物から成る群より選択される、請求項33記載の方法。
- 前記オピオイドアンタゴニストが、シクラゾシン、ナロキソン、ナルトレキソン、ナルメフェン、ナルブフィン、ナロルフィン、シクラザシン、レバロルファン、これらの製薬上許容されうる塩、及び上記したものの2又はそれ以上の混合物から成る群より選択される、請求項33記載の方法。
- 前記オピオイドアンタゴニストが、ナルメフェン、ナロキソン、ナルトレキソン、これらの製薬上許容されうる塩、及び上記したものの2又はそれ以上の混合物から成る群より選択される、請求項33記載の方法。
- 前記剤型が、全ての寸法において約0.1mm〜約3mmの大きさを有する複数の粒子を含有する、請求項31記載の方法。
- 複数の粒子をカプセルに入れることをさらに含む、請求項38記載の方法。
- 前記不正使用防止剤型が経口投与剤型である、請求項31記載の方法。
- 前記コア及び前記シェルの各々が疎水性物質を含有する、請求項31記載の方法。
- 前記疎水性物質が、アクリル酸及びメタクリル酸ポリマー及びコポリマー、アルキルセルロース、天然及び合成ロウ、水不溶性ロウ、脂肪アルコール、脂肪酸、水添脂肪、脂肪酸エステル、脂肪酸グリセリド、炭化水素、炭化水素骨格を有する疎水性及び親水性ポリマー、並びに上記したものの2又はそれ以上の混合物から成る群より選択される、請求項41記載の方法。
- 前記疎水性物質がアンモニオメタクリレートコポリマーを含む、請求項42記載の方法。
- 前記不正使用防止剤型が、少なくとも約12時間、インビボで前記作用薬の制御放出を提供する、請求項31記載の方法。
- 前記不正使用防止剤型が、少なくとも約24時間、インビボで前記作用薬の制御放出を提供する、請求項31記載の方法。
- 前記作用薬がオピオイドアゴニストであり、逆作用薬がオピオイドアンタゴニストであって、前記不正使用防止剤型が、投与後にインビボで約0.5mg以下のオピオイドアンタゴニストを放出する、請求項45記載の方法。
- 前記不正使用防止剤型が、投与後にインビボで約0.05mg以下のオピオイドアンタゴニストを放出する、請求項46記載の方法。
- a)逆作用薬及び疎水性物質を含有するコア;
疎水性物質を含有し前記コアを少なくとも部分的に取り囲むシース;及び
作用薬及び疎水性物質を含有し前記シースを少なくとも部分的に取り囲むシェル
を共押出することによって多層押出物を形成すること、
b)ローリングパンチを用いて前記多層押出物から1以上の粒子を形成すること、並びに
c)1以上の粒子を剤型に組み込むこと
を含む、不正使用防止剤型を製造する方法。 - 前記剤型が、患者への投与時に作用薬の制御放出を提供する、請求項48記載の方法。
- 前記作用薬がオピオイドアゴニストであり、前記逆作用薬がオピオイドアンタゴニストである、請求項48記載の方法。
- 前記オピオイドアゴニストが、アルフェンタニル、アリルプロジン、アルファプロジン、アニレリジン、ベンジルモルフィン、ベジトラミド、ブプレノルフィン、ブトルファノール、クロニタゼン、コデイン、デソモルフィン、デキストロモラミド、デゾシン、ジアンプロミド、ジヒドロコデイン、ジヒドロモルフィン、ジメノキサドール、ジメフェプタノール、ジメチルチアンブテン、ジオキサフェチルブチレート、ジピパノン、エプタゾシン、エトヘプタジン、エチルメチルチアンブテン、エチルモルフィン、エトニタゼン、フェンタニル、ヘロイン、ヒドロコドン、ヒドロモルフォン、ヒドロキシペチジン、イソメタドン、ケトベミドン、レバロルファン、レボルファノール、レボフェナシルモルファン、ロフェンタニル、メペリジン、メプタジノール、メタゾシン、メタドン、メトフォン、モルフィン、ミロフィン、ナルブフィン、ナルセイン、ニコモルフィン、ノルレボルファノール、ノルメタドン、ナロルフィン、ノルモルフィン、ノルピパノン、アヘン、オキシコドン、オキシモルフォン、パパベレタム、ペンタゾシン、フェナドキソン、フェノモルファン、フェナゾシン、フェノペリジン、ピミノジン、ピリトラミド、プロヘプタジン、プロメドール、プロペリジン、プロピラム、プロポキシフェン、スフェンタニル、トラマドール、チリジン、これらの製薬上許容されうる塩、及び上記したものの2又はそれ以上の混合物から成る群より選択される、請求項50記載の方法。
- 前記オピオイドアゴニストが、モルフィン、コデイン、ヒドロモルフォン、ヒドロコドン、オキシコドン、オキシモルフォン、ジヒドロコデイン、ヒジドロモルフィン、これらの製薬上許容されうる塩、及び上記したものの2又はそれ以上の混合物から成る群より選択される、請求項50記載の方法。
- 前記オピオイドアンタゴニストが、シクラゾシン、ナロキソン、ナルトレキソン、ナルメフェン、ナルブフィン、ナロルフィン、シクラザシン、レバロルファン、これらの製薬上許容されうる塩、及び上記したものの2又はそれ以上の混合物から成る群より選択される、請求項50記載の方法。
- 前記オピオイドアンタゴニストが、ナルメフェン、ナロキソン、ナルトレキソン、これらの製薬上許容されうる塩、及び上記したものの2又はそれ以上の混合物から成る群より選択される、請求項50記載の方法。
- 前記粒子が、全ての寸法において約0.1mm〜約3mmの大きさを有する、請求項48記載の方法。
- 複数の粒子をカプセルに入れることをさらに含む、請求項55記載の方法。
- 前記不正使用防止剤型が経口投与剤型である、請求項48記載の方法。
- 前記疎水性物質が、アクリル酸及びメタクリル酸ポリマー及びコポリマー、アルキルセルロース、天然及び合成ロウ、水不溶性ロウ、脂肪アルコール、脂肪酸、水添脂肪、脂肪酸エステル、脂肪酸グリセリド、炭化水素、炭化水素骨格を有する疎水性及び親水性ポリマー、並びに上記したものの2又はそれ以上の混合物から成る群より選択される少なくとも1つの物質を含む、請求項48記載の方法。
- 前記疎水性物質がアンモニオメタクリレートコポリマーを含む、請求項58記載の方法。
- 前記不正使用防止剤型が、少なくとも約12時間、インビボで前記作用薬の制御放出を提供する、請求項48記載の方法。
- 前記不正使用防止剤型が、少なくとも約24時間、インビボで前記作用薬の制御放出を提供する、請求項48記載の方法。
- 前記作用薬がオピオイドアゴニストであり、逆作用薬がオピオイドアンタゴニストであって、前記不正使用防止剤型が、投与後にインビボで約0.5mg以下のオピオイドアンタゴニストを放出する、請求項61記載の方法。
- 前記不正使用防止剤型が、投与後にインビボで約0.05mg以下のオピオイドアンタゴニストを放出する、請求項62記載の方法。
- 請求項48記載の方法により製造された不正使用防止剤型を患者に投与することを含む、患者の病状又はその症状を治療する方法。
- 前記病状又は症状が疼痛を含む、請求項64記載の方法。
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JP2011272389A Division JP2012082214A (ja) | 2003-12-09 | 2011-12-13 | 作用薬及び逆作用薬を含有する不正使用防止共押出剤型、及びその製造方法 |
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AT (1) | ATE355103T1 (ja) |
CA (1) | CA2548834C (ja) |
CY (1) | CY1106600T1 (ja) |
DE (1) | DE602004005076T2 (ja) |
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2004
- 2004-12-08 CA CA002548834A patent/CA2548834C/en active Active
- 2004-12-08 JP JP2006543959A patent/JP4917893B2/ja active Active
- 2004-12-08 US US10/582,256 patent/US20070269505A1/en not_active Abandoned
- 2004-12-08 SI SI200430281T patent/SI1691892T1/sl unknown
- 2004-12-08 EP EP04813471A patent/EP1691892B1/en active Active
- 2004-12-08 DE DE602004005076T patent/DE602004005076T2/de active Active
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Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2010536770A (ja) * | 2007-08-13 | 2010-12-02 | アビューズ ディタレント ファーマスティカル エルエルシー | 乱用抵抗性医薬組成物、その使用方法および作製方法 |
JP2016138126A (ja) * | 2007-08-13 | 2016-08-04 | インスピリオン デリバリー テクノロジーズ エルエルシー | 乱用抵抗性医薬組成物、その使用方法および作製方法 |
JP2012508254A (ja) * | 2008-11-11 | 2012-04-05 | ターガセプト,インコーポレイテッド | α7選択的リガンドを用いる治療 |
JP2014530185A (ja) * | 2011-09-16 | 2014-11-17 | パーデュー ファーマ エルピー | 不正改変抵抗性即時放出性製剤 |
Also Published As
Publication number | Publication date |
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JP5473958B2 (ja) | 2014-04-16 |
JP2011126895A (ja) | 2011-06-30 |
ES2281851T3 (es) | 2007-10-01 |
JP2012082214A (ja) | 2012-04-26 |
JP4917893B2 (ja) | 2012-04-18 |
EP1691892A2 (en) | 2006-08-23 |
PL1691892T3 (pl) | 2007-07-31 |
CA2548834A1 (en) | 2005-06-23 |
CA2548834C (en) | 2009-08-11 |
DE602004005076T2 (de) | 2007-11-15 |
DK1691892T3 (da) | 2007-06-25 |
EP1691892B1 (en) | 2007-02-28 |
SI1691892T1 (sl) | 2007-08-31 |
PT1691892E (pt) | 2007-05-31 |
WO2005055981A2 (en) | 2005-06-23 |
WO2005055981A3 (en) | 2005-08-11 |
ATE355103T1 (de) | 2006-03-15 |
US20070269505A1 (en) | 2007-11-22 |
DE602004005076D1 (de) | 2007-04-12 |
CY1106600T1 (el) | 2012-01-25 |
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