JP2009524626A - タンパリング防止剤形 - Google Patents
タンパリング防止剤形 Download PDFInfo
- Publication number
- JP2009524626A JP2009524626A JP2008551790A JP2008551790A JP2009524626A JP 2009524626 A JP2009524626 A JP 2009524626A JP 2008551790 A JP2008551790 A JP 2008551790A JP 2008551790 A JP2008551790 A JP 2008551790A JP 2009524626 A JP2009524626 A JP 2009524626A
- Authority
- JP
- Japan
- Prior art keywords
- opioid
- amount
- extract
- opioid agonist
- dosage form
- 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.)
- Granted
Links
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- 239000000203 mixture Substances 0.000 claims abstract description 79
- 238000009472 formulation Methods 0.000 claims abstract description 70
- 238000013270 controlled release Methods 0.000 claims abstract description 52
- 239000003402 opiate agonist Substances 0.000 claims description 99
- 239000003401 opiate antagonist Substances 0.000 claims description 79
- 239000000284 extract Substances 0.000 claims description 60
- 238000000605 extraction Methods 0.000 claims description 50
- 239000011159 matrix material Substances 0.000 claims description 43
- -1 vegitramide Chemical compound 0.000 claims description 30
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- 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
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Abstract
Description
塩酸塩、臭化水素酸塩、硫酸塩、リン酸塩などの無機酸塩;ギ酸塩、酢酸塩、トリフルオロ酢酸塩、マレイン酸塩、酒石酸塩などの有機酸塩;メタンスルホン酸、ベンゼンスルホン酸、p−トルエンスルホン酸などのスルホン酸塩;アルギン酸塩、アスパラギン酸塩、グルタミン酸塩などのアミノ酸塩を含む。
a)ピルクラッシャーもしくは錠剤用乳鉢を使用して、または2つのスプーンを使用してスプーンで少なくとも4回粉砕して、1剤形の製剤を粉砕するステップと、
b)1剤形の粉砕した製剤を、抽出剤として2mlの沸騰した水道水、および加熱手段としてたばこ用ライターを使用して、水を沸騰させるのに必要な時間スプーン上で抽出するステップと、
c)コットンを使用して溶液を濾過するステップと
を含むワンステップ抽出手順による、オピオイド作動薬を含む前記放出制御マトリックス製剤の抽出物であって、オピオイド拮抗薬は、前記抽出物中に、剤形中のオピオイド拮抗薬の全量に基づく重量パーセント量で、剤形中のオピオイド作動薬全量に基づく、抽出物中に存在するオピオイド作動薬の重量パーセント量より20%ポイント超、好ましくは15%ポイント超、より好ましくは12%ポイント超少なく存在する
前記抽出物の形成を防止するための使用を対象とする。
a)ピルクラッシャーもしくは錠剤用乳鉢を使用して、または2つのスプーンを使用してスプーンで少なくとも4回粉砕して、1剤形の製剤を粉砕するステップと、
b)前記製剤をスプーン上で、抽出剤として2mlの沸騰した脱イオン水、水を沸騰させるのに必要な時間の加熱手段としてたばこ用ライターを使用して抽出するステップと、
c)コットンを使用して溶液を濾過するステップと
を含むワンステップ抽出手順による、オピオイド作動薬を含む前記放出制御マトリックス製剤の抽出物であって、オピオイド拮抗薬は、前記抽出物中に、剤形中のオピオイド拮抗薬の全量に基づく重量パーセント量で、剤形中のオピオイド作動薬全量に基づく、抽出物中に存在するオピオイド作動薬の重量パーセント量より15%ポイント超、好ましくは10ポイント超、より好ましくは7%ポイント超少なく存在する
前記抽出物の形成を防止するための使用を対象とする。
a)ピルクラッシャーを使用して、10個の剤形の製剤を粉砕するステップと、
b)前記粉砕した製剤を、ガラスのバイアル中で、脱イオン水、塩酸(2N)、酢酸(2N)、水酸化ナトリウム溶液(0.1N、0.5N、1Nまたは2N)およびエタノール(40%)の群から選択される100mlの抽出溶媒を使用し、少なくとも15分間、少なくとも室温で振とうさせて抽出するステップと
を含むワンステップ抽出手順による、オピオイド作動薬を含む前記放出制御マトリックス製剤の抽出物であって、オピオイド拮抗薬は、前記抽出物中に、剤形中のオピオイド拮抗薬の全量に基づく重量パーセント量で、剤形中のオピオイド作動薬全量に基づく、抽出物中に存在するオピオイド作動薬の重量パーセント量より10%ポイント超、好ましくは5%ポイント超、より好ましくは3%ポイント超少なく存在する
前記抽出物の形成を防止するための使用を対象とする。前記抽出物の形成が、たとえ120分間振とうされても防止されることが好ましい。前記抽出物の形成が、脱イオン水が抽出溶媒として使用され、抽出の際に脱イオン水を50℃まで、好ましくは75℃まで、最も好ましくは100℃まで、5分間加熱する場合でも、なお防止されることが好ましい。
a)脱イオン水を70℃に加熱するステップと、
b)1剤形の未処理製剤を加え、15分間撹拌するステップと、
c)抽出物を分離するステップと
を含むワンステップ抽出手順による、オピオイド作動薬を含む前記放出制御マトリックス製剤の抽出物であって、オピオイド拮抗薬は、前記抽出物中に、剤形中のオピオイド拮抗薬の全量に基づく重量パーセント量で、剤形中のオピオイド作動薬全量に基づく、抽出物中に存在するオピオイド作動薬の重量パーセント量より15%ポイント超、好ましくは10%ポイント超少なく存在する
前記抽出物の形成を防止するための使用を対象とする。
使用材料
2ml注射器 注射針
DBプラスチパック(Plastipak)(登録商標) (0.90×40mm)
バッチ番号0502018 100Sterican(商標)
バッチ番号98K2982510
B/Braun Melsungen/ドイツ
コットン
Lohmann Rauscher
バッチ番号1055314
Rengsdorf、ドイツ
ACU医療用ピルクラッシャー EZ-SWALLOW(登録商標)ピルクラッシャー
Health Enterprises, Inc. American Medical Industries
North Attleboro、 Dell Papids, USA
米国マサチューセッツ州02760
錠剤用乳鉢
Medi−Globe(商標)、Vertriebs GmbH
Eppstein、ドイツ
1)(静脈注射)静脈注射投与技術を評価する方法は、実施例1または2の錠剤を粉砕するステップ、その後少量の水に抽出するステップを含む。得られた溶液をその後インスリン用注射器に引き入れた。錠剤の粉砕は、異なるピルクラッシャーおよびステンレス製のテーブルスプーンを使用して行った。
Claims (20)
- 少なくとも1種の疎水性ポリマーおよび少なくとも1種の脂肪アルコールまたは脂肪酸を含む疎水性材料、ならびに治療量のオピオイド作動薬および十分量のオピオイド拮抗薬を含む、均一な放出制御マトリックス製剤を含む放出制御剤形の形態で、オピオイド作動薬およびオピオイド拮抗薬の両方を同時に静脈内投与する場合の、前記治療量のオピオイド作動薬を実質的に拮抗するのに少なくとも十分な量のオピオイド拮抗薬のある量の使用であって、
a)ピルクラッシャーもしくは錠剤用乳鉢を使用して、または2つのスプーンを使用してスプーンで少なくとも4回粉砕して、1剤形の製剤を粉砕するステップと、
b)1剤形の粉砕した製剤を、抽出剤として2mlの沸騰した水道水、および加熱手段としてたばこ用ライターを使用して、水を沸騰させるのに必要な時間スプーン上で抽出するステップと、
c)コットンを使用して溶液を濾過するステップと
を含むワンステップ抽出手順による、オピオイド作動薬を含む前記放出制御マトリックス製剤の抽出物であって、前記オピオイド拮抗薬は、前記抽出物中に、剤形中のオピオイド拮抗薬の全量に基づく重量パーセント量で、剤形中のオピオイド作動薬全量に基づく、抽出物中に存在するオピオイド作動薬の重量パーセント量より20%ポイント超少なく存在する
前記抽出物の形成を防止するための使用。 - 前記オピオイド拮抗薬が、前記抽出物中に、剤形中のオピオイド拮抗薬の全量に基づく重量パーセント量で、剤形中のオピオイド作動薬全量に基づく、抽出物中に存在するオピオイド作動薬の重量パーセント量より15%ポイント超、好ましくは12%ポイント超少なく存在する抽出物の形成を防止するための、請求項1に記載の使用。
- 少なくとも1種の疎水性ポリマーおよび少なくとも1種の脂肪アルコールまたは脂肪酸を含む疎水性材料、ならびに治療量のオピオイド作動薬および十分量のオピオイド拮抗薬を含む、均一な放出制御マトリックス製剤を含む放出制御剤形の形態で、オピオイド作動薬およびオピオイド拮抗薬の両方を同時に静脈内投与する場合の、前記治療量のオピオイド作動薬を実質的に拮抗するのに少なくとも十分な量のオピオイド拮抗薬のある量の使用であって、
a)ピルクラッシャーもしくは錠剤用乳鉢を使用して、または2つのスプーンを使用してスプーンで少なくとも4回粉砕して、1剤形の製剤を粉砕するステップと、
b)前記製剤をスプーン上で、抽出剤として2mlの沸騰した脱イオン水、水を沸騰させるのに必要な時間の加熱手段としてたばこ用ライターを使用して抽出するステップと、
c)コットンを使用して溶液を濾過するステップと
を含むワンステップ抽出手順による、オピオイド作動薬を含む前記放出制御マトリックス製剤の抽出物であって、前記オピオイド拮抗薬は、前記抽出物中に、剤形中のオピオイド拮抗薬の全量に基づく重量パーセント量で、剤形中のオピオイド作動薬全量に基づく、抽出物中に存在するオピオイド作動薬の重量パーセント量より15%ポイント超少なく存在する
前記抽出物の形成を防止するための使用。 - 前記オピオイド拮抗薬が、前記抽出物中に、剤形中のオピオイド拮抗薬の全量に基づく重量パーセント量で、剤形中のオピオイド作動薬全量に基づく、抽出物中に存在するオピオイド作動薬の重量パーセント量より10%ポイント超、好ましくは7%ポイント超少なく存在する抽出物の形成を防止するための、請求項1に記載の使用。
- 少なくとも1種の疎水性ポリマーおよび少なくとも1種の脂肪アルコールまたは脂肪酸を含む疎水性材料、ならびに治療量のオピオイド作動薬および十分量のオピオイド拮抗薬を含む、均一な放出制御マトリックス製剤を含む放出制御剤形の形態で、オピオイド作動薬およびオピオイド拮抗薬の両方を同時に静脈内投与する場合の、前記治療量のオピオイド作動薬を実質的に拮抗するのに少なくとも十分な量のオピオイド拮抗薬のある量の使用であって、
a)ピルクラッシャーを使用して、10個の剤形の製剤を粉砕するステップと、
b)前記粉砕した製剤を、ガラスのバイアル中で、脱イオン水、塩酸(2N)、酢酸(2N)、水酸化ナトリウム溶液(0.1N、0.5N、1Nまたは2N)およびエタノール(40%)の群から選択される100mlの抽出溶媒を使用し、少なくとも15分間、少なくとも室温で振とうさせて抽出するステップと
を含むワンステップ抽出手順による、オピオイド作動薬を含む前記放出制御マトリックス製剤の抽出物であって、前記オピオイド拮抗薬は、前記抽出物中に、剤形中のオピオイド拮抗薬の全量に基づく重量パーセント量で、剤形中のオピオイド作動薬全量に基づく、抽出物中に存在するオピオイド作動薬の重量パーセント量より10%ポイント超少なく存在する
前記抽出物の形成を防止するための使用。 - 前記オピオイド拮抗薬が、前記抽出物中に、剤形中のオピオイド拮抗薬の全量に基づく重量パーセント量で、剤形中のオピオイド作動薬全量に基づく、抽出物中に存在するオピオイド作動薬の重量パーセント量より5%ポイント超、または3%ポイント超少なく存在する抽出物の形成を防止するための、請求項5に記載の使用。
- 振とうが120分間行われる、抽出物の形成を防止するための、請求項5または6に記載の使用。
- 脱イオン水を抽出溶媒として使用し、抽出中に脱イオン水を50℃、好ましくは75℃、最も好ましくは100℃に5分間加熱する抽出物の形成を防止するための、請求項5から7のいずれか一項に記載の使用。
- 少なくとも1種の疎水性ポリマーおよび少なくとも1種の脂肪アルコールまたは脂肪酸を含む疎水性材料、ならびに治療量のオピオイド作動薬および十分量のオピオイド拮抗薬を含む、均一な放出制御マトリックス製剤を含む放出制御剤形の形態で、オピオイド作動薬およびオピオイド拮抗薬の両方を同時に静脈内投与する場合の、前記治療量のオピオイド作動薬を実質的に拮抗するのに少なくとも十分な量のオピオイド拮抗薬のある量の使用であって、
a)脱イオン水を70℃に加熱するステップと、
b)1剤形の未処理製剤を加え、15分間撹拌するステップと、
c)抽出物を分離するステップと
を含むワンステップ抽出手順による、オピオイド作動薬を含む前記放出制御マトリックス製剤の抽出物であって、前記オピオイド拮抗薬は、前記抽出物中に、剤形中のオピオイド拮抗薬の全量に基づく重量パーセント量で、剤形中のオピオイド作動薬全量に基づく、抽出物中に存在するオピオイド作動薬の重量パーセント量より15%ポイント超少なく存在する
前記抽出物の形成を防止するための使用。 - 前記オピオイド拮抗薬が、前記抽出物中に、剤形中のオピオイド拮抗薬の全量に基づく重量パーセント量で、剤形中のオピオイド作動薬全量に基づく、抽出物中に存在するオピオイド作動薬の重量パーセント量より10%ポイント超少なく存在する抽出物の形成を防止するための、請求項9に記載の使用。
- 前記製剤が、均一なマトリックスを成形するために溶融押出しステップにより調製される、請求項1から10のいずれか一項に記載の使用。
- 前記オピオイドが、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、ベンジルモルヒネ、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、デソモルヒネ、デキストロモラミド、デゾシン、ジアンプロミド、ジアモルフォン、ジヒドロコデイン、ジヒドロモルヒネ、ジメノキサドール、ジメフェプタノール、ジメチルチアムブテン、ジオキサフェチルブチラート、ジピパノン、エプタゾシン、エトヘプタジン、エチルメチルチアムブテン、エチルモルヒネ、エトニタゼン、エトルフィン、ジヒドロエトルフィン、フェンタニルおよび誘導体、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、レボルファノール、レボル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、メトポン、モルヒネ、ミロフィン、ナルセイン、ニコモルヒネ、ノルレボルファノール、ノルメタドン、ナロルフィン、ナルブフェン、ノルモルヒネ、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、プロフェプタジン、プロメドール、プロペリジン、プロポキシフェン、スフェンタニル、チリジン、トラマドール、前述のいずれかの医薬として許容される塩および前述のいずれかの混合物などから選択され、好ましくはコデイン、モルヒネ、オキシコドン、ヒドロコドン、ヒドロモルフォンまたはオキシモルフォンのいずれかの医薬として許容される塩から選択される、請求項1から11のいずれか一項に記載の使用。
- 前記オピオイド拮抗薬が、ナロキソン、ナルトレキソンおよびナロルフィンの群から選択される、請求項1から12のいずれか一項に記載の使用。
- 前記オピオイド作動薬が塩酸オキシコドンであり、前記オピオイド拮抗薬が塩酸ナロキソンである、請求項1から13のいずれか一項に記載の使用。
- 前記オピオイド作動薬が塩酸オキシコドンであり、前記オピオイド拮抗薬が塩酸ナロキソンであり、これらが剤形中に2:1の量比で存在する、請求項1から14のいずれか一項に記載の使用。
- 前記疎水性ポリマーがアルキルセルロース、好ましくはエチルセルロースである、請求項1から15のいずれか一項に記載の使用。
- 前記アルキルセルロース、好ましくは前記エチルセルロースの量が、前記マトリックス製剤の20(重量)%未満であり、好ましくは15(重量)%未満であり、最も好ましくは10(重量)%未満であるが、5(重量)%は超える、請求項16に記載の使用。
- 前記脂肪アルコールまたは脂肪酸が、C12からC36の脂肪族アルコールまたは脂肪酸、好ましくはステアリルアルコール、セチルアルコール、セトステアリルアルコール、ステアリン酸、パルミチン酸およびこれらの混合物から選択される、請求項1から17のいずれか一項に記載の使用。
- 前記C12からC36の脂肪族アルコールまたは脂肪酸の量が、前記マトリックス製剤の少なくとも5%、より好ましくは少なくとも10(重量)%、より好ましくは少なくとも15(重量)%、最も好ましくは20から25(重量)%である、請求項18に記載の使用。
- 前記エチルセルロースの量が、前記マトリックス製剤の10(重量)%未満であり、さらに20から25(重量)%の量のステアリルアルコールを含み、かつ、塩酸オキシコドンと塩酸ナロキソンとを2:1の量比で含む、請求項16に記載の使用。
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US10864164B2 (en) | 2011-07-29 | 2020-12-15 | Grünenthal GmbH | Tamper-resistant tablet providing immediate drug release |
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US10624862B2 (en) | 2013-07-12 | 2020-04-21 | Grünenthal GmbH | Tamper-resistant dosage form containing ethylene-vinyl acetate polymer |
US10449547B2 (en) | 2013-11-26 | 2019-10-22 | Grünenthal GmbH | Preparation of a powdery pharmaceutical composition by means of cryo-milling |
US10842750B2 (en) | 2015-09-10 | 2020-11-24 | Grünenthal GmbH | Protecting oral overdose with abuse deterrent immediate release formulations |
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