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1. 发明专利

JP2015044834A オピオイド鎮痛薬を含む不正改変抵抗性経口医薬剤形有权
标题翻译：具有对包含OPIOID ANALGESIC的未经改变的改变的电阻率的口服药物剂型
公开(公告)号：JP2015044834A
公开(公告)日：2015-03-12
申请号：JP2014220816
申请日：2014-10-29
申请人：パーデュー、ファーマ、リミテッド、パートナーシップ , Purdue Pharma Lp
发明人： MANNION RICHARD OWEN , O'DONNELL EDWARD PATRICK , MCKENNA WILLIAM HENRY , HUANG HAIYONG HUGH
IPC分类号： A61K45/00 , A61K9/22 , A61K9/24 , A61K9/26 , A61K31/135 , A61K31/4468 , A61K31/4535 , A61K31/454 , A61K31/4725 , A61K31/485 , A61K31/5377 , A61K31/55 , A61K47/04 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/26 , A61K47/32 , A61K47/34 , A61P25/04
CPC分类号： A61K9/2027 , A61J3/005 , A61J3/06 , A61J3/10 , A61K9/0002 , A61K9/0053 , A61K9/1641 , A61K9/2013 , A61K9/2018 , A61K9/2031 , A61K9/2054 , A61K9/2072 , A61K9/2077 , A61K9/209 , A61K9/2095 , A61K9/28 , A61K9/284 , A61K9/2853 , A61K9/2866 , A61K9/2893 , A61K31/485 , A61K45/06 , A61K47/10 , A61K47/34 , B29B7/02 , B29B7/88 , B29C35/045 , B29C35/16 , B29C37/0025 , B29C43/003 , B29C43/02 , B29C43/52 , B29C71/00 , B29C71/009 , B29C2035/046 , B29C2035/1658 , B29K2071/02 , B29K2105/0035 , B29K2105/251 , B29K2995/0088 , B29L2031/753
摘要：【課題】不正改変抵抗性のある、オピオイド鎮痛薬等の活性薬剤を含む持続放出性経口剤の調整方法の提供。【解決手段】(1)レオロジー測定に基づいて少なくとも1,000,000の概略分子量を有する少なくとも1種のポリエチレンオキシド、及び(2)少なくとも1種の活性薬剤を組み合わせて組成物を形成するステップと、(b)前記組成物を成形して持続放出性マトリックス製剤を形成するステップと、(c)前記持続放出性マトリックス製剤を低くても前記ポリエチレンオキシドの軟化温度である温度に少なくとも約1分間さらす硬化ステップを少なくとも含む、前記持続放出性マトリックス製剤を硬化するステップとを少なくとも含む持続放出性経口剤の調整方法。【選択図】なし
摘要翻译：要解决的问题：提供一种制备具有包括活性药物如阿片样镇痛剂的未经授权的改变的耐药性的缓释口服剂的方法。溶解性：提供一种制备缓释口服剂的方法，所述缓释口服剂至少包括以下步骤：（a）通过组合（1）基于流变学测量至少一种具有至少1,000,000个粗分子量的聚环氧乙烷和（2）至少一种活性药物来形成组合物; （b）模塑该组合物以形成缓释基质制剂; 和（c）硬化缓释基质制剂，其至少包括硬化步骤，其中缓释基质制剂在最低温度下暴露于聚环氧乙烷的软化温度至少约1分钟的温度。

2. 发明专利

JP2014094947A Substituted-quinoxaline-type piperidine compounds and uses thereof 审中-公开
标题翻译：替代 - 喹啉类型哌啶化合物及其用途
公开(公告)号：JP2014094947A
公开(公告)日：2014-05-22
申请号：JP2013263803
申请日：2013-12-20
申请人： Purdue Pharma Lp , パーデュー、ファーマ、リミテッド、パートナーシップ , Shionogi & Co Ltd , 塩野義製薬株式会社
发明人： RICHARD R GOEHRING , MATSUMURA AKIRA , SHAO BIN , TAODA YOSHIYUKI , TSUNO MAKI , JOHN WILLIAM FRANK WHITEHEAD , YAO JIANGCHAO , FUCHINO MITSUKI
IPC分类号： C07D401/04 , A61K31/498 , A61K31/5377 , A61K31/5386 , A61P1/10 , A61P1/12 , A61P1/14 , A61P3/04 , A61P7/00 , A61P9/12 , A61P11/14 , A61P13/10 , A61P25/08 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/36 , A61P43/00 , C07D401/14 , C07D451/04 , C07D487/04 , C07D487/08 , C07D498/08 , C07D519/00
CPC分类号： C07D451/14 , A61K31/498 , C07D401/04 , C07D401/14 , C07D451/04 , C07D471/08 , C07D471/14 , C07D487/04 , C07D498/08 , C07D519/00
摘要： PROBLEM TO BE SOLVED: To provide novel compounds which either exhibit agonist activity at the opioid receptor-like (ORL-1) receptor, exhibit partial agonist activity at the ORL-1 receptor, or exhibit antagonist activity at the ORL-1 receptor.SOLUTION: Provided are substituted-quinoxaline-type piperidine compounds represented by the general formula (I) or (II), where Y1 is O or S; Q is fused benzo or 5- or 6-membered heteroaryl; each R2 is independently selected from specific substituents; and a is an integer selected from 0, 1, and 2.
摘要翻译：要解决的问题：提供在阿片受体样受体（ORL-1）受体表现出激动剂活性的新化合物，在ORL-1受体中表现出部分激动剂活性，或在ORL-1受体上表现出拮抗剂活性。：提供由通式（I）或（II）表示的取代的喹喔啉型哌啶化合物，其中Y 1为O或S; Q是稠合的苯并或5或6元杂芳基; 每个R 2独立地选自具体的取代基; a是选自0,1和2的整数。

3. 发明专利

JP2014040467A Heterocyclic-substituted piperidine compounds and use thereof 审中-公开
标题翻译：杂环取代的哌啶化合物及其用途
公开(公告)号：JP2014040467A
公开(公告)日：2014-03-06
申请号：JP2013216047
申请日：2013-10-17
申请人： Purdue Pharma Lp , パーデュー、ファーマ、リミテッド、パートナーシップPurdue Pharma L.P. , Shionogi & Co Ltd , 塩野義製薬株式会社
发明人： BABA YOSHIYASU , KEVIN C BROWN , GOEHRING R RICHARD , TSUNO MAKI
IPC分类号： C07D401/04 , A61K31/498 , A61K31/4985 , A61K31/5377 , A61K31/5513 , A61P1/10 , A61P1/12 , A61P3/04 , A61P9/12 , A61P11/14 , A61P13/02 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/22 , A61P25/30 , A61P35/00 , A61P43/00 , C07D401/14 , C07D451/14 , C07D471/04
CPC分类号： C07D401/04 , C07D451/14 , C07D471/04 , C07D471/08
摘要： PROBLEM TO BE SOLVED: To provide new compounds that exhibit affinity for an opioid receptor-like (ORL-1) receptor.SOLUTION: The invention provides compounds, heterocyclic-substituted piperidine compounds, represented by formula (i), and pharmaceutically acceptable derivatives thereof. There are also provided methods of, in order to treat or prevent conditions such as a pain, administering an effective dose of the compounds to an animal in need of them.
摘要翻译：要解决的问题：提供对阿片样物质受体（ORL-1）受体显示亲和力的新化合物。解决方案：本发明提供由式（i）表示的化合物，杂环取代的哌啶化合物及其药学上可接受的衍生物。还提供了为了治疗或预防诸如疼痛的病症，向有需要的动物施用有效剂量的化合物的方法。

4. 发明专利

JP2013237692A Tamper-resistant transdermal opioid delivery device 审中-公开
标题翻译：防篡改变速器输送装置
公开(公告)号：JP2013237692A
公开(公告)日：2013-11-28
申请号：JP2013160887
申请日：2013-08-02
申请人： Purdue Pharma Lp , パーデュー、ファーマ、リミテッド、パートナーシップ
发明人： SHEVCHUK IHOR , CASSIDY JAMES P , REIDENBERG BRUCE , SHARP DALE E , KUPPER ROBERT J
IPC分类号： A61K31/485 , A61K9/70 , A61K31/4535 , A61K45/06 , A61K47/38 , A61P25/04 , A61P25/36 , C07D489/08
CPC分类号： A61K9/7084 , A61K31/485 , A61K45/06 , C07D489/08 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide improved transdermal-delivery devices that are effective for preventing abuse yet useful for delivering a therapeutic agent, such as an opioid or a pharmaceutically acceptable salt thereof.SOLUTION: The invention relates to a tamper-resistant transdermal-delivery comprising an analgesically effective amount of an opioid, or a pharmaceutically acceptable salt thereof, and an acyl opioid antagonist, or a pharmaceutically acceptable salt thereof, in an amount sufficient to inhibit the euphoric effect of the opioid, or pharmaceutically acceptable salt thereof. The transdermal-delivery device allows an analgesically effective amount of the opioid, or a pharmaceutically acceptable salt thereof, to be transdermally administered to a patient. The invention includes a step of contacting the skin of a patient in need of the treatment or prevention with the transdermal-delivery device for an amount of time sufficient to treat or prevent pain. The opioid is oxycodone or the like, and the acyl opioid antagonist is 3-(p-anisoylnaltrexone) or the like.
摘要翻译：要解决的问题：提供改进的透皮递送装置，其有效预防滥用，但可用于递送治疗剂，例如阿片样物质或其药学上可接受的盐。解决方案：本发明涉及抗篡改的经皮递送其包含足以抑制阿片样物质或其药学上可接受的盐的欣快作用的量的止痛有效量的阿片样物质或其药学上可接受的盐和酰基阿片样物质拮抗剂或其药学上可接受的盐。透皮递送装置允许将止痛有效量的阿片样物质或其药学上可接受的盐透皮给药给患者。本发明包括将需要治疗或预防的患者的皮肤与透皮递送装置接触足以治疗或预防疼痛的时间的步骤。阿片样物质为羟考酮等，酰基阿片样拮抗剂为3-（对茴香酰纳曲酮）等。

5. 发明专利

JP2012229250A Tamper-resistant oral pharmaceutical dosage form comprising opioid analgesic 审中-公开
标题翻译：抗抑郁药物口服药物形式包含OPIOID ANALGESIC
公开(公告)号：JP2012229250A
公开(公告)日：2012-11-22
申请号：JP2012157159
申请日：2012-07-13
申请人： Purdue Pharma Lp , パーデュー、ファーマ、リミテッド、パートナーシップ
发明人： MANNION RICHARD OWEN , O'DONNELL EDWARD PATRICK , MCKENNA WILLIAM HENRY , HUANG HAIYONG HUGH
IPC分类号： A61K31/4468 , A61K9/22 , A61K9/26 , A61K9/28 , A61K31/485 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/26 , A61K47/32 , A61K47/34 , A61P25/04
CPC分类号： A61K9/2027 , A61J3/005 , A61J3/06 , A61J3/10 , A61K9/0002 , A61K9/0053 , A61K9/1641 , A61K9/2013 , A61K9/2018 , A61K9/2031 , A61K9/2054 , A61K9/2072 , A61K9/2077 , A61K9/209 , A61K9/2095 , A61K9/28 , A61K9/284 , A61K9/2853 , A61K9/2866 , A61K9/2893 , A61K31/485 , A61K45/06 , A61K47/10 , A61K47/34 , B29B7/02 , B29B7/88 , B29C35/045 , B29C35/16 , B29C37/0025 , B29C43/003 , B29C43/02 , B29C43/52 , B29C71/00 , B29C71/009 , B29C2035/046 , B29C2035/1658 , B29K2071/02 , B29K2105/0035 , B29K2105/251 , B29K2995/0088 , B29L2031/753
摘要： PROBLEM TO BE SOLVED: To provide a tamper-resistant dosage form comprising an opioid analgesic, to provide a method for producing the same, and to provide a method for use and treatment thereof.SOLUTION: There is provided a controlled release solid oral pharmaceutical dosage form comprising a controlled release matrix formulation in the form of a tablet or multi-particulates as the object. The tablet or individual multi-particulates can be at least flattened without breaking, characterized by a thickness of the tablet or of the individual multi-particulates after flattening which corresponds to about ≤60% of the thickness of the tablet or of the individual multi-particulates before flattening. In the dosage form, the flattened tablet or flattened multi-particulates provide an in vitro dissolution rate, when measured in a USP Apparatus 1 (basket) at 100 rpm in 900 mL simulated gastric fluid without enzymes (SGF) at 37°C, characterized by the percent amount of an active agent released at 0.5 h of the dissolution that deviates no more than about 20% points from the corresponding in vitro dissolution rate of a non-flattened reference tablet or non-flattened reference multi-particulates.
摘要翻译：要解决的问题：提供包含阿片类镇痛剂的防篡改剂型，以提供其制备方法，并提供其使用和治疗方法。提供了一种控释型固体口服药物剂型，其包含片剂或多颗粒形式的受控释放基质制剂作为对象。片剂或单个多颗粒可以至少平坦化而不破裂，其特征在于片剂或扁平化后的单个多颗粒的厚度对应于片剂或单个多颗粒的厚度的约≤60％压扁之前的颗粒物在剂型中，当在USP装置1（篮）中以100rpm在37℃下在900mL不含酶（SGF）的模拟胃液中测量时，扁平片或扁平多颗粒提供体外溶出速率，其特征在于通过溶解0.5小时释放的活性剂的百分数，其偏离不相对于未平坦化参考片或非扁平参考多颗粒的体外溶出速率的不超过约20％的点。版权所有（C）2013，JPO＆INPIT

6. 发明专利

JP2012136543A Tamper-resistant oral pharmaceutical dosage form comprising opioid analgesic 有权
标题翻译：抗抑郁药物口服药物形式包含OPIOID ANALGESIC
公开(公告)号：JP2012136543A
公开(公告)日：2012-07-19
申请号：JP2012045261
申请日：2012-03-01
申请人： Purdue Pharma Lp , パーデュー、ファーマ、リミテッド、パートナーシップ
发明人： MANNION RICHARD OWEN , O'DONNELL EDWARD PATRICK , MCKENNA WILLIAM HENRY , HUANG HAIYONG HUGH
IPC分类号： A61K9/22 , A61K9/26 , A61K9/28 , A61K31/4468 , A61K31/485 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/26 , A61K47/32 , A61K47/34 , A61P25/04
CPC分类号： A61K9/2027 , A61J3/005 , A61J3/06 , A61J3/10 , A61K9/0002 , A61K9/0053 , A61K9/1641 , A61K9/2013 , A61K9/2018 , A61K9/2031 , A61K9/2054 , A61K9/2072 , A61K9/2077 , A61K9/209 , A61K9/2095 , A61K9/28 , A61K9/284 , A61K9/2853 , A61K9/2866 , A61K9/2893 , A61K31/485 , A61K45/06 , A61K47/10 , A61K47/34 , B29B7/02 , B29B7/88 , B29C35/045 , B29C35/16 , B29C37/0025 , B29C43/003 , B29C43/02 , B29C43/52 , B29C71/00 , B29C71/009 , B29C2035/046 , B29C2035/1658 , B29K2071/02 , B29K2105/0035 , B29K2105/251 , B29K2995/0088 , B29L2031/753
摘要： PROBLEM TO BE SOLVED: To provide a tamper-resistant dosage form of an opioid analgesic, etc., and production methods, uses, and treatment methods thereof.SOLUTION: The present invention is directed to a solid oral extended release pharmaceutical dosage form comprising an extended release matrix formulation in the form of a tablet or multi-particulates, wherein the tablet or the individual multi-particulates can at least be flattened without breaking, characterized by a thickness of the tablet or the individual multi-particulate after the flattening which corresponds to no more than about 60% of the thickness of the tablet or the individual multi-particulate before flattening, and wherein the flattened tablet or the flattened multi-particulates provide an in-vitro dissolution rate, when measured in a USP (United States Pharmacopeia) apparatus 1 (basket) at 100 rpm in 900 mL simulated gastric fluid (SGF) without enzymes at 37°C characterized by the percent amount of active agent released at 0.5 hours of dissolution that deviates no more than a limit of about 20% from the corresponding in-vitro dissolution rate of a non flattened reference tablet or non flattened reference multi-particulates.
摘要翻译：要解决的问题：提供阿片样镇痛剂等的抗篡改剂型及其制备方法，用途和治疗方法。解决方案：本发明涉及一种固体口服延长释放药物剂型，其包含片剂或多颗粒形式的延长释放基质制剂，其中片剂或单个多微粒可以至少被平坦化不破裂，其特征在于平整后的片剂或单个多颗粒的厚度，其对应于在平坦化之前片剂或单个多颗粒的厚度不超过约60％，并且其中扁平片剂或当在USP（美国药典）设备1（篮子）中以100rpm在900mL不含酶的900mL模拟胃液（SGF）中测量时，扁平多颗粒提供体外溶出速率，其特征在于百分比量在0.5小时溶解时释放出的活性剂，其偏差不超过相对于非扁平化参考的体外溶出速率约20％的极限包含片剂或非扁平参考多颗粒物。版权所有（C）2012，JPO＆INPIT

7. 发明专利

JP2010189403A Tamper-resistant transdermal opioid delivery devices 有权
标题翻译：防篡改传感器输送装置
公开(公告)号：JP2010189403A
公开(公告)日：2010-09-02
申请号：JP2010075835
申请日：2010-03-29
申请人： Purdue Pharma Lp , パーデュー、ファーマ、リミテッド、パートナーシップ
发明人： SHEVCHUK IHOR , CASSIDY JAMES P , REIDENBERG BRUCE , SHARP DALE E , KUPPER ROBERT J
IPC分类号： A61K45/06 , A61K9/70 , A61K31/4468 , A61K31/485 , A61P25/04 , A61P25/36 , A61P43/00 , C07D489/08
CPC分类号： A61K9/7084 , A61K31/485 , A61K45/06 , C07D489/08 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide a tamper-resistant transdermal opioid delivery device which includes opioid or a pharmaceutical acceptable salt thereof, and an acyl opioid antagonist or a pharmaceutical acceptable salt thereof. SOLUTION: The transdermal delivery device includes: an analgesically effective amount of the opioid or the pharmaceutical acceptable salt thereof; and, when the transdermal delivery device is used as indicated and if a detectable amount does not permeate human's skin, and after the transdermal delivery device is misused and the absorption into human's blood flow has occurred, the acyl opioid antagonist or the pharmaceutical acceptable salt thereof which exists in the transdermal delivery device in an amount enough to control an inebriety effect of the opioid or the pharmaceutical acceptable salt thereof. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供包含阿片样物质或其药学上可接受的盐的抗篡改的透皮阿片样物质递送装置和酰基阿片样物质拮抗剂或其药学上可接受的盐。透皮递送装置包括：止痛有效量的阿片样物质或其药学上可接受的盐; 并且当如所述使用透皮递送装置时，如果可检测量不渗透人的皮肤，并且在透皮递送装置误用并且已经发生对人的血流的吸收之后，则该酰基阿片样物质拮抗剂或其药学上可接受的盐其以足以控制阿片样物质或其药学上可接受的盐的饮酒效果的量存在于透皮递送装置中。版权所有（C）2010，JPO＆INPIT

8. 发明专利

JP2014015465A Trpv1 antagonist and use thereof 审中-公开
标题翻译： TRPV1拮抗剂及其用途
公开(公告)号：JP2014015465A
公开(公告)日：2014-01-30
申请号：JP2013156236
申请日：2013-07-29
申请人： Purdue Pharma Lp , パーデュー、ファーマ、リミテッド、パートナーシップ , Shionogi & Co Ltd , 塩野義製薬株式会社
发明人： TAFESSE LAYKEA , KUROSE NORIYUKI
IPC分类号： C07D213/74 , A61K31/4545 , A61K31/496 , A61P1/00 , A61P1/04 , A61P13/00 , A61P25/04 , A61P43/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D407/14 , C07D417/12 , C07D417/14 , C12N15/09
CPC分类号： C07D401/04 , C07D213/61 , C07D213/72 , C07D213/74 , C07D401/12 , C07D401/14 , C07D405/14 , C07D407/14 , C07D417/12 , C07D417/14
摘要： PROBLEM TO BE SOLVED: To provide a new drug for treating or preventing pain, UI, an ulcer, IBD and IBS.SOLUTION: Provided are a compound represented by the following formula I [where X represents O, S, N-CN, N-OH, or N-OR10, W represents N or C, Rrepresents hydrogen atom, hydroxy group, -OCF3, -halogen atom and the like, Arrepresents a specific 6-membered ring containing a nitrogen atom, Arrepresents a specific heterocycle and the like, each Rindependently represents hydrogen atom, an alkyl group and the like, each Rindependently represents hydrogen atom, an alkyl group and the like] and a pharmaceutical composition containing the compound. Effect of the invention is that the compound is useful for treating or preventing pain, UI, an ulcer, IBD, and IBS by inhibiting a function of Transient Receptor Potential Vanilloid 1 in a cell.
摘要翻译：要解决的问题：提供治疗或预防疼痛，UI，溃疡，IBD和IBS的新药。解决方案：提供由下式I表示的化合物[其中X表示O，S，N-CN，N -OH或N-OR 10，W表示N或C，R表示氢原子，羟基，-OCF 3，卤素原子等，Ar表示含有氮原子的特定6元环，Ar表示特定的杂环等中，R 1各自独立地表示氢原子，烷基等，各自独立地表示氢原子，烷基等]和含有该化合物的药物组合物。本发明的效果是该化合物可用于通过抑制细胞中瞬时受体电位香草酸1的功能来治疗或预防疼痛，UI，溃疡，IBD和IBS。

9. 发明专利

JP2012236835A Tamper resistant oral pharmaceutical dosage form comprising opioid analgesic 有权
标题翻译：抗抑郁药物口服药物形式包含OPIOID ANALGESIC
公开(公告)号：JP2012236835A
公开(公告)日：2012-12-06
申请号：JP2012157157
申请日：2012-07-13
申请人： Purdue Pharma Lp , パーデュー、ファーマ、リミテッド、パートナーシップ
发明人： MANNION RICHARD OWEN , O'DONNELL EDWARD PATRICK , MCKENNA WILLIAM HENRY , HUANG HAIYONG HUGH
IPC分类号： A61K9/22 , A61K9/20 , A61K9/32 , A61K31/485 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/34 , A61P29/00
CPC分类号： A61K9/2027 , A61J3/005 , A61J3/06 , A61J3/10 , A61K9/0002 , A61K9/0053 , A61K9/1641 , A61K9/2013 , A61K9/2018 , A61K9/2031 , A61K9/2054 , A61K9/2072 , A61K9/2077 , A61K9/209 , A61K9/2095 , A61K9/28 , A61K9/284 , A61K9/2853 , A61K9/2866 , A61K9/2893 , A61K31/485 , A61K45/06 , A61K47/10 , A61K47/34 , B29B7/02 , B29B7/88 , B29C35/045 , B29C35/16 , B29C37/0025 , B29C43/003 , B29C43/02 , B29C43/52 , B29C71/00 , B29C71/009 , B29C2035/046 , B29C2035/1658 , B29K2071/02 , B29K2105/0035 , B29K2105/251 , B29K2995/0088 , B29L2031/753
摘要： PROBLEM TO BE SOLVED: To provide a pharmaceutical dosage, for example a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment.SOLUTION: The process of preparing a solid oral extended release pharmaceutical dosage form, comprising at least the steps of: (a) combining (1) at least one polyethylene oxide having, based on rheological measurements, an approximate molecular weight of at least 1,000,000, and (2) at least one active agent, to form a composition; (b) shaping the composition to form an extended release matrix formulation; and (c) curing the extended release matrix formulation including at least a curing step of subjecting the extended release matrix formulation to a temperature which is at least the softening temperature of the polyethylene oxide for a time period of at least about 1 minute.
摘要翻译：要解决的问题：提供药物剂量，例如包括阿片样镇痛剂的防篡改剂型，以及制备，使用和治疗方法。解决方案：制备固体口服延长释放药物剂型的方法，至少包括以下步骤：（a）将（1）至少一种聚环氧乙烷与基于流变学测量值的近似分子量至少1,000,000，和（2）至少一种活性剂，形成组合物; （b）使组合物成形以形成延长释放基质制剂; 和（c）固化延长释放基质制剂，其包括至少一种固化步骤，其将延长释放基质制剂的温度至少达到聚环氧乙烷的软化温度至少约1分钟的时间。版权所有（C）2013，JPO＆INPIT

10. 发明专利

JP2012229249A Tamper-resistant oral pharmaceutical dosage form comprising opioid analgesic 审中-公开
标题翻译：抗抑郁药物口服药物形式包含OPIOID ANALGESIC
公开(公告)号：JP2012229249A
公开(公告)日：2012-11-22
申请号：JP2012157158
申请日：2012-07-13
申请人： Purdue Pharma Lp , パーデュー、ファーマ、リミテッド、パートナーシップ
发明人： MANNION RICHARD OWEN , O'DONNELL EDWARD PATRICK , MCKENNA WILLIAM HENRY , HUANG HAIYONG HUGH
IPC分类号： A61K9/22 , A61K9/16 , A61K9/24 , A61K9/32 , A61K31/485 , A61K45/00 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/26 , A61K47/32 , A61K47/34 , A61P25/04 , A61P29/02
CPC分类号： A61K9/2027 , A61J3/005 , A61J3/06 , A61J3/10 , A61K9/0002 , A61K9/0053 , A61K9/1641 , A61K9/2013 , A61K9/2018 , A61K9/2031 , A61K9/2054 , A61K9/2072 , A61K9/2077 , A61K9/209 , A61K9/2095 , A61K9/28 , A61K9/284 , A61K9/2853 , A61K9/2866 , A61K9/2893 , A61K31/485 , A61K45/06 , A61K47/10 , A61K47/34 , B29B7/02 , B29B7/88 , B29C35/045 , B29C35/16 , B29C37/0025 , B29C43/003 , B29C43/02 , B29C43/52 , B29C71/00 , B29C71/009 , B29C2035/046 , B29C2035/1658 , B29K2071/02 , B29K2105/0035 , B29K2105/251 , B29K2995/0088 , B29L2031/753
摘要： PROBLEM TO BE SOLVED: To provide a controlled release oral pharmaceutical dosage form comprising an active agent which is tamper resistant, and to provide a method for preparing the same.SOLUTION: There is provided a method for preparing a controlled release solid oral pharmaceutical dosage form including at least the steps of: (a) a step of combining at least one polyethylene oxide having, based on (1) rheological measurements, an approximate molecular weight of at least 1,000,000, and (2) at least one active agent, to form a composition; (b) a step of shaping the composition, to form a controlled release matrix formulation; and (c) a curing step of subjecting the controlled release matrix formulation to a temperature which is at least the softening temperature of the polyethylene oxide for a time period of at least about 1 min; and comprising at least a step of curing the controlled release matrix formulation. Furthermore, there is provided the extended release oral pharmaceutical dosage form. The active agent is preferably an opioid analgesic, especially oxycodone hydrochloride.
摘要翻译：要解决的问题：提供包含抗篡改活性剂的控释口服药物剂型，并提供其制备方法。提供了一种制备控释固体口服药物剂型的方法，其包括至少以下步骤：（a）将至少一种聚环氧乙烷与（1）流变学测量结合的步骤，近似分子量为至少1,000,000，和（2）至少一种活性剂，以形成组合物; （b）使组合物成形以形成控释基质制剂的步骤; 和（c）固化步骤，将控释基质制剂的温度至少达到聚环氧乙烷的软化温度至少约1分钟; 并且包括至少固化控释基质制剂的步骤。此外，提供了延长释放的口服药物剂型。活性剂优选为阿片类止痛剂，特别是盐酸羟考酮。版权所有（C）2013，JPO＆INPIT

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