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21. 发明授权

US5958459A Opioid formulations having extended controlled released 失效
标题翻译：具有延长受控释放的阿片制剂
公开(公告)号：US5958459A
公开(公告)日：1999-09-28
申请号：US561829
申请日：1995-11-27
申请人： Mark Chasin , Benjamin Oshlack , Frank Pedi, Jr.
发明人： Mark Chasin , Benjamin Oshlack , Frank Pedi, Jr.
IPC分类号： A61K9/14 , A61K9/16 , A61K9/36 , A61K9/62
CPC分类号： A61K9/14 , A61K9/16
摘要： Solid controlled-release oral dosage forms comprising a therapeutically effective amount of an opioid analgesic or a salt thereof which provide an extended duration of pain relief of about 24 hours, have a dissolution rate in-vitro of the dosage form, when measured by the USP Paddle Method of 100 rpm in 900 ml aqueous buffer at 37.degree. C. from about 12.5% to about 42.5% (by weight) active agent released after 1 hour, from about 25% to about 55% (by weight) active agent released after 2 hours, from about 45% to about 75% (by weight) opioid analgesic released after 4 hours and greater than about 60% (by weight) opioid analgesic released after 8 hours, the in-vitro release rate being substantially independent of pH and chosen such that the peak plasma level of active agent obtained in-vivo between about 2 and about 8 hours after administration of the dosage form.
摘要翻译：包含治疗有效量的阿片类止痛剂或其盐的固体控制释放口服剂型提供延长的疼痛缓解时间约24小时，当通过USP测量时具有剂型的体外溶出速率桨式法在900ml含水缓冲液中于37℃从约12.5％至约42.5％（重量）的活性剂在1小时后释放，约25％至约55％（重量）的活性剂释放出来后释放 2小时，约4小时后释放大约45％至大约75％（重量）的阿片样物质止痛剂，并且在8小时后释放大于约60％（重量）的阿片类止痛剂，体外释放速率基本上不依赖于pH和选择使得在施用剂型后约2至约8小时之间在体内获得的活性剂的血浆水平峰值。

22. 发明授权

US5958452A Extruded orally administrable opioid formulations 失效
标题翻译：挤压口服阿片制剂
公开(公告)号：US5958452A
公开(公告)日：1999-09-28
申请号：US833948
申请日：1997-04-10
申请人： Benjamin Oshlack , Mark Chasin , Hua-Pin Huang
发明人： Benjamin Oshlack , Mark Chasin , Hua-Pin Huang
IPC分类号： A61K20060101 , A61K9/14 , A61K9/16 , A61K9/20 , A61K9/22 , A61K9/26 , A61K9/52 , A61K31/135 , A61K31/485 , A61K47/00 , A61K47/10 , A61K47/12 , A61K47/32 , A61K47/38 , A61K47/44 , A61K47/46
CPC分类号： A61K9/1635 , A61K9/1617 , A61K9/1652 , A61K9/1694 , A61K9/2018 , A61K9/2027 , A61K9/2077 , A61K9/2081 , A61K9/2095 , A61K9/145 , Y10S514/951 , Y10S514/962
摘要： Bioavailable sustained release oral opioid analgesic dosage forms, comprising a plurality of multiparticulates produced via melt extrusion techniques are disclosed.
摘要翻译：公开了包含通过熔融挤出技术生产的多个多颗粒的生物可用持续释放口服阿片类镇痛剂型。

23. 发明授权

US08518443B2 Opioid agonist formulations with releasable and sequestered antagonist 有权
公开(公告)号：US08518443B2
公开(公告)日：2013-08-27
申请号：US13535605
申请日：2012-06-28
申请人： Christopher Breder , Curtis Wright , Benjamin Oshlack
发明人： Christopher Breder , Curtis Wright , Benjamin Oshlack
IPC分类号： A61K9/20
CPC分类号： A61K9/2077 , A61K9/14 , A61K9/1635 , A61K9/1647 , A61K9/167 , A61K9/2009 , A61K9/2013 , A61K9/2027 , A61K9/2054 , A61K9/2081 , A61K9/2086 , A61K9/5026 , A61K9/5078 , A61K9/5084 , A61K31/44 , A61K31/445 , A61K31/46 , A61K31/485 , A61K45/06 , A61K47/32 , A61K47/38 , A61K2300/00
摘要： Disclosed are oral dosage forms, comprising (i) a therapeutically effective amount of an opioid agonist; (ii) an opioid antagonist in releasable form; and (iii) a sequestered opioid antagonist which is not released when the dosage form is administered intact, and methods thereof.

24. 发明申请

US20120288565A1 TAMPER-RESISTANT ORAL OPIOID AGONIST FORMULATIONS 有权
标题翻译：抗痉挛性口服阿片类药物激素制剂
公开(公告)号：US20120288565A1
公开(公告)日：2012-11-15
申请号：US13544333
申请日：2012-07-09
申请人： Benjamin Oshlack , Curtis Wright , J. David Haddox
发明人： Benjamin Oshlack , Curtis Wright , J. David Haddox
IPC分类号： A61K9/00 , A61K9/14 , A61P25/04 , A61K31/485
CPC分类号： A61K9/5084 , A61K9/0043 , A61K9/0053 , A61K9/006 , A61K9/02 , A61K9/14 , A61K9/1617 , A61K9/1635 , A61K9/1647 , A61K9/1676 , A61K9/1694 , A61K9/2077 , A61K9/2081 , A61K9/2866 , A61K9/4808 , A61K9/50 , A61K9/501 , A61K9/5015 , A61K9/5026 , A61K9/5031 , A61K9/5078 , A61K9/51 , A61K9/7053 , A61K9/7061 , A61K31/485
摘要： Disclosed is an oral dosage form comprising: (i) an opioid agonist in releasable form and (ii) a sequestered opioid antagonist which is not released when the dosage form is administered orally intact.
摘要翻译：公开了口服剂型，其包含：（i）可释放形式的阿片样物质激动剂和（ii）当所述剂型口服完整时不释放的螯合阿片样物质拮抗剂。

25. 发明申请

US20110262532A1 Controlled Release Hydrocodone Formulations 有权
标题翻译：控释氢可酮配方
公开(公告)号：US20110262532A1
公开(公告)日：2011-10-27
申请号：US12982386
申请日：2010-12-30
申请人： Benjamin Oshlack , Hua-Pin Huang , John Masselink , Alfred P. Tonelli
发明人： Benjamin Oshlack , Hua-Pin Huang , John Masselink , Alfred P. Tonelli
IPC分类号： A61K9/48 , A61P25/04 , A61K31/485
CPC分类号： A61K31/485 , A61K9/0053 , A61K9/0087 , A61K9/1617 , A61K9/1635 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2031 , A61K9/2054 , A61K9/2077 , A61K9/2081 , A61K9/282 , A61K9/2846 , A61K9/4808 , A61K9/4866 , A61K9/50 , A61K9/5026
摘要： A solid oral controlled-release oral dosage form of hydrocodone is disclosed. The dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a sufficient amount of a controlled release material to render the dosage form suitable for twice-a-day administration to a human patient, the dosage form providing a C12/Cmax ratio of 0.55 to 0.85, said dosage form providing a therapeutic effect for at least about 12 hours.
摘要翻译：公开了一种固体口服缓释口服剂型的氢可酮。包含镇痛有效量的氢可酮或其药学上可接受的盐的剂型和足够量的控制释放材料以使剂型适合于每天两次给予人类患者，所述剂型提供C12 / Cmax比为0.55至0.85，所述剂型提供至少约12小时的治疗效果。

26. 发明授权

US07842309B2 Tamper-resistant oral opioid agonist formulations 有权
标题翻译：遏制抗性口服阿片样物质激动剂配方
公开(公告)号：US07842309B2
公开(公告)日：2010-11-30
申请号：US10700861
申请日：2003-11-04
申请人： Benjamin Oshlack , Curtis Wright , J. David Haddox
发明人： Benjamin Oshlack , Curtis Wright , J. David Haddox
IPC分类号： A61K9/24 , A61K9/20 , A61K9/22
CPC分类号： A61K9/5084 , A61K9/0043 , A61K9/0053 , A61K9/006 , A61K9/02 , A61K9/14 , A61K9/1617 , A61K9/1635 , A61K9/1647 , A61K9/1676 , A61K9/1694 , A61K9/2077 , A61K9/2081 , A61K9/2866 , A61K9/4808 , A61K9/50 , A61K9/501 , A61K9/5015 , A61K9/5026 , A61K9/5031 , A61K9/5078 , A61K9/51 , A61K9/7053 , A61K9/7061 , A61K31/485
摘要： Disclosed is an oral dosage form comprising (i) an opioid agonist in releasable form and (ii) a sequestered opioid antagonist which is substantially not released when the dosage form is administered intact.
摘要翻译：公开了一种口服剂型，其包含（i）可释放形式的阿片样物质激动剂和（ii）当所述剂型完整施用时基本上不释放的螯合阿片样物质拮抗剂。

27. 发明授权

US07842307B2 Pharmaceutical formulation containing opioid agonist, opioid antagonist and gelling agent 有权
标题翻译：含阿片样物质激动剂，阿片拮抗剂和胶凝剂的药物制剂
公开(公告)号：US07842307B2
公开(公告)日：2010-11-30
申请号：US10214413
申请日：2002-08-06
申请人： Benjamin Oshlack , Curtis Wright , Christopher Breder
发明人： Benjamin Oshlack , Curtis Wright , Christopher Breder
IPC分类号： A61K9/127
CPC分类号： A61K31/485 , A61K9/0053 , A61K9/1635 , A61K9/1647 , A61K9/2027 , A61K9/205 , A61K9/2081 , A61K9/5078 , A61K47/10 , A61K47/32 , A61K47/36
摘要： Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of an opioid analgesic, an opioid antagonist and one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid.
摘要翻译：在某些实施方案中公开的是口服剂型，其包含治疗有效量的阿片类止痛剂，阿片样物质拮抗剂和一种或多种药学上可接受的赋形剂; 所述剂型还包括有效量的胶凝剂，以使得不适于施用的粘度，所述粘度选自肠胃外和鼻内施用于当所述剂型粉碎时形成的溶解混合物，并与约0.5至约10ml 的水性液体。

28. 发明授权

US07790215B2 Sustained-release gel coated compositions 有权
标题翻译：持续释放凝胶涂层组合物
公开(公告)号：US07790215B2
公开(公告)日：2010-09-07
申请号：US10401111
申请日：2003-03-26
申请人： Richard S. Sackler , Benjamin Oshlack , Curtis Wright
发明人： Richard S. Sackler , Benjamin Oshlack , Curtis Wright
IPC分类号： A61J3/00
CPC分类号： A61K9/2077 , A61K9/1635 , A61K9/1658 , A61K9/2846 , A61K9/2866 , A61K9/2873 , A61K9/5078 , A61K31/485
摘要： Disclosed in certain embodiments is a coating comprising a pharmaceutically acceptable mixture of gelatin and hydrophobic polymer.
摘要翻译：在某些实施方案中公开了包含明胶和疏水性聚合物的药学上可接受的混合物的涂层。

29. 发明申请

US20100092570A1 CONTROLLED RELEASE OXYCODONE COMPOSITIONS 审中-公开
标题翻译：受控释放的氧化钙组合物
公开(公告)号：US20100092570A1
公开(公告)日：2010-04-15
申请号：US12579805
申请日：2009-10-15
申请人： Benjamin Oshlack , Mark Chasin , John Joseph Minogue , Robert Francis Kaiko
发明人： Benjamin Oshlack , Mark Chasin , John Joseph Minogue , Robert Francis Kaiko
IPC分类号： A61K9/14 , A61K31/34
CPC分类号： A61K9/5026 , A61K9/2081 , A61K31/485
摘要： A method for substantially reducing the range in daily dosages required to control pain in approximately 90% of patients is disclosed whereby an oral solid controlled release dosage formulation having from about 10 to about 40 mg of oxycodone or a salt thereof is administered to a patient. The formulation provides a mean maximum plasma concentration of oxycodone from about 6 to about 60 ng/ml from a mean of about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration from about 3 to about 30 ng/ml from about 10 to about 14 hours after repeated “q12h” (i.e., every 12 hour) administration through steady-state conditions. Another embodiment is directed to a method for substantially reducing the range in daily dosages required to control pain in substantially all patients by administering an oral solid controlled release dosage formulation comprising up to about 160 mg of oxycodone or a salt thereof, such that a mean maximum plasma concentration of oxycodone up to about 240 ng/ml from a mean of up to about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration up to about 120 ng/ml from about 10 to about 14 hours after repeated “q12h” (i.e., every 12 hour) administration through steady-state conditions are achieved. Controlled release oxycodone formulations for achieving the above are also disclosed.
摘要翻译：公开了一种用于大大减少约90％患者中控制疼痛所需的日剂量范围的方法，其中向患者施用具有约10至约40mg羟可待酮或其盐的口服固体控释剂量制剂。所述制剂提供给药后平均约2至约4.5小时约6至约60ng / ml的羟考酮的平均最大血浆浓度，并且平均最小血浆浓度为约3至约30ng / ml，约10 通过稳态条件重复“q12h”（即每12小时）至约14小时。另一个实施方案涉及通过施用包含高达约160mg羟考酮或其盐的口服固体控制释放剂量制剂来显着降低在基本上所有患者中控制疼痛所需的日剂量范围的方法，使得平均最大值在给药后平均高达约2至约4.5小时，羟考酮的血浆浓度高达约240ng / ml，重复“q12h”后约10至约14小时的平均最小血浆浓度高达约120ng / ml “（即每12小时一次）通过稳态条件实现。还公开了用于实现上述目标的控释羟考酮制剂。

30. 发明申请

US20080044482A1 ORALLY ADMINISTRABLE OPIOID FORMULATIONS HAVING EXTENDED DURATION OF EFFECT 审中-公开
公开(公告)号：US20080044482A1
公开(公告)日：2008-02-21
申请号：US11856610
申请日：2007-09-17
申请人： Benjamin Oshlack , Mark Chasin
发明人： Benjamin Oshlack , Mark Chasin
IPC分类号： A61K31/55 , A61K31/135 , A61K31/137 , A61K31/195 , A61K31/196 , A61K31/197 , A61K31/381 , A61K31/40 , A61K31/4015 , A61K31/405 , A61K31/4152 , A61K31/42 , A61K31/436 , A61K31/4412 , A61K31/445 , A61K31/485 , A61K31/5377 , A61K31/54 , A61K9/16 , A61P43/00
CPC分类号： A61K9/1635 , A61K9/1617 , A61K9/1623 , A61K9/2013 , A61K9/2054 , A61K9/2072 , A61K9/2077 , A61K9/2081 , A61K9/2095 , A61K9/2846 , A61K9/2866 , A61K9/5026 , A61K9/5047 , A61K9/5078 , A61K31/485 , A61K31/522 , Y10S514/951
摘要： Sustained release oral solid dosage forms of opioid analgesics are provided as multiparticulate systems which are bioavailable and which provide effective blood levels of the opioid analgesic for at least about 24 hours. A unit dose of the opioid analgesic contains a plurality of substrates including the opioid analgesic in sustained release form. The substrates have a diameter from about 0.1 mm to about 3 mm.

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