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41. 发明授权

US5266331A Controlled release oxycodone compositions 失效
标题翻译：对照释放羟考酮组合物
公开(公告)号：US5266331A
公开(公告)日：1993-11-30
申请号：US800549
申请日：1991-11-27
申请人： Benjamin Oshlack , John J. Minogue , Mark Chasin
发明人： Benjamin Oshlack , John J. Minogue , Mark Chasin
IPC分类号： A61K9/16 , A61K20060101 , A61K9/20 , A61K9/22 , A61K9/26 , A61K9/28 , A61K9/30 , A61K9/58 , A61K31/485 , A61K47/30 , A61K47/32 , A61K47/38 , A61P20060101 , A61P25/04
CPC分类号： A61K9/2013 , A61K31/485 , A61K9/2027 , A61K9/2054 , A61K9/2081 , A61K9/5015
摘要： A solid controlled release, oral dosage form, the dosage form comprising a therapeutically effective amount of oxycodone or a salt thereof in a matrix wherein the dissolution rate in vitro of the dosage form, when measured by the USP Paddle Method of 100 rpm in 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37.degree. C. is between 12.5% and 42.5% (by weight) oxycodone released after 1 hour, between 25% and 55% (by weight) oxycodone released after 2 hours, between 45% and 75% (by weight) oxycodone released after 4 hours and between 55% and 85% (by weight) oxycodone released after 6 hours, the in vitro release rate being independent of pH between pH 1.6 and 7.2 and chosen such that the peak plasma level of oxycodone obtained in vivo occurs between 2 and 4 hours after administration of the dosage form.
摘要翻译：固体控制释放的口服剂型，所述剂型包含基质中治疗有效量的羟考酮或其盐，其中当通过USP桨法以100rpm在900ml中测量时，剂型的体外溶出速率在37℃下的水性缓冲液（pH在1.6和7.2之间）在1小时后释放的羟考酮的12.5％至42.5％（重量），2小时后释放的羟考酮的25％至55％（重量），45％和4小时后释放的75％（重量）羟考酮和6小时后释放55％至85％（重量）羟考酮的体外释放速率与pH在1.6至7.2之间的pH无关，并选择使峰值等离子体体内获得的羟考酮水平在施用剂型后2至4小时发生。

42. 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。

43. 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.

44. 发明申请

US20060165791A1 Controlled release oxycodone compositions 审中-公开
标题翻译：对照释放羟考酮组合物
公开(公告)号：US20060165791A1
公开(公告)日：2006-07-27
申请号：US11332632
申请日：2006-01-12
申请人： Benjamin Oshlack , John Minogue , Mark Chasin , Robert Kaiko
发明人： Benjamin Oshlack , John Minogue , Mark Chasin , Robert Kaiko
IPC分类号： A61K31/485 , A61K9/22
CPC分类号： A61K9/2013 , A61K9/2027 , A61K9/2054 , A61K9/2081 , A61K9/5015 , 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 2.40 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：用于大大减少大约减少控制疼痛所需的日剂量范围的方法。公开了90％的患者，其中向患者施用具有约10至约40mg羟考酮或其盐的口服固体控制释放剂量制剂。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，使得平均最大值从给药后至多约2至约4.5小时的平均值，羟考酮的血浆浓度高达约2.40ng / 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。

45. 发明申请

US20060099255A1 Controlled release oxycodone compositions 审中-公开
公开(公告)号：US20060099255A1
公开(公告)日：2006-05-11
申请号：US11303553
申请日：2005-12-16
申请人： Benjamin Oshlack , Mark Chasin , John Minogue , Robert Kaiko
发明人： Benjamin Oshlack , Mark Chasin , John Minogue , Robert Kaiko
IPC分类号： A61K9/22
CPC分类号： A61K9/2013 , A61K9/2027 , A61K9/2054 , A61K9/2081 , A61K9/5015 , 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.

46. 发明授权

US06294195B1 Orally administrable opioid formulations having extended duration of effect 失效
标题翻译：口服给药的阿片制剂具有延长的效果持续时间
公开(公告)号：US06294195B1
公开(公告)日：2001-09-25
申请号：US09390719
申请日：1999-09-07
申请人： Benjamin Oshlack , Mark Chasin
发明人： Benjamin Oshlack , Mark Chasin
IPC分类号： A61K952
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.
摘要翻译：提供阿片类镇痛药的持续释放口服固体剂型作为生物可利用的多颗粒系统，并且提供阿片类止痛剂的有效血液水平至少约24小时。阿片类镇痛剂的单位剂量含有多种底物，包括持续释放形式的阿片样镇痛药。基材的直径为约0.1mm至约3mm。

47. 发明授权

US6143353A Controlled release formulations coated with aqueous dispersions of acrylic polymers 失效
公开(公告)号：US6143353A
公开(公告)日：2000-11-07
申请号：US816023
申请日：1997-03-11
申请人： Benjamin Oshlack , Mark Chasin , Frank Pedi, Jr.
发明人： Benjamin Oshlack , Mark Chasin , Frank Pedi, Jr.
IPC分类号： A61J3/06 , A61J3/00 , A61K9/22 , A61K9/24 , A61K9/28 , A61K9/32 , A61K9/50 , A61K9/52 , A61K9/54 , A61K9/56 , A61K9/58 , A61K9/62 , A61M37/00
CPC分类号： A61K9/2846 , A61K9/5026 , A61K9/5078
摘要： A stable solid controlled release formulation having a coating derived from an aqueous dispersion of a hydrophobic acrylic polymer includes a substrate including an active agent selected from the group consisting of a systemically active therapeutic agent, a locally active therapeutic agent, a disinfecting and sanitizing agent, a cleansing agent, a fragrance agent and a fertilizing agent, overcoated with an aqueous dispersion of the plasticized water-insoluble acrylic polymer. The formulation provides a stable dissolution of the active agent which is unchanged after exposure to accelerated storage conditions.

48. 发明授权

US6129933A Stabilized controlled release substrate having a coating derived from an aqueous dispersion of hydrophobic polymer 失效
标题翻译：具有由疏水性聚合物的水分散体衍生的涂层的稳定的控释基材
公开(公告)号：US6129933A
公开(公告)日：2000-10-10
申请号：US899924
申请日：1997-07-24
申请人： Benjamin Oshlack , Mark Chasin , Frank Pedi, Jr.
发明人： Benjamin Oshlack , Mark Chasin , Frank Pedi, Jr.
IPC分类号： A61K9/16 , A61K9/20 , A61K9/28 , A61K9/50 , A61K9/52 , A61K31/485 , A61K31/522 , A61K9/62
CPC分类号： A61K9/5089 , A61K31/485 , A61K31/522 , A61K9/1617 , A61K9/1635 , A61K9/2013 , A61K9/2054 , A61K9/2072 , A61K9/2081 , A61K9/2095 , A61K9/2866 , A61K9/5078
摘要： A stabilized solid controlled release dosage form having a coating derived from an aqueous dispersion of ethylcellulose is obtained by overcoating a substrate including a therapeutically active with an aqueous dispersion of ethylcellulose and then curing the coated substrate at a temperature and relative humidity elevated to a suitable level above ambient conditions until the coated dosage form attains a stabilized dissolution profile substantially unaffected by exposure to storage conditions of elevated temperature and/or elevated relative humidity.
摘要翻译：具有衍生自乙基纤维素的水性分散体的涂层的稳定的固体控制释放剂型通过用包含乙基纤维素的水分散体的包含治疗活性的底物进行涂覆，然后在温度和相对湿度升高至适当水平的条件下固化所涂覆的基底直到涂覆的剂型达到稳定的溶解曲线，其基本上不受暴露于升高的温度和/或相对湿度升高的储存条件的影响。

49. 发明授权

US6103261A Opioid formulations having extended controlled release 有权
标题翻译：具有延长受控释放的阿片制剂
公开(公告)号：US6103261A
公开(公告)日：2000-08-15
申请号：US225959
申请日：1999-01-06
申请人： Mark Chasin , Benjamin Oshlack , Frank Pedi, Jr.
发明人： Mark Chasin , Benjamin Oshlack , Frank Pedi, Jr.
IPC分类号： A61K9/52 , A61K9/16 , A61K9/20 , A61K9/22 , A61K9/28 , A61K9/50 , A61K31/445 , A61K31/485 , A61K31/522 , A61K47/32 , A61K47/36 , A61K47/38 , A61K47/42 , A61K47/44 , A61P25/04
CPC分类号： A61K9/1635 , A61K31/485 , A61K31/522 , A61K9/1617 , A61K9/2013 , A61K9/2054 , A61K9/2072 , A61K9/2081 , A61K9/2095 , A61K9/2866 , A61K9/5078
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 a 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，4小时后释放的约45％至约75％（重量）的阿片样物质止痛剂，并且大约约60％（重量）阿片类镇痛剂在一小时后释放，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。

50. 发明授权

US5580578A Controlled release formulations coated with aqueous dispersions of acrylic polymers 失效
公开(公告)号：US5580578A
公开(公告)日：1996-12-03
申请号：US97558
申请日：1993-07-27
申请人： Benjamin Oshlack , Frank Pedi, Jr. , Mark Chasin
发明人： Benjamin Oshlack , Frank Pedi, Jr. , Mark Chasin
IPC分类号： A61J3/06 , A61J3/00 , A61K9/22 , A61K9/24 , A61K9/28 , A61K9/32 , A61K9/50 , A61K9/52 , A61K9/54 , A61K9/56 , A61K9/58 , A61K9/62 , A61M37/00
CPC分类号： A61K9/2846 , A61K9/5026 , A61K9/5078
摘要： A stable solid controlled release formulation having a coating derived from an aqueous dispersion of a hydrophobic acrylic polymer includes a substrate including an active agent selected from the group consisting of a systemically active therapeutic agent, a locally active therapeutic agent, a disinfecting and sanitizing agent, a cleansing agent, a fragrance agent and a fertilizing agent, overcoated with an aqueous dispersion of the plasticized water-insoluble acrylic polymer. The formulation provides a stable dissolution of the active agent which is unchanged after exposure to accelerated storage conditions.

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