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1. 发明申请

US20050192309A1 Method of preventing abuse of opioid dosage forms 审中-公开
标题翻译：防止阿片类药物剂型滥用的方法
公开(公告)号：US20050192309A1
公开(公告)日：2005-09-01
申请号：US10665735
申请日：2003-09-18
申请人： Philip Palermo , Robert Colucci , Robert Kaiko
发明人： Philip Palermo , Robert Colucci , Robert Kaiko
IPC分类号： A61K31/439 , A61K31/44 , A61K31/485 , A61P25/34 , A61P25/36
CPC分类号： A61K31/44 , A61K31/485 , Y10S514/81 , Y10S514/812 , A61K2300/00
摘要： The invention relates in part to a method of reducing the abuse potential of an oral dosage form of an opioid analgesic, wherein an analgesically effective amount of an orally active opioid agonist is combined with an opioid antagonist into an oral dosage form which would require at least a two-step extraction process to be separated from the opioid agonist, the amount of opioid antagonist including being sufficient to counteract opioid effects if extracted together with the opioid agonist and administered parenterally.
摘要翻译：本发明部分地涉及减少口服剂型阿片类止痛剂的滥用潜力的方法，其中止痛有效量的口服活性阿片样物质激动剂与阿片样物质拮抗剂组合成口服剂型，其至少需要与阿片样物质激动剂分离的两步提取过程，阿片样物质拮抗剂的量如果与阿片样物质激动剂一起提取并肠胃外给药，则其量足以抵消阿片样物质的影响。

2. 发明申请

US20070122348A1 Opioid agonist/antagonist combinations 有权
标题翻译：阿片类激动剂/拮抗剂组合
公开(公告)号：US20070122348A1
公开(公告)日：2007-05-31
申请号：US11645401
申请日：2006-12-26
申请人： Robert Kaiko , Robert Colucci
发明人： Robert Kaiko , Robert Colucci
IPC分类号： A61K49/00 , A61K31/60 , A61K31/16 , A61K31/485
CPC分类号： A61K31/485 , A61K31/16 , A61K31/60 , A61K45/06 , Y10S514/81 , Y10S514/812 , A61K2300/00
摘要： The invention is directed in part to oral dosage forms comprising a combination of an orally analgesically effective amount of an opioid agonist and an orally active opioid antagonist, the opioid antagonist being included in a ratio to the opioid agonist to provide a combination product which is analgesically effective when the combination is administered orally, but which is aversive in a physically dependent subject. Preferably, the amount of opioid antagonist included in the combination product provides at least a mildly negative, “aversive” experience in physically dependent addicts (e.g., precipitated abstinence syndrome).
摘要翻译：本发明部分地涉及口服剂型，其包含口服镇痛有效量的阿片样物质激动剂和口服活性阿片样物质拮抗剂的组合，所述阿片样物质拮抗剂以与阿片样物质激动剂的比例包含以提供止痛剂的组合产品当组合口服给药但是在身体依赖的受试者中是厌恶的时候有效。优选地，包括在组合产品中的阿片样物质拮抗剂的量在物理依赖性成瘾者中提供至少轻度，“厌恶”的经验（例如，沉淀的戒断综合征）。

3. 发明申请

US20080075781A1 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：US20080075781A1
公开(公告)日：2008-03-27
申请号：US11804518
申请日：2007-05-17
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： A61K9/16 , A61K31/485 , A61P25/04
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。

4. 发明申请

US20080031963A1 METHOD OF TREATING PAIN BY ADMINISTERING 24 HOUR ORAL OPIOID FORMULATIONS EXHIBITING RAPID RATE OF INITIAL RISE OF PLASMA DRUG LEVEL 审中-公开
标题翻译：通过管理24小时口服阿片类药物治疗疼痛的方法展现血浆药物水平初始升高的快速
公开(公告)号：US20080031963A1
公开(公告)日：2008-02-07
申请号：US11760316
申请日：2007-06-08
申请人： Richard Sackler , Paul Goldenheim , Robert Kaiko
发明人： Richard Sackler , Paul Goldenheim , Robert Kaiko
IPC分类号： A61K9/16 , A61K31/485 , A61K9/52 , A61K9/54 , A61K9/58
CPC分类号： A61K9/5078 , A61K9/2081 , A61K9/4808 , A61K9/5026 , A61K9/5073 , A61K31/485
摘要： Patients are treated with 24-hour oral sustained release opioid formulations which, upon administration, provide an initially rapid opioid absorption such that the minimum effective analgesic concentration of the opioid is more quickly achieved. These sustained release opioid formulations include an effective amount of at least one retardant material to cause said opioid analgesic to be released at a such a rate as to provide an analgesic effect after oral administration to a human patient for at least about 24 hours, and are characterized by providing an absorption half-life from 1 to about 8 hours. A method of titrating a human patient utilizing these sustained release opioid formulations is also disclosed.
摘要翻译：患者用24小时口服持续释放的阿片类药物制剂治疗，其在给药时提供最初快速的阿片样物质吸收，使得阿片样物质的最小有效镇痛浓度更快地达到。这些持续释放的阿片样物质制剂包括有效量的至少一种阻燃剂材料，以使所述阿片样物质镇痛剂以对口服给予人类患者至少约24小时后提供镇痛作用的速率释放，并且分别为其特征在于提供1至约8小时的吸收半衰期。还公开了利用这些持续释放的阿片样物质制剂滴定人类患者的方法。

5. 发明申请

US20060165792A1 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：US20060165792A1
公开(公告)日：2006-07-27
申请号：US11332644
申请日：2006-01-12
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 , B27N3/00
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 reguired to control pain-in-approximately 90% of patients is disclosed whereby an oral solid controlled release dosage formulation having from about 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：公开了一种用于基本上减少在约90％的患者中控制疼痛的日剂量的范围的方法，其中将具有约40mg羟可待酮或其盐的口服固体控制释放剂量制剂施用于患者。所述制剂在施用后从约2至约4.5小时的平均值提供约6至约60ng / ml的羟考酮的平均最大血浆浓度，并且从约3至约30ng / ml的平均最小血浆浓度约为约3至约30ng / 。通过稳态条件重复“q12h”（即每12小时）10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，高达约240ng / ml的羟考酮的血浆浓度高达约120ng / ml，平均最小血浆浓度为约10至约14小时， q12h“（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。

6. 发明申请

US20070275062A1 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：US20070275062A1
公开(公告)日：2007-11-29
申请号：US11728983
申请日：2007-03-26
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 , A61K31/485
CPC分类号： A61K31/485 , A61K9/2081
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。

7. 发明授权

US6143322A Method of treating humans with opioid formulations having extended controlled release 失效
标题翻译：用延长受控释放的阿片样物质制剂治疗人的方法
公开(公告)号：US6143322A
公开(公告)日：2000-11-07
申请号：US838368
申请日：1997-04-08
申请人： Richard Sackler , Robert Kaiko , Paul Goldenheim
发明人： Richard Sackler , Robert Kaiko , Paul Goldenheim
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 , A61K9/58 , A61K9/60
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 at 100 rpm at 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37.degree. C. of from about 12.5% to about 42.5% (by wt) opioid released after 1 hour, from about 25% to about 65% (by wt) opioid released after 2 hours, from about 45% to about 85% (by wt) opioid released after 4 hours, and greater than about 60% (by wt) opioid released after 8 hours, the in-vitro release rate being substantially independent of pH and chosen such that the peak plasma level of said opioid analgesic obtained in-vivo occurs from about 2 to 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方法在900rpm水浴缓冲液（pH1.6和7.2之间），在37℃下，约1小时后释放的约12.5％至约42.5％（重量）的阿片样物质，约25％至约65％ 2小时后释放的阿片样物质，4小时后释放的约45％至约85％的阿片样物质和8小时后释放大于约60重量％的阿片样物质，体外释放速率为基本上不依赖于pH并且选择使得在给药剂型后约2至约8小时发生在体内获得的所述阿片样物质止痛剂的峰值血浆水平。

8. 发明授权

US5478577A Method of treating pain by administering 24 hour oral opioid formulations exhibiting rapid rate of initial rise of plasma drug level 失效
标题翻译：通过施用24小时口服阿片样物质制剂来治疗疼痛的方法，显示血浆药物水平初始升高的速度
公开(公告)号：US5478577A
公开(公告)日：1995-12-26
申请号：US156468
申请日：1993-11-23
申请人： Richard Sackler , Paul Goldenheim , Robert Kaiko
发明人： Richard Sackler , Paul Goldenheim , Robert Kaiko
IPC分类号： A61K9/52 , A61K9/22 , A61K9/50 , A61K9/54 , A61K9/62 , A61K31/485 , A61K45/00 , A61K47/32 , A61K47/38 , A61K47/42 , A61K47/44 , A61K47/46 , A61P25/04 , A61K9/14
CPC分类号： A61K9/5078 , A61K31/485 , A61K9/2081 , A61K9/4808 , A61K9/5026 , A61K9/5073
摘要： Patients are treated with 24-hour oral sustained release opioid formulations which upon administration quickly release an effective portion of the opioid contained therein such that there is an initially more rapid opioid release so that the minimum effective analgesic concentration of the opioid can be more quickly achieved. In the method, the formulations are designed to provide a relatively large peak to trough concentration of the opioid, rather than a flattened serum concentration curve.
摘要翻译：患者用24小时口服持续释放的阿片样物质制剂治疗，其在施用时快速释放其中含有的阿片样物质的有效部分，使得存在最初更快速的阿片样物质释放，使得可以更快地实现阿片样物质的最小有效镇痛浓度。在该方法中，制剂被设计成提供阿片样物质的相对较大的峰谷浓度，而不是平坦的血清浓度曲线。

9. 发明授权

US07740881B1 Method of treating humans with opioid formulations having extended controlled release 失效
标题翻译：用延长受控释放的阿片样物质制剂治疗人的方法
公开(公告)号：US07740881B1
公开(公告)日：2010-06-22
申请号：US09624530
申请日：2000-07-24
申请人： Richard Sackler , Robert Kaiko , Paul Goldenheim
发明人： Richard Sackler , Robert Kaiko , Paul Goldenheim
IPC分类号： A61K9/58 , A61K9/60 , A61K9/36 , A61K9/14 , A61K9/16 , A61K9/62
CPC分类号： A61K31/485 , A61K9/1617 , A61K9/1635 , A61K9/2013 , A61K9/2054 , A61K9/2072 , A61K9/2081 , A61K9/2095 , A61K9/2866 , A61K9/5078 , A61K31/522
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 at 100 rpm at 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37° C. of from about 12.5% to about 42.5% (by wt) opioid released after 1 hour, from about 25% to about 65% (by wt) opioid released after 2 hours, from about 45% to about 85% (by wt) opioid released after 4 hours, and greater than about 60% (by wt) opioid released after 8 hours, the in-vitro release rate being substantially independent of pH and chosen such that the peak plasma level of said opioid analgesic obtained in-vivo occurs from about 2 to 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方法在37℃下以900rpm的水溶液缓冲液（pH在1.6和7.2之间）以约12.5％至约42.5％（以重量计）的阿片样物质在约1小时后释放，约25％至约65％（ 2小时后释放的阿片样物质，4小时后释放的约45％至约85％的阿片样物质和8小时后释放大于约60重量％的阿片样物质，体外释放速率为基本上不依赖于pH并且选择使得在给药剂型后约2至约8小时发生在体内获得的所述阿片样物质止痛剂的峰值血浆水平。

10. 发明申请

US20070275065A1 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：US20070275065A1
公开(公告)日：2007-11-29
申请号：US11824855
申请日：2007-07-03
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： A61K31/34 , A61K9/22
CPC分类号： A61K31/34 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/2081
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：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。所述制剂提供了从施用后约2至约4.5小时的平均值约6至约60ng / ml的羟考酮的平均最大血浆浓度，并且从约3至约30ng / ml的平均最小血浆浓度为约3至约30ng / 重复“q12h”（即每12小时）10〜14小时：通过稳态条件给药。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。

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