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21. 发明申请

US20120191068A1 Methods for Sustained Treatment of Bladder Pain and Irritative Voiding 有权
标题翻译：持续治疗膀胱疼痛和刺激性空洞的方法
公开(公告)号：US20120191068A1
公开(公告)日：2012-07-26
申请号：US13347513
申请日：2012-01-10
申请人： Julie Himes , Dennis Geising , Cheryl Larrivee-Elkins , Michael J. Cima , Purnanand Sarma , Paul Goldenheim
发明人： Julie Himes , Dennis Geising , Cheryl Larrivee-Elkins , Michael J. Cima , Purnanand Sarma , Paul Goldenheim
IPC分类号： A61K31/167 , A61M19/00 , A61M25/00
CPC分类号： A61K31/167 , A61K9/0034 , A61M25/00 , A61M31/002
摘要： Method are provided for treating a patient having bladder pain and/or irritative voiding symptoms. The method includes administering to the patient's bladder lidocaine or another anesthetic agent continuously over a treatment period of 24 hours or more in an amount effective to achieve a therapeutic effect which is sustained beyond the end of the treatment period.
摘要翻译：提供了治疗患有膀胱疼痛和/或刺激性排尿症状的患者的方法。该方法包括在24小时以上的治疗期间连续施用患者膀胱利多卡因或其他麻醉剂，其用量有效地达到治疗期结束以后持续的治疗效果。

22. 发明授权

US06645527B2 Stabilized sustained release tramadol formulations 有权
公开(公告)号：US06645527B2
公开(公告)日：2003-11-11
申请号：US10052844
申请日：2001-10-19
申请人： Benjamin Oshlack , Hua-Pin Huang , Mark Chasin , Paul Goldenheim
发明人： Benjamin Oshlack , Hua-Pin Huang , Mark Chasin , Paul Goldenheim
IPC分类号： A61K922
CPC分类号： A61K9/2054 , A61K9/2013 , A61K9/2095
摘要： A stabilized sustained release oral solid dosage form which includes an effective amount of tramadol or a pharmaceutically acceptable salt thereof dispersed in a matrix of a hydrophobic material comprising a wax-like substance which was melted or softened during the preparation of the matrix, is cured at a temperature from about 35° C. to about 65° C. for a time period from about 4 to about 72 hours, such that the formulation, when subjected to in-vitro dissolution after exposure to accelerated storage conditions of at least one month at 40° C./75% RH, releases an amount of tramadol which does not vary at any given dissolution time point by more than about 20% of the total amount of tramadol released when compared to in-vitro dissolution conducted prior to subjecting the dosage form to the accelerated storage conditions.

23. 发明授权

US5672360A Method of treating pain by administering 24 hour oral opioid formulations 失效
标题翻译：通过施用24小时口服阿片样物质制剂治疗疼痛的方法
公开(公告)号：US5672360A
公开(公告)日：1997-09-30
申请号：US578688
申请日：1996-07-22
申请人： Richard S. Sackler , Robert F. Kaiko , Paul Goldenheim
发明人： Richard S. Sackler , Robert F. Kaiko , Paul Goldenheim
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 , A61K9/16
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, 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： PCT No.PCT / US94 / 13606 Sec。 371日期：1996年7月22日 102（e）日期1996年7月22日PCT 1994年11月22日PCT PCT。出版物WO95 / 14460 日期1995年6月1日患者用24小时口服持续释放阿片样物质制剂治疗，在给药后，提供最初的快速阿片样物质吸收，使得阿片样物质的最低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。

24. 发明申请

US20100209514A1 Method of treating pain by administering 24 hour oral oploid formulations exhibiting rapid rate of initial rise of plasma drug level 审中-公开
标题翻译：通过施用24小时口服鸦片制剂治疗疼痛的方法，其表现出血浆药物水平的初始升高的快速率
公开(公告)号：US20100209514A1
公开(公告)日：2010-08-19
申请号：US12653116
申请日：2009-12-08
申请人： Richard S. Sackler , Robert F. Kaiko , Paul Goldenheim
发明人： Richard S. Sackler , Robert F. Kaiko , Paul Goldenheim
IPC分类号： A61K31/485 , A61K31/454 , A61K31/445 , A61K31/439 , A61K31/4184 , A61K31/16 , A61K31/235 , A61K31/135 , A61K9/14 , A61P29/00
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。

25. 发明申请

US20060216340A1 Method of providing sustained analgesia with buprenorphine 审中-公开
公开(公告)号：US20060216340A1
公开(公告)日：2006-09-28
申请号：US11442512
申请日：2006-05-26
申请人： Robert Reder , Paul Goldenheim , Robert Kaiko
发明人： Robert Reder , Paul Goldenheim , Robert Kaiko
IPC分类号： A61K31/485 , A61K9/70
CPC分类号： A61K31/485 , A61K9/0014 , A61K9/0019 , A61K9/7023 , A61K9/7053 , A61K9/7061 , A61K31/4748
摘要： A method of effectively treating pain in humans is achieved by administering buprenorphine in accordance with first order kinetics over an initial three-day dosing interval, such that a maximum plasma concentration from about 20 pg/ml to about 1052 pg/ml is attained, and thereafter maintaining the administration of buprenorphine for at least an additional two-day dosing interval in accordance with substantially zero order kinetics, such that the patients experience analgesia throughout the at least two-day additional dosing interval.

26. 发明授权

US06306438B1 Stabilized sustained release tramadol formulations 失效
标题翻译：稳定缓释曲马多配方
公开(公告)号：US06306438B1
公开(公告)日：2001-10-23
申请号：US09109615
申请日：1998-07-02
申请人： Benjamin Oshlack , Hua-Pin Huang , Mark Chasin , Paul Goldenheim
发明人： Benjamin Oshlack , Hua-Pin Huang , Mark Chasin , Paul Goldenheim
IPC分类号： A61K922
CPC分类号： A61K9/2054 , A61K9/2013 , A61K9/2095
摘要： A stabilized sustained release oral solid dosage form which includes an effective amount of tramadol or a pharmaceutically acceptable salt thereof dispersed in a matrix of a hydrophobic material comprising a wax-like substance which was melted or softened during the preparation of the matrix, is cured at a temperature from about 35° C. to about 65° C. for a time period from about 4 to about 72 hours, such that the formulation, when subjected to in-vitro dissolution after exposure to accelerated storage conditions of at least one month at 40° C./75% RH, releases an amount of tramadol which does not vary at any given dissolution time point by more than about 20% of the total amount of tramadol released when compared to in-vitro dissolution conducted prior to subjecting the dosage form to the accelerated storage conditions.
摘要翻译：稳定的持续释放口服固体剂型，其包含分散在疏水性材料的基质中的有效量的曲马朵或其药学上可接受的盐，其包含在制备基质期间熔融或软化的蜡状物质，其在温度为约35℃至约65℃，时间为约4至约72小时，使得当暴露于至少一个月的加速储存条件后经受体外溶解时，该制剂 40℃/ 75％RH时，释放一定量的曲马多，与任何给定的溶解时间点相比，在与给药剂量之前进行的体外溶出相比，释放曲马多总量的大约20％形成加速存储条件。

27. 发明申请

US20100209351A1 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，显示血浆药物水平的初始升高速度
公开(公告)号：US20100209351A1
公开(公告)日：2010-08-19
申请号：US12653109
申请日：2009-12-08
申请人： Richard S. Sackler , Robert F. Kaiko , Paul Goldenheim
发明人： Richard S. Sackler , Robert F. Kaiko , Paul Goldenheim
IPC分类号： A61K49/00 , A61K31/485 , A61K31/4355 , A61K9/00 , A61K9/14 , A61K9/10 , A61P25/04
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。

28. 发明授权

US06451335B1 Formulations and methods for providing prolonged local anesthesia 失效
标题翻译：提供延长局部麻醉的制剂和方法
公开(公告)号：US06451335B1
公开(公告)日：2002-09-17
申请号：US09109323
申请日：1998-07-02
申请人： Paul Goldenheim , Donna Donigi-Gale , Kevin Burton , Mohammed Shameem , Amol Ketkar , Mark Chasin , Richard Maskiewicz
发明人： Paul Goldenheim , Donna Donigi-Gale , Kevin Burton , Mohammed Shameem , Amol Ketkar , Mark Chasin , Richard Maskiewicz
IPC分类号： A61F202
CPC分类号： A61M19/00 , A61K9/1647 , A61K45/06
摘要： A formulation for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material prolonging the release of the local anesthetic from the substrate to obtain a reversible local anesthesia when implanted or injected in a patient, and a non-toxic augmenting agent effective to prolong the duration of the local anesthesia for a time period longer than that obtainable from the substrate without the augmenting agent. In preferred embodiments, the controlled release material is a low molecular weight, acid-terminated polymer. A further aspect of the invention is directed to such formulations which release the local anesthetic in two phases, the first a rapid “bolus” to initiate anesthesia and a second, slower release to maintain anesthesia.
摘要翻译：一种用于在患者中诱导持续区域局部麻醉的制剂，其包含包含局部麻醉剂和有效量的生物相容的可生物降解的受控释放材料的底物，其延长了局部麻醉剂从基质的释放，以在植入时获得可逆局部麻醉，注射在患者体内，以及无毒性增强剂，其有效地延长局部麻醉的持续时间比在不含增强剂的情况下可获得的时间长。在优选的实施方案中，控释材料是低分子量的酸封端的聚合物。本发明的另一方面涉及这样的制剂，其释放两个阶段的局部麻醉剂，第一次是快速“推注”以引发麻醉，第二次较慢释放以维持麻醉。

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