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1. 发明授权

US07070806B2 Controlled release formulations coated with aqueous dispersions of acrylic polymers 失效
公开(公告)号：US07070806B2
公开(公告)日：2006-07-04
申请号：US10273434
申请日：2002-10-17
申请人： Benjamin Oshlack , Mark Chasin , Frank Pedi, Jr.
发明人： Benjamin Oshlack , Mark Chasin , Frank Pedi, Jr.
IPC分类号： A61K9/22 , A61K9/32 , A61K9/50 , A61K9/28 , A01N25/26
CPC分类号： A61K9/5026 , A61K9/2846 , 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.

2. 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。

3. 发明授权

US06316031B1 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：US06316031B1
公开(公告)日：2001-11-13
申请号：US09469478
申请日：1999-12-22
申请人： Benjamin Oshlack , Frank Pedi, Jr. , Mark Chasin
发明人： Benjamin Oshlack , Frank Pedi, Jr. , Mark Chasin
IPC分类号： A61K962
CPC分类号： A61K9/5089 , A61K9/1617 , A61K9/1635 , A61K9/2013 , A61K9/2054 , A61K9/2072 , A61K9/2081 , A61K9/2095 , A61K9/2866 , A61K9/5078 , A61K31/485 , A61K31/522
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。

4. 发明授权

US5286493A Stabilized controlled release formulations having acrylic polymer coating 失效
标题翻译：具有丙烯酸聚合物涂层的稳定的控释制剂
公开(公告)号：US5286493A
公开(公告)日：1994-02-15
申请号：US826084
申请日：1992-01-27
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 , A61K9/22 , A61K9/28 , A61K9/32 , A61K9/50 , A61K9/52 , A61K9/54 , A61K9/58 , A61K9/62 , A61M37/00 , A61K9/00
CPC分类号： A61K9/5026 , A61K9/2846 , A61K9/5078
摘要： A stabilized solid controlled release dosage form having a coating derived from an aqueous dispersion of an acrylic polymer is obtained by overcoating a substrate including a therapeutically active with an aqueous dispersion of the plasticized acrylic polymer and then curing the coated substrate at a temperature above the glass transition temperature of the plasticized acrylic polymer, 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：具有衍生自丙烯酸类聚合物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增塑的丙烯酸类聚合物的水性分散体的包含治疗活性的底物进行外涂，然后在高于玻璃的温度下固化涂覆的基材直到涂覆的剂型达到稳定的溶解曲线，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。

5. 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.

6. 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。

7. 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。

8. 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.

9. 发明授权

US5472712A Controlled-release formulations coated with aqueous dispersions of ethylcellulose 失效
标题翻译：用乙基纤维素的水性分散体涂覆的控制释放制剂
公开(公告)号：US5472712A
公开(公告)日：1995-12-05
申请号：US81618
申请日：1993-06-23
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 , A01N25/26 , A01N25/28 , A61K9/20 , A61K9/22 , A61K9/28 , A61K9/36 , A61K9/48 , A61K9/50 , A61K9/52 , A61K9/54 , A61K9/58 , A61K9/62 , A61K31/485 , A61K31/52 , A61K31/522 , A61K45/00 , A61K47/38 , A61P25/04 , A61K9/14
CPC分类号： A61K9/167 , A61K31/522 , A61K9/2866 , A61K9/5078
摘要： A stabilized solid controlled release formulation having a coating derived from an aqueous dispersion of a hydrophobic polymer is obtained by overcoating 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, with an aqueous dispersion of the plasticized hydrophobic polymer and then curing the coated substrate at a temperature above the glass transition temperature of the plasticized hydrophobic polymer, until a curing endpoint is reached at which the coated substrate provides a stabilized dissolution of the active agent which is unchanged after exposure to accelerated storage conditions, the endpoint being determined by comparing the dissolution profile of the formulation immediately after curing to the dissolution profile of the formulation after exposure to accelerated storage conditions of at least one month at a temperature of 37.degree. C. and at a relative humidity of 80%.
摘要翻译：具有衍生自疏水性聚合物的水性分散体的涂层的稳定的固体控制释放制剂通过对包含选自以下的活性剂的底物进行外涂层，所述活性剂选自系统活性治疗剂，局部活性治疗剂，消毒和消毒试剂，清洁剂，香料和施肥剂，与增塑的疏水性聚合物的水分散体，然后在高于塑化的疏水性聚合物的玻璃化转变温度的温度下固化涂覆的基材，直至达到固化终点涂覆的基底提供活性剂的稳定溶解，其在暴露于加速储存条件后不变，终点通过将刚刚固化后的制剂的溶出曲线与暴露于加速储存条件后的制剂的溶出曲线进行比较来确定 o f在37℃的温度和80％的相对湿度下至少一个月。

10. 发明授权

US5273760A 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：US5273760A
公开(公告)日：1993-12-28
申请号：US814111
申请日：1991-12-24
申请人： Benjamin Oshlack , Frank Pedi, Jr. , Mark Chasin
发明人： Benjamin Oshlack , Frank Pedi, Jr. , Mark Chasin
IPC分类号： A61K9/16 , A61K9/20 , A61K9/22 , A61K9/28 , A61K9/36 , A61K9/48 , A61K9/50 , A61K9/54 , A61K9/62 , A61K31/485 , A61K31/52 , A61K31/522 , A61K45/00 , A61K47/38 , A61K9/14
CPC分类号： A61K31/522 , 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 agent 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.

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