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1. 发明授权

US08492334B2 Sustained intraocular delivery of drugs from biodegradable polymeric microparticles 有权
标题翻译：从可生物降解的聚合物微粒中持续的眼内输送药物
公开(公告)号：US08492334B2
公开(公告)日：2013-07-23
申请号：US12664792
申请日：2008-06-18
申请人： Erin Lavik , Young H. Kwon , Markus Kuehn , Sandeep Saluja , James Bertram , John Huang
发明人： Erin Lavik , Young H. Kwon , Markus Kuehn , Sandeep Saluja , James Bertram , John Huang
IPC分类号： A61K38/18 , A61K38/22 , A61K31/7036 , A61K31/704 , A61K31/57 , A61K31/573
CPC分类号： A61K9/1647 , A61K9/0048 , A61K9/5153
摘要： Biodegradable polymeric microparticle compositions containing one or more active agents, especially those useful for treating or preventing one or more diseases or disorders of the eye, and methods of making and using thereof, are described. In a preferred embodiment, the microparticle compositions contain one or more active agents useful for managing elevated intraocular pressure (IOP) in the eye. Relatively hydrophilic, and preferably carboxylated, polymeric materials such as PLGA are used for a drug such as timolol maleate, which is relatively water soluble, to increase drug loading. Higher molecular weight polymers, as well as the ratio of LA (which has a longer degradation time, up to one to two years) to GA (which has a short degradation time, as short as a few days to a week), are used to provide release over a longer period of time.
摘要翻译：描述了包含一种或多种活性剂，特别是可用于治疗或预防一种或多种眼睛疾病或病症的活性剂的生物降解性聚合物微粒组合物及其制备和使用方法。在优选的实施方案中，微粒组合物含有一种或多种用于治疗眼中升高的眼内压（IOP）的活性剂。相对亲水的，优选羧化的聚合物材料如PLGA用于药物，例如相对水溶性的马来酸噻吗洛尔，以增加药物负荷。使用较高分子量的聚合物，以及LA（其具有较长的降解时间，长达一至两年）与GA（其具有短的降解时间，短至几天至一周）的比率被使用提供更长时间的释放。

2. 发明申请

US20100261646A1 SUSTAINED INTRAOCULAR DELIVERY OF DRUGS FROM BIODEGRADABLE POLYMERIC MICROPARTICLES 有权
标题翻译：从生物可降解的聚合物微生物中持续的药物输送
公开(公告)号：US20100261646A1
公开(公告)日：2010-10-14
申请号：US12664792
申请日：2008-06-18
申请人： Erin Lavik , Young H. Kwon , Markus Kuehn , Sandeep Saluja , James Bertram , John Huang
发明人： Erin Lavik , Young H. Kwon , Markus Kuehn , Sandeep Saluja , James Bertram , John Huang
IPC分类号： A61K38/18 , A61K31/704 , A61K31/7036 , A61K31/57 , A61K31/573 , A61K31/5365 , A61K31/5377 , A61K31/496 , A61K31/505 , A61K31/4709 , A61K31/47 , A61K31/222 , A61K31/138
CPC分类号： A61K9/1647 , A61K9/0048 , A61K9/5153
摘要： Biodegradable polymeric microparticle compositions containing one or more active agents, especially those useful for treating or preventing or one or more diseases or disorders of the eye, and methods of making and using thereof, are described. The microsphere compositions release an effective amount of the one or more active agents for a period greater than 14 days in vivo, preferably greater than 60 days in vivo, more preferably up to 73 days in vivo, more preferably greater than 90 days in vivo, even more preferably over 100 days in vivo, and most preferably greater than 107 days in vivo. In a preferred embodiment, the microparticle compositions contain one or more active agents useful for managing elevated intraocular pressure (TOP) in the eye. In one embodiment, the microspheres are formed from polylactide-co-glycolide (“PLGA”); in another embodiment, the microspheres are formed from a blend PLGA and poly lactic acid (“PLA”). Relatively hydrophilic, and preferably carboxylated, polymeric materials such as PLGA are used for a drug such as timolol maleate, which is relatively water soluble, to increase drug loading. Higher molecular weight polymers, as well as the ratio of LA (which has a longer degradation time, up to one to two years) to GA (which has a short degradation time, as short as a few days to a week), are used to provide release over a longer period of time. The combination of drug loading and release rate, as well as the minimization of initial burst release, result in prolonged release of a higher amount of drug.
摘要翻译：描述了包含一种或多种活性剂，特别是可用于治疗或预防或一种或多种眼睛疾病或障碍的活性剂的生物可降解聚合物微粒组合物及其制备和使用方法。微球组合物在体内释放有效量的一种或多种活性剂大于14天，体内优选大于60天，更优选体内至多73天，更优选在体内释放大于90天，甚至更优选在体内超过100天，最优选在体内大于107天。在优选的实施方案中，微粒组合物含有一种或多种用于管理眼中升高的眼内压（TOP）的活性剂。在一个实施方案中，微球由聚丙交酯 - 共 - 乙交酯（“PLGA”）形成; 在另一个实施方案中，微球由共混PLGA和聚乳酸（“PLA”）形成。相对亲水的，优选羧化的聚合物材料如PLGA用于药物，例如相对水溶性的马来酸噻吗洛尔，以增加药物负荷。使用较高分子量的聚合物，以及LA（其具有较长的降解时间，长达一至两年）与GA（其具有短的降解时间，短至几天至一周）的比率被使用提供更长时间的释放。药物负载和释放速率的组合以及初始爆发释放的最小化导致更长量的药物释放。

3. 发明申请

US20110206773A1 SUSTAINED DELIVERY OF DRUGS FROM BIODEGRADABLE POLYMERIC MICROPARTICLES 审中-公开
标题翻译：从生物可降解聚合物微生物中持续输送药物
公开(公告)号：US20110206773A1
公开(公告)日：2011-08-25
申请号：US12945246
申请日：2010-11-12
申请人： Erin Lavik , James Bertram , Sandeep Saluja , Markus Kuehn , Young H. Kwon , Rebecca Robinson , John J. Huang
发明人： Erin Lavik , James Bertram , Sandeep Saluja , Markus Kuehn , Young H. Kwon , Rebecca Robinson , John J. Huang
IPC分类号： A61K9/14 , A61K31/573 , A61K31/216 , A61K31/517 , A61P27/02 , B65D69/00
CPC分类号： A61K9/1647 , A61K9/0048 , A61K31/216 , A61K31/517 , A61K31/519 , A61K31/57 , A61K31/573
摘要： Biodegradable polymeric microparticle compositions containing one or more active agents, especially those useful for treating or preventing or one or more diseases or disorders of the eye, and methods of making and using thereof, are described. The microsphere compositions release an effective amount of the one or more active agents for a period greater than 14 days in vivo, preferably greater than 60 days in vivo, more preferably up to 73 days in vivo, more preferably greater than 90 days in vivo, even more preferably over 100 days in vivo, and most preferably greater than 107 days in vivo. In a preferred embodiment, the microparticle compositions contain one or more active agents such as AG1478 to induce nerve regeneration, specifically regeneration of the optic nerve useful for managing elevated intraocular pressure (TOP) in the eye.
摘要翻译：描述了包含一种或多种活性剂，特别是可用于治疗或预防或一种或多种眼睛疾病或障碍的活性剂的生物可降解聚合物微粒组合物及其制备和使用方法。微球组合物在体内释放有效量的一种或多种活性剂大于14天，体内优选大于60天，更优选体内至多73天，更优选在体内释放大于90天，甚至更优选在体内超过100天，最优选在体内大于107天。在优选的实施方案中，微粒组合物含有一种或多种活性剂，例如用于诱导神经再生的AG1478，特别是可用于管理眼中升高的眼内压（TOP）的视神经再生。

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