公开(公告)号：US08182836B2

公开(公告)日：2012-05-22

申请号：US12478952

申请日：2009-06-05

申请人： Atul M. Mehta

发明人： Atul M. Mehta

IPC分类号： A61K31/485

CPC分类号： A61K9/1676 ,  A61K9/4808 ,  A61K9/5026 ,  A61K9/5078 ,  A61K31/485

摘要： An opioid-antagonist oral dosage form which does not release a therapeutically effective amount of the opioid antagonist when the oral dosage form is orally administered to a human being, but whereby a physical alteration of the oral dosage form results in a release of the therapeutically effective amount of the opioid antagonist. An embodiment of the oral dosage form includes an opioid-antagonist layer coated onto a biologically inert pellet, and a non-releasing membrane coated onto the opioid-antagonist layer. Optionally, the oral dosage form can also include an opioid agonist, such that a method of preventing the abuse of an oral dosage form of an opioid agonist is provided by forming the oral dosage form including an opioid agonist and an opioid antagonist.

摘要翻译： 一种阿片类拮抗剂口服剂型，当口服给药于人时，不释放治疗有效量的阿片样物质拮抗剂，但由此口服剂型的物理改变导致治疗有效的释放 阿片类拮抗剂的量。 口服剂型的一个实施方案包括涂覆在生物惰性颗粒上的阿片样物质 - 拮抗剂层和涂覆在阿片样物质 - 拮抗剂层上的非释放膜。 任选地，口服剂型还可以包括阿片样物质激动剂，使得通过形成包括阿片样物质激动剂和阿片样物质拮抗剂的口服剂型来提供防止滥用口服剂型的阿片样物质激动剂的方法。

公开(公告)号：US06926909B2

公开(公告)日：2005-08-09

申请号：US10406961

申请日：2003-04-04

申请人： Atul M. Mehta

发明人： Atul M. Mehta

IPC分类号： A61K9/24 ,  A61K9/20 ,  A61K9/22 ,  A61K9/32 ,  A61K9/50 ,  A61K9/52 ,  A61K31/554 ,  A61K47/12 ,  A61K47/26 ,  A61K47/32 ,  A61K47/38 ,  A61P9/10 ,  A61P9/12 ,  A61K9/14

CPC分类号： A61K31/554 ,  A61K9/2081 ,  A61K9/5026 ,  A61K9/5078

摘要： A dosage formulation for once daily administration prior to sleeping is described that provides an initial delay in pharmaceutical release followed by controlled release of the pharmaceutical. There is also provided a method for preparing a time specific delayed, controlled release formulation of dosage, which method includes coating a single pellet with at least one dosage layer, which is coated by at least one seal coat and at least one outer rate controlling layer of a water soluble polymer coat. The dosage formulation of this invention provides substantially a drug free interval of about 0 to 5 hours followed by a drug delivery interval at a rate permitting bioavailability thereof for up to about 24 hours following oral administration. A method of using the formulations of the present invention for the treatment of early morning pathologies is also described.

摘要翻译： 描述了在睡眠之前每日一次给药的剂量制剂，其提供药物释放的初始延迟，然后控制释放药物。 还提供了制备时间特异性延迟控制释放剂量的方法，该方法包括用至少一个剂量层涂覆单个颗粒，该剂量层由至少一个密封涂层和至少一个外部速率控制层 的水溶性聚合物涂层。 本发明的剂量制剂基本上提供约0至5小时的药物释放间隔，然后以允许其口服给药后约24小时的生物利用度的速率进行药物递送间隔。 还描述了使用本发明的制剂用于治疗清晨病变的方法。

公开(公告)号：US5871776A

公开(公告)日：1999-02-16

申请号：US738925

申请日：1996-10-28

申请人： Atul M. Mehta

发明人： Atul M. Mehta

IPC分类号： A61K9/50 ,  A61K31/4422 ,  A61K9/16 ,  A61K9/58

CPC分类号： A61K9/5078 ,  A61K31/4422 ,  Y10S514/964

摘要： A nifedipine formulation for oral administration is described that provides controlled, constant release of the pharmaceutical for about twenty four hours after a short delay following oral administration. There is also provided a method for preparing a controlled release formulation of nifedipine, which method includes coating pellets with multiple nifedipine-containing layers, along with an outer controlled release coating comprised of a water permeable polymer and lubricant/glidant. The pellets are then cured at an elevated temperature over several days. A method of using the formulations of the present invention for the treatment of patients is also described.

摘要翻译： 描述了用于口服给药的硝苯地平制剂，其在口服给药后短暂延迟后提供药物的受控的恒定释放约二十四小时。 还提供了一种制备硝苯地平的控释制剂的方法，该方法包括用多个含硝苯地平的层涂覆颗粒，以及由透水性聚合物和润滑剂/助流剂组成的外部控释层。 然后将颗粒在升高的温度下固化数天。 还描述了使用本发明的制剂治疗患者的方法。

公开(公告)号：US4794001A

公开(公告)日：1988-12-27

申请号：US100646

申请日：1987-09-24

申请人： Atul M. Mehta ,  Lizbeth A. Bachand ,  Thomas W. Leonard ,  Ronald N. Warner

发明人： Atul M. Mehta ,  Lizbeth A. Bachand ,  Thomas W. Leonard ,  Ronald N. Warner

IPC分类号： A61K9/50 ,  A61K9/52 ,  A61K9/54 ,  A61K9/58

CPC分类号： A61K9/5084 ,  A61K9/5073

摘要： A therapeutic preparation consisting of three groups of spheroids containing an active medicinal substance. The first group of spheroids is uncoated and rapidly disintegrates upon ingestion to release an initial dose of medicinal substance a second group of spheroids is coated with a pH sensitive coat to provide a second dose and a third group of spheroids is coated with a pH independent coat to provide a third dose. A powder blend of active medicinal substance may be substituted for the first group of uncoated spheroids.The therapeutic preparation may be utilized as a mixture of groups of spheroids in a capsule.

公开(公告)号：US20090238868A1

公开(公告)日：2009-09-24

申请号：US12478952

申请日：2009-06-05

申请人： Atul M. Mehta

发明人： Atul M. Mehta

IPC分类号： A61K31/485 ,  A61K9/16 ,  A61K9/24 ,  A61K9/52 ,  A61P25/36

CPC分类号： A61K9/1676 ,  A61K9/4808 ,  A61K9/5026 ,  A61K9/5078 ,  A61K31/485

摘要： An opioid-antagonist oral dosage form which does not release a therapeutically effective amount of the opioid antagonist when the oral dosage form is orally administered to a human being, but whereby a physical alteration of the oral dosage form results in a release of the therapeutically effective amount of the opioid antagonist. An embodiment of the oral dosage form includes an opioid-antagonist layer coated onto a biologically inert pellet, and a non-releasing membrane coated onto the opioid-antagonist layer. Optionally, the oral dosage form can also include an opioid agonist, such that a method of preventing the abuse of an oral dosage form of an opioid agonist is provided by forming the oral dosage form including an opioid agonist and an opioid antagonist.

摘要翻译： 一种阿片类拮抗剂口服剂型，当口服给药于人时，不释放治疗有效量的阿片样物质拮抗剂，但由此口服剂型的物理改变导致治疗有效的释放 阿片类拮抗剂的量。 口服剂型的一个实施方案包括涂覆在生物惰性颗粒上的阿片样物质 - 拮抗剂层和涂覆在阿片样物质 - 拮抗剂层上的非释放膜。 任选地，口服剂型还可以包括阿片样物质激动剂，使得通过形成包括阿片样物质激动剂和阿片样物质拮抗剂的口服剂型来提供防止滥用口服剂型的阿片样物质激动剂的方法。

公开(公告)号：US06620439B1

公开(公告)日：2003-09-16

申请号：US09678335

申请日：2000-10-03

申请人： Atul M. Mehta

发明人： Atul M. Mehta

IPC分类号： A61K916

CPC分类号： A61K31/554 ,  A61K9/2081 ,  A61K9/5026 ,  A61K9/5078

摘要： A dosage formulation for once daily administration prior to sleeping is described that provides an initial delay in pharmaceutical release followed by controlled release of the pharmaceutical. There is also provided a method for preparing a time specific delayed, controlled release formulation of dosage, which method includes coating a single pellet with at least one dosage layer, which is coated by at least one seal coat and at least one outer rate controlling layer of a water soluble polymer coat. The dosage formulation of this invention provides substantially a drug free interval of about 0 to 5 hours followed by a drug delivery interval at a rate permitting bioavailability thereof for up to about 24 hours following oral administration. A method of using the formulations of the present invention for the treatment of early morning pathologies is also described.

摘要翻译： 描述了在睡眠之前每日一次给药的剂量制剂，其提供药物释放的初始延迟，然后控制释放药物。 还提供了制备时间特异性延迟控制释放剂量的方法，该方法包括用至少一个剂量层涂覆单个颗粒，该剂量层由至少一个密封涂层和至少一个外部速率控制层 的水溶性聚合物涂层。 本发明的剂量制剂基本上提供约0至5小时的药物释放间隔，然后以允许其口服给药后约24小时的生物利用度的速率进行药物递送间隔。 还描述了使用本发明的制剂用于治疗清晨病变的方法。

公开(公告)号：US4904476A

公开(公告)日：1990-02-27

申请号：US252424

申请日：1988-09-30

申请人： Atul M. Mehta ,  Lizbeth A. Bachand ,  Thomas W. Leonard ,  Ronald N. Warner

发明人： Atul M. Mehta ,  Lizbeth A. Bachand ,  Thomas W. Leonard ,  Ronald N. Warner

IPC分类号： A61K9/50 ,  A61K9/64

CPC分类号： A61K9/5073 ,  A61K9/5084

摘要： A therapeutic preparation consisting of three groups of spheroids containing an active medicinal substance. The first group of spheroids is uncoated and rapidly disintegrates upon ingestion to release an initial dose of medicinal substance a second group of spheroids is coated with a pH sensitive coat to provide a second dose and a third group of spheroids is coated with a pH independent coat to provide a third dose. A powder blend of active medicinal substance may be substituted for the first group of uncoated spheroids. The therapeutic preparation may be utilized as a mixture of groups of spheroids in a capsule.

摘要翻译： 由含有活性药物的三组球体组成的治疗制剂。 第一组球体是未涂层的，并且在摄入时快速崩解以释放初始剂量的药用物质，第二组球体涂覆有pH敏感的涂层以提供第二剂量，第三组球体涂覆有不依赖于pH的涂层 提供第三剂。 活性药物的粉末混合物可以代替第一组未涂覆的球体。 治疗制剂可以用作胶囊中的球体组的混合物。

公开(公告)号：US4800087A

公开(公告)日：1989-01-24

申请号：US933988

申请日：1986-11-24

申请人： Atul M. Mehta

发明人： Atul M. Mehta

IPC分类号： A61K47/30 ,  A61K9/00 ,  A61K9/32 ,  A61K9/50 ,  A61K9/56 ,  A61K9/58

CPC分类号： A61K9/0056 ,  A61K9/5026 ,  Y10S514/963

摘要： In accordance with the present invention, these and other objects are achieved by a pharmaceutical composition comprised of (1) a pharmaceutical core which is further comprised of a pharmaceutically active dose of a compound and, (2) a microencapsulating polymer which coats the pharmaceutical core and is capable of taste-making the active compound. The polymer coating maintains its integrity, i.e., does not fracture and release active when tabletted and/or chewed, and can provide immediate release of the active compound in the stomach, or alternatively, in certain embodiments, can release the active agent in the upper intestinal tract or in sustained release fashion. Additionally, the polymeric coating compositions or the pharmaceutical core may contain diluents, fillers, bulking agents, and plasticizers. The polymeric coatings may also contain pigments and opacifiers to promote compliance and enhance the storage stability of light sensitive active agents.

摘要翻译： 根据本发明，这些和其它目的通过药物组合物实现，药物组合物包含（1）药物核心，其还包含药物活性剂量的化合物，和（2）包封药物核心的微胶囊化聚合物 并且能够制造活性化合物。 聚合物涂层维持其完整性，即在压片和/或咀嚼时不断裂和释放活性，并且可以提供活性化合物在胃中的即时释放，或者在某些实施方案中，可以将活性剂在上部 肠道或以缓释方式。 此外，聚合物涂料组合物或药物核心可以含有稀释剂，填充剂，填充剂和增塑剂。 聚合物涂层还可以含有颜料和遮光剂以促进柔顺性并提高光敏性活性剂的储存稳定性。

公开(公告)号：US08425933B2

公开(公告)日：2013-04-23

申请号：US12640344

申请日：2009-12-17

申请人： Atul M. Mehta

发明人： Atul M. Mehta

IPC分类号： A61K31/485

CPC分类号： A61K9/1676 ,  A61K9/4808 ,  A61K9/5026 ,  A61K9/5078 ,  A61K31/485

摘要： An opioid-antagonist oral dosage form which does not release a therapeutically effective amount of the opioid antagonist when the oral dosage form is orally administered to a human being, but whereby a physical alteration of the oral dosage form results in a release of the therapeutically effective amount of the opioid antagonist. An embodiment of the oral dosage form includes an opioid-antagonist layer coated onto a biologically inert pellet, and a non-releasing membrane coated onto the opioid-antagonist layer. Optionally, the oral dosage form can also include an opioid agonist, such that a method of preventing the abuse of an oral dosage form of an opioid agonist is provided by forming the oral dosage form including an opioid agonist and an opioid antagonist.

摘要翻译： 一种阿片类拮抗剂口服剂型，当口服给药于人时，不释放治疗有效量的阿片样物质拮抗剂，但由此口服剂型的物理改变导致治疗有效的释放 阿片类拮抗剂的量。 口服剂型的一个实施方案包括涂覆在生物惰性颗粒上的阿片样物质 - 拮抗剂层和涂覆在阿片样物质 - 拮抗剂层上的非释放膜。 任选地，口服剂型还可以包括阿片样物质激动剂，使得通过形成包括阿片样物质激动剂和阿片样物质拮抗剂的口服剂型来提供防止滥用口服剂型的阿片样物质激动剂的方法。

公开(公告)号：US20100098771A1

公开(公告)日：2010-04-22

申请号：US12640344

申请日：2009-12-17

申请人： Atul M. Mehta

发明人： Atul M. Mehta

IPC分类号： A61K9/14 ,  A61K31/439 ,  A61P25/00

CPC分类号： A61K9/1676 ,  A61K9/4808 ,  A61K9/5026 ,  A61K9/5078 ,  A61K31/485

摘要： An opioid-antagonist oral dosage form which does not release a therapeutically effective amount of the opioid antagonist when the oral dosage form is orally administered to a human being, but whereby a physical alteration of the oral dosage form results in a release of the therapeutically effective amount of the opioid antagonist. An embodiment of the oral dosage form includes an opioid-antagonist layer coated onto a biologically inert pellet, and a non-releasing membrane coated onto the opioid-antagonist layer. Optionally, the oral dosage form can also include an opioid agonist, such that a method of preventing the abuse of an oral dosage form of an opioid agonist is provided by forming the oral dosage form including an opioid agonist and an opioid antagonist.

摘要翻译： 一种阿片类拮抗剂口服剂型，当口服给药于人时，不释放治疗有效量的阿片样物质拮抗剂，但由此口服剂型的物理改变导致治疗有效的释放 阿片类拮抗剂的量。 口服剂型的一个实施方案包括涂覆在生物惰性颗粒上的阿片样物质 - 拮抗剂层和涂覆在阿片样物质 - 拮抗剂层上的非释放膜。 任选地，口服剂型还可以包括阿片样物质激动剂，使得通过形成包括阿片样物质激动剂和阿片样物质拮抗剂的口服剂型来提供防止滥用口服剂型的阿片样物质激动剂的方法。