公开(公告)号：US5277916A

公开(公告)日：1994-01-11

申请号：US523239

申请日：1990-05-14

申请人： Mark Dwyer ,  Mark C. Fisher ,  Angelo M. Morella

发明人： Mark Dwyer ,  Mark C. Fisher ,  Angelo M. Morella

IPC分类号： A61K9/32 ,  A61K9/50 ,  A61K31/65 ,  A61K9/28

CPC分类号： A61K31/65 ,  A61K9/5026 ,  A61K9/5042 ,  A61K9/5078

摘要： A tetracycline pharmaceutical composition having a core element containing a tetracycline antibiotic and a core coating which dissolves more slowly in the stomach than in the intestine. Administration of the composition to a human results in drug concentrations in the blood which are bioequivalent to those achieved with immediate release formulations.

摘要翻译： 一种四环素药物组合物，其具有含有四环素抗生素的核心元件和在胃中比在肠中更缓慢地溶解的核心涂层。 将组合物施用于人导致血液中的药物浓度与用速释制剂实现的药物浓度生物等效。

公开(公告)号：US5202128A

公开(公告)日：1993-04-13

申请号：US574551

申请日：1990-08-24

申请人： Angelo M. Morella ,  Mark C. Fisher

发明人： Angelo M. Morella ,  Mark C. Fisher

IPC分类号： A61K9/22 ,  A61K9/50 ,  A61K9/58

CPC分类号： A61K9/5078 ,  A61K9/5005 ,  A61K9/5026 ,  A61K9/5031 ,  A61K9/5047

摘要： The present invention relates to a pharmaceutical pellet composition having a core element including at least one highly soluble active ingredient and a core coating which is partially soluble at a highly acidic pH. The pharmaceutical composition provides a slow release of active ingredient at a highly acidic pH and provides a constant, relatively faster rate of release at a more alkaline pH such as that of the intestine. Oral administration of the pharmaceutical pellet composition of the present invention to a patient is effective to deliver to the blood levels of active ingredient within the therapeutic range and to maintain such levels over an extended period of time.

摘要翻译： 本发明涉及具有至少一种高可溶性活性成分的核心元件和在高酸性pH下可部分溶解的核心涂层的药物颗粒组合物。 药物组合物在高酸性pH下提供活性成分的缓慢释放，并且在更碱性的pH（例如肠）下提供恒定的，相对较快的释放速率。 将本发明的药物颗粒组合物口服施用于患者可有效地递送到治疗范围内的活性成分的血液水平并且在延长的时间段内维持该水平。

公开(公告)号：US5378474A

公开(公告)日：1995-01-03

申请号：US21276

申请日：1993-02-22

申请人： Angelo M. Morella ,  Mark C. Fisher

发明人： Angelo M. Morella ,  Mark C. Fisher

IPC分类号： A61K9/22 ,  A61K9/50 ,  A61K9/58 ,  A61K9/24

CPC分类号： A61K9/5078 ,  A61K9/5005 ,  A61K9/5026 ,  A61K9/5031 ,  A61K9/5047

摘要： The present invention relates to a pharmaceutical pellet composition having a core element including at least one highly soluble active ingredient and a core coating which is partially soluble at a highly acidic pH. The pharmaceutical composition provides a slow release of active ingredient at a highly acidic pH and provides a constant, relatively faster rate of release at a more alkaline pH such as that of the intestine. Oral administration of the pharmaceutical pellet composition of the present invention to a patient is effective to deliver to the blood levels of active ingredient within the therapeutic range and to maintain such levels over an extended period of time.

摘要翻译： 本发明涉及具有至少一种高可溶性活性成分的核心元件和在高酸性pH下可部分溶解的核心涂层的药物颗粒组合物。 药物组合物在高酸性pH下提供活性成分的缓慢释放，并且在更碱性的pH（例如肠）下提供恒定的，相对较快的释放速率。 将本发明的药物颗粒组合物口服施用于患者可有效地递送到治疗范围内的活性成分的血液水平并且在延长的时间段内维持该水平。

公开(公告)号：US5330766A

公开(公告)日：1994-07-19

申请号：US7633

申请日：1993-01-21

申请人： Angelo M. Morella ,  Mark C. Fisher

发明人： Angelo M. Morella ,  Mark C. Fisher

IPC分类号： A61K9/22 ,  A61K9/50 ,  A61K9/58 ,  A61K9/16 ,  A61K9/30 ,  B05D7/00

CPC分类号： A61K9/5005 ,  A61K9/5026 ,  A61K9/5031 ,  A61K9/5047 ,  A61K9/5078

摘要： The present invention relates to a pharmaceutical pellet composition having a core element including at least one highly soluble active ingredient and a core coating which is partially soluble at a highly acidic pH. The pharmaceutical composition provides a slow release of active ingredient at a highly acidic pH and provides a constant, relatively faster rate of release at a more alkaline pH such as that of the intestine. Oral administration of the pharmaceutical pellet composition of the present invention to a patient is effective to deliver to the blood levels of active ingredient within the therapeutic range and to maintain such levels over an extended period of time.

摘要翻译： 本发明涉及具有至少一种高可溶性活性成分的核心元件和在高酸性pH下可部分溶解的核心涂层的药物颗粒组合物。 药物组合物在高酸性pH下提供活性成分的缓慢释放，并且在更碱性的pH（例如肠）下提供恒定的，相对较快的释放速率。 将本发明的药物颗粒组合物口服施用于患者可有效地递送到治疗范围内的活性成分的血液水平并且在延长的时间段内维持该水平。

公开(公告)号：US08771739B2

公开(公告)日：2014-07-08

申请号：US11763578

申请日：2007-06-15

申请人： David Hayes ,  Angelo M. Morella

发明人： David Hayes ,  Angelo M. Morella

IPC分类号： A61K9/20 ,  A61K9/14 ,  A61K47/00 ,  A61K9/48 ,  A61K31/4965 ,  A61P43/00

CPC分类号： A61K31/496 ,  A61K9/146 ,  A61K9/1652 ,  A61K9/4866

摘要： The present invention provides a pharmaceutical composition of a practically insoluble drug, wherein the composition may be administered with food or without food. The composition may be in the form of a solid dispersion of the practically insoluble drug and a polymer having acidic functional groups, and the composition may in vitro form a suspension.

摘要翻译： 本发明提供了几乎不溶性药物的药物组合物，其中所述组合物可以与食物或不含食物一起施用。 组合物可以是几乎不溶性药物的固体分散体和具有酸性官能团的聚合物的形式，组合物可以在体外形成悬浮液。

公开(公告)号：US6033687A

公开(公告)日：2000-03-07

申请号：US287904

申请日：1999-04-07

申请人： Grant W. Heinicke ,  Angelo Lepore ,  Angelo M. Morella

发明人： Grant W. Heinicke ,  Angelo Lepore ,  Angelo M. Morella

IPC分类号： A61K9/50 ,  A61K9/54 ,  A61K31/554

CPC分类号： A61K9/5078 ,  A61K31/554 ,  A61K9/5084

摘要： A controlled absorption diltiazem pellet formulation for oral administration comprises a core having diltiazem or a pharmaceutically acceptable salt thereof as the active ingredient. The core is surrounded by a coating which has only a single layer which is comprised of a relatively major proportion of talc and relatively minor proportion of sodium lauryl sulfate admixed with a minor proportion of a pharmaceutically acceptable film-forming, first polymer permeable to water and diltiazem, and a major proportion of a pharmaceutically acceptable film-forming, second polymer that is less permeable to water and diltiazem than the first polymer. The core and the coating layer both exclude organic acids. The composition of the coating layer as well as the proportion of core to coating layer are effective to permit release of the diltiazem allowing controlled absorption following oral administration. By combining short lag and long lag pellets into a single formulation, the release of diltiazem is controlled over a twenty four hour period.

摘要翻译： 用于口服给药的受控吸收性地尔硫卓丸剂制剂包括具有地尔硫卓或其药学上可接受的盐作为活性成分的核心。 核心被仅由单一层组成的涂层包围，该层由相​​对较大比例的滑石和相对较少比例的十二烷基硫酸钠组成，其中少量的可药用成膜的第一聚合物可渗透水分， 地尔硫卓和大部分可药用成膜的第二聚合物，其比第一聚合物对水和地尔硫卓渗透性较差。 核心和涂层都排除有机酸。 涂层的组成以及芯与包衣层的比例对于允许释放硫酸盐是有效的，允许经口给药后受控吸收。 通过将短滞后和长滞后丸混合成单一制剂，地尔硫卓的释​​放可控制在二十四小时内。

公开(公告)号：US07067151B1

公开(公告)日：2006-06-27

申请号：US09606629

申请日：2000-06-29

申请人： Grant W. Heinicke ,  Angelo Lepore ,  Angelo M. Morella

发明人： Grant W. Heinicke ,  Angelo Lepore ,  Angelo M. Morella

IPC分类号： A61K9/54

CPC分类号： A61K9/5078 ,  A61K9/5084 ,  A61K31/554

摘要： A controlled absorption diltiazem pellet formulation for oral administration comprises a core having diltiazem or a pharmaceutically acceptable salt thereof as the active ingredient. The core is surrounded by a coating which has only a single layer which is comprised of a relatively major proportion of talc and relatively minor proportion of sodium lauryl sulfate admixed with a minor proportion of a pharmaceutically acceptable film-forming, first polymer permeable to water and diltiazem, and a major proportion of a pharmaceutically acceptable film-forming, second polymer that is less permeable to water and diltiazem than the first polymer. The core and the coating layer both exclude organic acids. The composition of the coating layer as well as the proportion of core to coating layer are effective to permit release of the diltiazem allowing controlled absorption following oral administration. By combining short lag and long lag pellets into a single formulation, the release of diltiazem is controlled over a twenty four hour period.

公开(公告)号：US06214385B1

公开(公告)日：2001-04-10

申请号：US09447642

申请日：1999-11-23

申请人： Grant W. Heinicke ,  Angelo Lepore ,  Angelo M. Morella

发明人： Grant W. Heinicke ,  Angelo Lepore ,  Angelo M. Morella

IPC分类号： A61K954

CPC分类号： A61K9/5078 ,  A61K9/5084 ,  A61K31/554

摘要： A controlled absorption diltiazem pellet formulation for oral administration comprises a core having diltiazem or a pharmaceutically acceptable salt thereof as the active ingredient. The core is surrounded by a coating which has only a single layer which is comprised of a relatively major proportion of talc and relatively minor proportion of sodium lauryl sulfate admixed with a minor proportion of a pharmaceutically acceptable film-forming, first polymer permeable to water and diltiazem, and a major proportion of a pharmaceutically acceptable film-forming, second polymer that is less permeable to water and diltiazem than the first polymer. The core and the coating layer both exclude organic acids. The composition of the coating layer as well as the proportion of core to coating layer are effective to permit release of the diltiazem allowing controlled absorption following oral administration. By combining short lag and long lag pellets into a single formulation, the release of diltiazem is controlled over a twenty four hour period.

摘要翻译： 用于口服给药的受控吸收性地尔硫卓丸剂制剂包括具有地尔硫卓或其药学上可接受的盐作为活性成分的核心。 核心被仅由单一层组成的涂层包围，该层由相​​对较大比例的滑石和相对较少比例的十二烷基硫酸钠组成，其中少量的可药用成膜的第一聚合物可渗透水分， 地尔硫卓和大部分可药用成膜的第二聚合物，其比第一聚合物对水和地尔硫卓渗透性较差。 核心和涂层都排除有机酸。 涂层的组成以及芯与包衣层的比例对于允许释放硫酸盐是有效的，允许经口给药后受控吸收。 通过将短滞后和长滞后丸混合成单一制剂，地尔硫卓的释​​放可控制在二十四小时内。