公开(公告)号：US20080118556A1

公开(公告)日：2008-05-22

申请号：US11422226

申请日：2006-06-05

申请人： John G. Devane ,  Paul Stark ,  Niall M. M. Fanning ,  Gurvinder Singh Rekhi ,  Gary Liversidge ,  Scott A. Jenkins

发明人： John G. Devane ,  Paul Stark ,  Niall M. M. Fanning ,  Gurvinder Singh Rekhi ,  Gary Liversidge ,  Scott A. Jenkins

IPC分类号： A61K31/195 ,  A61K9/14 ,  A61K9/20 ,  A61K9/48 ,  A61P25/16

CPC分类号： A61K31/195 ,  A61K9/1676 ,  A61K9/5078 ,  A61K9/5084 ,  A61K31/275 ,  A61K2300/00

摘要： The invention relates to a multiparticulate modified release composition that, upon administration to a patient, delivers a combination of carbidopa, levodopa and entacapone in a bimodal, multimodal or continuous manner. The multiparticulate modified release composition comprises a first component and at least one subsequent component, the first component comprising a first population of active ingredient containing particles and the at least one subsequent component comprising a second population of active ingredient containing particles. The invention also relates to a solid oral dosage form containing such a multiparticulate modified release composition, and to a method for the treatment of Parkinson's disease.

摘要翻译： 本发明涉及一种多微粒改性释放组合物，其在给予患者时以双峰，多峰或连续方式递送卡比多巴，左旋多巴和恩他卡朋的组合。 多微粒改性释放组合物包含第一组分和至少一个后续组分，第一组分包含含有颗粒的第一组活性成分和至少一种随后的组分，其包含第二组含有颗粒的活性成分。 本发明还涉及含有这种多微粒释放组合物的固体口服剂型，以及治疗帕金森病的方法。

公开(公告)号：US06902742B2

公开(公告)日：2005-06-07

申请号：US10331754

申请日：2002-12-30

申请人： John G. Devane ,  Paul Stark ,  Niall M. M. Fanning ,  Gurvinder Singh Rekhi

发明人： John G. Devane ,  Paul Stark ,  Niall M. M. Fanning ,  Gurvinder Singh Rekhi

IPC分类号： A61K9/26 ,  A61K9/20 ,  A61K9/40 ,  A61K9/48 ,  A61K9/50 ,  A61K9/54 ,  A61K9/56 ,  A61K9/58 ,  A61K31/4458 ,  A61K47/32 ,  A61P11/00 ,  A61P25/00 ,  A61P43/00 ,  A61K9/14

CPC分类号： A61K9/5084

摘要： The invention relates to a multiparticulate modified release composition that in operation delivers an active ingredient in a pulsed or bimodal manner. The multiparticulate modified release composition comprises an immediate release component and a modified release component; the immediate release component comprising a first population of active ingredient containing particles and the modified release component comprising a second population of active ingredient containing particles coated with a controlled release coating; wherein the combination of the immediate release and modified release components in operation deliver the active ingredient in a pulsed or a bimodal manner. The invention also relates to a solid oral dosage form containing such a multiparticulate modified release composition. The plasma profile achieved by the multiparticulate modified release composition is advantageous in reducing patient tolerance to the active ingredient and in increasing patient compliance by reducing dosage frequency.

摘要翻译： 本发明涉及一种多微粒改性释放组合物，其在操作中以脉冲或双峰方式递送活性成分。 多微粒改性释放组合物包含立即释放组分和改性释放组分; 所述立即释放组分包含含有颗粒的第一组活性成分，所述改性释放组分包含第二组活性成分，所述活性成分含有涂覆有控释涂层的颗粒; 其中操作中的速释组分和改进释放组分的组合以脉冲或双峰方式递送活性成分。 本发明还涉及含有这种多微粒改性释放组合物的固体口服剂型。 通过多微粒改性释放组合物实现的血浆曲线有利于减少患者对活性成分的耐受性，并通过降低剂量频率提高患者依从性。

公开(公告)号：US06793936B2

公开(公告)日：2004-09-21

申请号：US10354483

申请日：2003-01-30

申请人： John G. Devane ,  Paul Stark ,  Niall M. M. Fanning

发明人： John G. Devane ,  Paul Stark ,  Niall M. M. Fanning

IPC分类号： A61K914

CPC分类号： A61K9/5084

摘要： The invention relates to a multiparticulate modified release composition that in operation delivers an active ingredient in a pulsed or bimodal manner. The multiparticulate modified release composition comprises an immediate release component and a modified release component; the immediate release component comprising a first population of active ingredient containing particles and the modified release component comprising a second population of active ingredient containing particles coated with a controlled release coating; wherein the combination of the immediate release and modified release components in operation deliver the active ingredient in a pulsed or a bimodal manner. The invention also relates to a solid oral dosage form containing such a multiparticulate modified release composition. The plasma profile achieved by the multiparticulate modified release composition is advantageous in reducing patient tolerance to the active ingredient and in increasing patient compliance by reducing dosage frequency.

摘要翻译： 本发明涉及一种多微粒改性释放组合物，其在操作中以脉冲或双峰方式递送活性成分。 多微粒改性释放组合物包含立即释放组分和改性释放组分; 所述立即释放组分包含含有颗粒的第一组活性成分，所述改性释放组分包含第二组活性成分，所述活性成分含有涂覆有控释涂层的颗粒; 其中操作中的速释组分和改进释放组分的组合以脉冲或双峰方式递送活性成分。 本发明还涉及含有这种多微粒改性释放组合物的固体口服剂型。 通过多微粒改性释放组合物实现的血浆曲线有利于减少患者对活性成分的耐受性，并通过降低剂量频率提高患者依从性。

公开(公告)号：US06730325B2

公开(公告)日：2004-05-04

申请号：US09850425

申请日：2001-05-07

申请人： John G. Devane ,  Paul Stark ,  Niall M. M. Fanning

发明人： John G. Devane ,  Paul Stark ,  Niall M. M. Fanning

IPC分类号： A61K914

CPC分类号： A61K9/5084

摘要： The invention relates to a multiparticulate modified release composition that in operation delivers an active ingredient in a pulsed or bimodal manner. The multiparticulate modified release composition comprises an immediate release component and a modified release component; the immediate release component comprising a first population of active ingredient containing particles and the modified release component comprising a second population of active ingredient containing particles coated with a controlled release coating; wherein the combination of the immediate release and modified release components in operation deliver the active ingredient in a pulsed or a bimodal manner. The invention also relates to a solid oral dosage form containing such a multiparticulate modified release composition. The plasma profile achieved by the multiparticulate modified release composition is advantageous in reducing patient tolerance to the active ingredient and in increasing patient compliance by reducing dosage frequency.

公开(公告)号：US06228398B1

公开(公告)日：2001-05-08

申请号：US09566636

申请日：2000-05-08

申请人： John G. Devane ,  Paul Stark ,  Niall M. M. Fanning

发明人： John G. Devane ,  Paul Stark ,  Niall M. M. Fanning

IPC分类号： A61K914

CPC分类号： A61K9/5084

摘要： The invention relates to a multiparticulate modified release composition that in operation delivers an active ingredient in a pulsed or bimodal manner. The multiparticulate modified release composition comprises an immediate release component and a modified release component; the immediate release component comprising a first population of active ingredient containing particles and the modified release component compnsimg a second population of active ingredient containing particles coated with a controlled release coating; wherein the combination of the immediate release and modified release components in operation deliver the active ingredient in a pulsed or a bimodal manner. The invention also relates to a solid oral dosage form containing such a multiparticulate modified release composition. The plasma profile achieved by the multiparticulate modified release composition is advantageous in reducing patient tolerance to the active ingredient and in increasing patient compliance by reducing dosage frequency.

摘要翻译： 本发明涉及一种多微粒改性释放组合物，其在操作中以脉冲或双峰方式递送活性成分。 多微粒改性释放组合物包含立即释放组分和改性释放组分; 所述速释组分包含含有颗粒的第一组活性成分和所述改性释放组分，包含含有受控释放包衣的颗粒的第二组活性成分; 其中操作中的速释组分和改进释放组分的组合以脉冲或双峰方式递送活性成分。 本发明还涉及含有这种多微粒改性释放组合物的固体口服剂型。 通过多微粒改性释放组合物实现的血浆曲线有利于减少患者对活性成分的耐受性，并通过降低剂量频率提高患者依从性。