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    Methods for making pharmaceutical formulations comprising deagglomerated microparticles
    1.
    发明申请
    Methods for making pharmaceutical formulations comprising deagglomerated microparticles 审中-公开
    制备包含解聚微粒的药物制剂的方法

    公开(公告)号：US20060093678A1

    公开(公告)日：2006-05-04

    申请号：US11305620

    申请日：2005-12-16

    申请人： Donald Chickering ,  Shaina Reese ,  Sridhar Narasimhan ,  Julie Straub ,  Howard Bernstein ,  David Altreuter ,  Eric Huang

    发明人： Donald Chickering ,  Shaina Reese ,  Sridhar Narasimhan ,  Julie Straub ,  Howard Bernstein ,  David Altreuter ,  Eric Huang

    IPC分类号： A61K9/14

    CPC分类号： B01D1/18 ,  A61K9/0075 ,  A61K9/145 ,  A61K9/1647 ,  A61K9/1694 ,  B01J2/04

    摘要： Methods are provided for making a dry powder blend pharmaceutical formulation comprising (i) forming microparticles which comprise a pharmaceutical agent; (ii) providing at least one excipient in the form of particles having a volume average diameter that is greater than the volume average diameter of the microparticles; (iii) blending the microparticles with the excipient to form a powder blend; and (iv) jet milling the powder blend to deagglomerate at least a portion of any of the microparticles which have agglomerated, while substantially maintaining the size and morphology of the individual microparticles. Jet milling advantageously can eliminate the need for more complicated wet deagglomeration processes, can lower residual moisture and solvent levels in the microparticles (which leads to better stability and handling properties for dry powder formulations), and can improve wettability, suspendability, and content uniformity of dry powder blend formulations.

    摘要翻译： 提供用于制备干粉混合物药物制剂的方法，其包含（i）形成包含药剂的微粒; （ii）提供至少一种具有体积平均直径大于微粒的体积平均直径的颗粒形式的赋形剂; （iii）将微粒与赋形剂混合以形成粉末混合物; 和（iv）喷射研磨粉末共混物以使至少一部分具有附聚的任何微粒分解，同时基本保持各个微粒的尺寸和形态。 喷射铣削有利地可以消除对更复杂的湿解聚过程的需要，可以降低微粒中的残留水分和溶剂水平（这导致干粉配方的更好的稳定性和处理性能），并且可以改善润湿性，悬浮性和含量均匀性 干粉混合配方。

    METHODS FOR MAKING AND USING PARTICULATE PHARMACEUTICAL FORMULATIONS FOR SUSTAINED RELEASE
    4.
    发明申请
    METHODS FOR MAKING AND USING PARTICULATE PHARMACEUTICAL FORMULATIONS FOR SUSTAINED RELEASE 审中-公开
    制备和使用颗粒状药物制剂用于持续释放的方法

    公开(公告)号：US20070264343A1

    公开(公告)日：2007-11-15

    申请号：US11829629

    申请日：2007-07-27

    申请人： Howard Bernstein ,  Donald Chickering ,  Eric Huang ,  Sridhar Narasimhan ,  Shaina Reese ,  Julie Straub

    发明人： Howard Bernstein ,  Donald Chickering ,  Eric Huang ,  Sridhar Narasimhan ,  Shaina Reese ,  Julie Straub

    IPC分类号： A61K9/14 ,  A61K31/56 ,  A61K31/7088 ,  A61K38/00 ,  A61K9/10

    CPC分类号： A61K9/1647 ,  A61K9/1617

    摘要： Pharmaceutical formulations and methods are provided for the sustained delivery of a pharmaceutical agent to a patient by injection. The injectable formulation includes porous microparticles which comprise a pharmaceutical agent and a matrix material, wherein upon injection of the formulation a therapeutically or prophylactically effective amount of the pharmaceutical agent is released from the microparticles for at least 24 hours. A method for making the injectable, sustained release pharmaceutical formulation may include dissolving a hydrophobic matrix material in a volatile solvent to form a first solution; adding a pharmaceutical agent to the first solution to form an emulsion, suspension, or second solution; and removing the volatile solvent from the emulsion, suspension, or second solution to yield porous microparticles which comprise the pharmaceutical agent dispersed, entrapped or encapsulated within the structure of the hydrophobic matrix material.

    摘要翻译： 提供药物制剂和方法用于通过注射将药剂持续递送至患者。 可注射制剂包括包含药剂和基质材料的多孔微粒，其中在注射制剂时，治疗或预防有效量的药剂从微粒释放至少24小时。 制备可注射的缓释药物制剂的方法可包括将疏水基质材料溶解在挥发性溶剂中以形成第一溶液; 向第一溶液中加入药剂以形成乳液，悬浮液或第二溶液; 并从乳液，悬浮液或第二溶液中除去挥发性溶剂以产生包含在疏水基质材料的结构内分散，包埋或包封的药剂的多孔微粒。

    Injectable, oral, or topical sustained release pharmaceutical formulations
    5.
    发明申请
    Injectable, oral, or topical sustained release pharmaceutical formulations 审中-公开
    注射剂，口服或局部持续释放药物制剂

    公开(公告)号：US20050069591A1

    公开(公告)日：2005-03-31

    申请号：US10950856

    申请日：2004-09-27

    申请人： Howard Bernstein ,  Donald Chickering ,  Eric Huang ,  Sridhar Narasimhan ,  Shaina Reese ,  Julie Straub

    发明人： Howard Bernstein ,  Donald Chickering ,  Eric Huang ,  Sridhar Narasimhan ,  Shaina Reese ,  Julie Straub

    IPC分类号： A61K9/16 ,  A61K48/00 ,  A61K9/14 ,  A61K31/56 ,  A61K38/17

    CPC分类号： A61K9/1647 ,  A61K9/1617

    摘要： Pharmaceutical formulations and methods are provided for the sustained delivery of a pharmaceutical agent to a patient by injection, by oral administration or by topical administration. The injectable formulation includes porous microparticles which comprise a pharmaceutical agent and a matrix material, wherein upon injection of the formulation a therapeutically or prophylactically effective amount of the pharmaceutical agent is released from the microparticles for at least 24 hours. The oral formulation includes porous microparticles which comprise a pharmaceutical agent and a matrix material, wherein a therapeutically or prophylactically effective amount of the pharmaceutical agent is released from the microparticles for at least 2 hours following oral administration. The topical formulation includes porous microparticles which comprise a pharmaceutical agent and a matrix material, wherein a therapeutically or prophylactically effective amount of the pharmaceutical agent is released from the microparticles for at least 2 hours following topical administration.

    摘要翻译： 提供药物制剂和方法用于通过注射，口服给药或通过局部给药将药剂持续递送至患者。 可注射制剂包括包含药剂和基质材料的多孔微粒，其中在注射制剂时，治疗或预防有效量的药剂从微粒释放至少24小时。 口服制剂包括包含药剂和基质材料的多孔微粒，其中在口服给药后至少2小时将治疗或预防有效量的药剂从微粒释放至少2小时。 局部制剂包括包含药剂和基质材料的多孔微粒，其中治疗或预防有效量的药剂在局部给药后从微粒释放至少2小时。