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    Powder-layered oral dosage forms
    2.
    发明授权
    Powder-layered oral dosage forms 失效
    粉末分层口服剂型

    公开(公告)号：US6077533A

    公开(公告)日：2000-06-20

    申请号：US5864

    申请日：1998-01-12

    申请人： Benjamin Oshlack ,  Frank Pedi

    发明人： Benjamin Oshlack ,  Frank Pedi

    IPC分类号： A61K9/16 ,  A61K9/50 ,  A61K9/62

    CPC分类号： A61K9/5078 ,  A61K9/1676

    摘要： An oral dosage form of morphine is formulated by powder-layering an homogeneous mixture of morphine sulfate and hydrous lactose impalpable onto inert beads to obtain a multiparticulate product. A plurality of the powder-layered beads may be administered either in immediate release form or in an extended release form by coating with a hydrophobic material. In addition, multi-particulate oral dosage forms containing therapeutically effective agents containing a plurality of pharmaceutically acceptable inert beads powder-layered with homogeneous mixture of a therapeutically effective agent and hydrous lactose impalpable are also disclosed. A method of preparing the dosage forms as well as a method preparing spheroids containing the homogeneous mixture of therapeutically effective agent and hydrous lactose impalpable are also disclosed.

    摘要翻译： 通过将硫酸吗啡和含水乳糖的均匀混合物粉末分层到惰性珠粒上来制备口服剂型，以获得多颗粒产品。 可以通过用疏水性材料涂布，以立即释放形式或延长释放形式施用多个粉末层状珠粒。 此外，还公开了含有治疗有效试剂的多颗粒口服剂型，其含有多个药物上可接受的惰性珠，粉末层叠有治疗有效剂和含水乳糖的均匀混合物。 还公开了制备剂型的方法以及制备含有治疗有效剂和含水乳糖的均匀混合物的球状体的方法。

    Opioid formulations having extended controlled released
    3.
    发明授权
    Opioid formulations having extended controlled released 失效
    具有延长受控释放的阿片制剂

    公开(公告)号：US5958459A

    公开(公告)日：1999-09-28

    申请号：US561829

    申请日：1995-11-27

    申请人： Mark Chasin ,  Benjamin Oshlack ,  Frank Pedi, Jr.

    发明人： Mark Chasin ,  Benjamin Oshlack ,  Frank Pedi, Jr.

    IPC分类号： A61K9/14 ,  A61K9/16 ,  A61K9/36 ,  A61K9/62

    CPC分类号： A61K9/14 ,  A61K9/16

    摘要： Solid controlled-release oral dosage forms comprising a therapeutically effective amount of an opioid analgesic or a salt thereof which provide an extended duration of pain relief of about 24 hours, have a dissolution rate in-vitro of the dosage form, when measured by the USP Paddle Method of 100 rpm in 900 ml aqueous buffer at 37.degree. C. from about 12.5% to about 42.5% (by weight) active agent released after 1 hour, from about 25% to about 55% (by weight) active agent released after 2 hours, from about 45% to about 75% (by weight) opioid analgesic released after 4 hours and greater than about 60% (by weight) opioid analgesic released after 8 hours, the in-vitro release rate being substantially independent of pH and chosen such that the peak plasma level of active agent obtained in-vivo between about 2 and about 8 hours after administration of the dosage form.

    摘要翻译： 包含治疗有效量的阿片类止痛剂或其盐的固体控制释放口服剂型提供延长的疼痛缓解时间约24小时，当通过USP测量时具有剂型的体外溶出速率 桨式法在900ml含水缓冲液中于37℃从约12.5％至约42.5％（重量）的活性剂在1小时后释放，约25％至约55％（重量）的活性剂释放出来后释放 2小时，约4小时后释放大约45％至大约75％（重量）的阿片样物质止痛剂，并且在8小时后释放大于约60％（重量）的阿片类止痛剂，体外释放速率基本上不依赖于pH和 选择使得在施用剂型后约2至约8小时之间在体内获得的活性剂的血浆水平峰值。

    Stabilized controlled release formulations having acrylic polymer coating
    5.
    发明授权
    Stabilized controlled release formulations having acrylic polymer coating 失效
    具有丙烯酸聚合物涂层的稳定的控释制剂

    公开(公告)号：US5286493A

    公开(公告)日：1994-02-15

    申请号：US826084

    申请日：1992-01-27

    申请人： Benjamin Oshlack ,  Mark Chasin ,  Frank Pedi, Jr.

    发明人： Benjamin Oshlack ,  Mark Chasin ,  Frank Pedi, Jr.

    IPC分类号： A61J3/06 ,  A61K9/22 ,  A61K9/28 ,  A61K9/32 ,  A61K9/50 ,  A61K9/52 ,  A61K9/54 ,  A61K9/58 ,  A61K9/62 ,  A61M37/00 ,  A61K9/00

    CPC分类号： A61K9/5026 ,  A61K9/2846 ,  A61K9/5078

    摘要： A stabilized solid controlled release dosage form having a coating derived from an aqueous dispersion of an acrylic polymer is obtained by overcoating a substrate including a therapeutically active with an aqueous dispersion of the plasticized acrylic polymer and then curing the coated substrate at a temperature above the glass transition temperature of the plasticized acrylic polymer, until the coated dosage form attains a stabilized dissolution profile substantially unaffected by exposure to storage conditions of elevated temperature and/or elevated relative humidity.

    摘要翻译： 具有衍生自丙烯酸类聚合物的水性分散体的涂层的稳定的固体控制释放剂型通过用包含增塑的丙烯酸类聚合物的水性分散体的包含治疗活性的底物进行外涂，然后在高于玻璃的温度下固化涂覆的基材 直到涂覆的剂型达到稳定的溶解曲线，基本上不受暴露于升高的温度和/或相对湿度升高的储存条件的影响。

    Powder-layered oral dosage forms
    6.
    发明授权
    Powder-layered oral dosage forms 有权

    公开(公告)号：US07060293B1

    公开(公告)日：2006-06-13

    申请号：US09598324

    申请日：2000-06-20

    申请人： Benjamin Oshlack ,  Frank Pedi, Jr.

    发明人： Benjamin Oshlack ,  Frank Pedi, Jr.

    IPC分类号： A61K9/62

    CPC分类号： A61K9/1676 ,  A61K9/5078

    摘要： An oral dosage form of morphine is formulated by powder-layering an homogeneous mixture of morphine sulfate and hydrous lactose impalpable onto inert beads to obtain a multiparticulate product. A plurality of the powder-layered beads may be administered either in immediate release form or in an extended release form by coating with a hydrophobic material. In addition, multi-particulate oral dosage forms containing therapeutically effective agents containing a plurality of pharmaceutically acceptable inert beads powder-layered with homogeneous mixture of a therapeutically effective agent and hydrous lactose impalpable are also disclosed. A method of preparing the dosage forms as well as a method preparing spheroids containing the homogeneous mixture of therapeutically effective agent and hydrous lactose impalpable are also disclosed.

    Opioid formulations having extended controlled release
    9.
    发明授权
    Opioid formulations having extended controlled release 有权
    具有延长受控释放的阿片制剂

    公开(公告)号：US6103261A

    公开(公告)日：2000-08-15

    申请号：US225959

    申请日：1999-01-06

    申请人： Mark Chasin ,  Benjamin Oshlack ,  Frank Pedi, Jr.

    发明人： Mark Chasin ,  Benjamin Oshlack ,  Frank Pedi, Jr.

    IPC分类号： A61K9/52 ,  A61K9/16 ,  A61K9/20 ,  A61K9/22 ,  A61K9/28 ,  A61K9/50 ,  A61K31/445 ,  A61K31/485 ,  A61K31/522 ,  A61K47/32 ,  A61K47/36 ,  A61K47/38 ,  A61K47/42 ,  A61K47/44 ,  A61P25/04

    CPC分类号： A61K9/1635 ,  A61K31/485 ,  A61K31/522 ,  A61K9/1617 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/2072 ,  A61K9/2081 ,  A61K9/2095 ,  A61K9/2866 ,  A61K9/5078

    摘要： Solid controlled-release oral dosage forms comprising a therapeutically effective amount of an opioid analgesic or a salt thereof which provide an extended duration of pain relief of about 24 hours, have a dissolution rate in-vitro of the dosage form, when measured by the USP Paddle Method of 100 rpm in 900 ml aqueous buffer at 37.degree. C. from about 12.5% to about 42.5% (by weight) active agent released after 1 hour, from about 25% to about 55% (by weight) active agent released after 2 hours, from about 45% to about 75% (by weight) opioid analgesic released after 4 hours and greater than about 60% (by weight) opioid analgesic released after a hours, the in-vitro release rate being substantially independent of pH and chosen such that the peak plasma level of active agent obtained in-vivo between about 2 and about 8 hours after administration of the dosage form.

    摘要翻译： 包含治疗有效量的阿片类止痛剂或其盐的固体控制释放口服剂型提供延长的疼痛缓解时间约24小时，当通过USP测量时具有剂型的体外溶出速率 桨式法在900ml含水缓冲液中于37℃从约12.5％至约42.5％（重量）的活性剂在1小时后释放，约25％至约55％（重量）的活性剂释放出来后释放 2小时，4小时后释放的约45％至约75％（重量）的阿片样物质止痛剂，并且大约约60％（重量）阿片类镇痛剂在一小时后释放，体外释放速率基本上不依赖于pH和 选择使得在施用剂型后约2至约8小时之间在体内获得的活性剂的血浆水平峰值。