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1. 发明授权

US4851228A Multiparticulate controlled porosity osmotic 失效
标题翻译：多重控制孔隙渗透
公开(公告)号：US4851228A
公开(公告)日：1989-07-25
申请号：US73596
申请日：1987-07-15
申请人： Gaylen M. Zentner , Kenneth J. Himmelstein , Gerald S. Rork
发明人： Gaylen M. Zentner , Kenneth J. Himmelstein , Gerald S. Rork
IPC分类号： A61K9/00 , A61K9/64
CPC分类号： A61K9/0004
摘要： The instant invention is directed to a multiparticulate osmotic pump, for the controlled release of a pharmaceutically active agent to an environment of use, said pump comprising:(I) a carrier medium which does not maintain its integrity in the environment of use;(II) a multiple of tiny osmotic pump elements each consisting essentially of:(A) a core comprises at least one pharmacologically active agent soluble in an external fluid, or a mixture of an agent having a limited solubility in the external fluid with an osmotically effective solute that is soluble in the fluid, which exhibit an osmotic pressure gradient across the wall against the external fluid surrounded by(B) a rate controlling water insoluble wall, having a fluid permeability of 6.96.times.10.sup.-18 to 6.96.times.10.sup.14 cm.sup.3 sec/g and a reflection coefficient of less than 0.5, prepared from:(i) a polymer permeable to water but impermeable to solute and(ii) 0.1 to 60% by weight, based on the total weight of (i) and (ii), of at least one pH insensitive pore forming additive dispersed throughout said wall.
摘要翻译：本发明涉及多颗粒渗透泵，用于将药物活性剂控制释放到使用环境中，所述泵包括：（I）在使用环境中不保持其完整性的载体介质; （II）多个微小的渗透泵元件，其各自主要由以下组成：（A）芯包含至少一种可溶于外部流体的药理学活性剂，或在外部流体中具有有限溶解度的试剂与渗透性的混合物可溶于流体的有效溶质，其表现出渗透压梯度横跨壁对抗由外界流体包围的外部流体（B）速率控制水不溶性壁，流体渗透率为6.96×10-18至6.96×1013cm3 / g 和反射系数小于0.5，由以下因素制备：（i）可渗透水但不溶于溶质的聚合物，和（ii）基于（i）和（ii）的总重量为0.1-60重量％至少一种pH不敏感的成孔添加剂分散在整个壁上。

2. 发明授权

US4968507A Controlled porosity osmotic pump 失效
标题翻译：可控孔隙渗透泵
公开(公告)号：US4968507A
公开(公告)日：1990-11-06
申请号：US073781
申请日：1987-07-15
申请人： Gaylen M. Zentner , Gerald S. Rork , Kenneth J. Himmelstein
发明人： Gaylen M. Zentner , Gerald S. Rork , Kenneth J. Himmelstein
IPC分类号： A61K9/00 , A61K9/64
CPC分类号： A61K9/0004
摘要： The instant invention is directed to an osmotic pump comprising:(A) at least one active agent surrounded by(B) a rate controlling water insoluble wall, having a fluid permeability of 6.96.times.10.sup.-18 to 6.96.times.10.sup.-14 cm.sup.3 sec/g and a reflection coefficient of less than 1, prepared from:(i) a polymer permeable to water but impermeable to solute and(ii) 0.1 to 60% by weight, based on the total weight of (i) and (ii), of at least one pH insensitive pore forming additive dispersed throughout said wall.
摘要翻译：本发明涉及一种渗透泵，其包括：（A）由（B）速率控制水不溶性壁包围的至少一种活性剂，其流体渗透性为6.96×10-18至6.96×10-14厘米3秒/克，反应系数小于1，由以下因素制备：（i）可渗透水但不溶于溶质的聚合物，和（ii）基于（i）和（ii）的总重量为0.1-60重量％至少一种pH不敏感的成孔添加剂分散在整个所述壁上。

3. 发明授权

US5366738A Controlled release drug dispersion delivery device 失效
标题翻译：控释药物分散体输送装置
公开(公告)号：US5366738A
公开(公告)日：1994-11-22
申请号：US118836
申请日：1993-09-08
申请人： Gerald S. Rork , James D. Pipkin
发明人： Gerald S. Rork , James D. Pipkin
IPC分类号： A61K9/00 , A61K9/20 , A61K9/22 , A61K9/24
CPC分类号： A61K9/0004 , A61K9/2027 , A61K9/2072
摘要： A device for the controlled delivery of a beneficial agent as a gelatinous dispersion consisting of (i) a core which contains a beneficial agent, a polymer which forms gelatinous microscopic particles upon hydration and if desired an agent to modulate the hydration of the polymer; and (ii) an impermeable, insoluble coating which adheres to and surrounds the core and contains apertures which provide an area for the hydration and release of a dispersion comprising gelatinous microscopic particles.
摘要翻译：用于作为凝胶状分散体受控输送有益剂的装置，其包含（i）含有有益试剂的核心，在水合时形成凝胶状微粒子的聚合物，如果需要，调节聚合物水合的试剂; 和（ii）不渗透的不溶性涂层，其粘附并包围芯并且包含孔，其提供用于水合和释放包含凝胶微观颗粒的分散体的区域。

4. 发明授权

US5882682A Controlled release simvastatin delivery device 失效
标题翻译：对照释放辛伐他汀递送装置
公开(公告)号：US5882682A
公开(公告)日：1999-03-16
申请号：US817129
申请日：1997-08-01
申请人： Gerald S. Rork , James D. Pipkin
发明人： Gerald S. Rork , James D. Pipkin
IPC分类号： A61K9/00 , A61K9/20 , A61K9/22 , A61K9/32 , A61K9/36 , A61K31/4422 , A61K9/24
CPC分类号： A61K9/2027 , A61K31/4422 , A61K9/0004 , A61K9/2072
摘要： Controlled delivery of a beneficial agent in a dispersion is provided using (i) a compressed core which contains the beneficial agent, a polymer which forms gelatinous microscopic particles upon hydration, and if desired, an agent to modulate the hydration; and (ii) a water insoluble coating which adheres to and surrounds the core and contains apertures which provide an area for the hydration and release of the dispersion. The release rate of the beneficial agent is a function of the number and size of the apertures in the coating.
摘要翻译： PCT No.PCT / US95 / 13693 Sec。 371日期：1997年8月1日 102（e）1997年8月1日PCT PCT 1995年10月19日PCT公布。公开号WO96 / 12478 日期1996年5月2日使用（i）包含有益试剂的压缩芯，在水合时形成凝胶微观颗粒的聚合物，以及如果需要，调节水合作用的试剂，提供分散体中的有益试剂的控制输送。和（ii）水不溶性涂层，其粘附并包围芯并且包含提供用于水分和释放分散体的区域的孔。有益剂的释放速率是涂层中孔的数量和尺寸的函数。

5. 发明授权

US5543154A Controlled release nifedipine delivery device 失效
标题翻译：控释硝苯地平递送装置
公开(公告)号：US5543154A
公开(公告)日：1996-08-06
申请号：US327083
申请日：1994-10-21
申请人： Gerald S. Rork , James D. Pipkin
发明人： Gerald S. Rork , James D. Pipkin
IPC分类号： A61K9/00 , A61K9/20 , A61K9/22 , A61K9/32 , A61K9/36 , A61K31/4422 , A61K9/24
CPC分类号： A61K9/2027 , A61K31/4422 , A61K9/0004 , A61K9/2072
摘要： A device for the controlled delivery of a beneficial agent as a gelatinous dispersion consisting of (i) a core which contains a beneficial agent, a polymer which forms gelatinous micoroscopic particles upon hydration and if desired an agent to modulate the hydration of the polymer; and (ii) an impermeable, insoluble coating which adheres to and surrounds the core and contains apertures which provide an area for the hydration and release of a disperson comprising gelatinous microscopic particles.
摘要翻译：用于作为凝胶状分散体受控输送有益剂的装置，其包含（i）含有有益试剂的核心，在水合时形成凝胶状微观观察颗粒的聚合物，如果需要，调节聚合物水合的试剂; 和（ii）不渗透的不溶性涂层，其粘附并包围芯并且包含孔，其提供用于水合和释放包含凝胶状微观颗粒的分散体的区域。

6. 发明授权

US5582838A Controlled release drug suspension delivery device 失效
标题翻译：控制释放药物悬浮液输送装置
公开(公告)号：US5582838A
公开(公告)日：1996-12-10
申请号：US363451
申请日：1994-12-22
申请人： Gerald S. Rork , James D. Pipkin
发明人： Gerald S. Rork , James D. Pipkin
IPC分类号： A61K9/24 , A61J3/10 , A61K9/20 , A61K9/32 , A61K9/36
CPC分类号： A61K9/2072 , A61K9/2086
摘要： A device is disclosed for the controlled delivery of a beneficial agent, the device consisting of (i) a core comprising at least two layers, wherein at least one layer comprises a beneficial agent and a polymer which forms microscopic gel beads upon hydration and at least one layer which comprises a polymer which forms microscopic gel beads upon hydration; and (ii) an impermeable, insoluble coating which adheres to and surrounds the core and contains apertures which provide an area for the hydration and release of the microscopic gel beads.
摘要翻译：公开了一种用于受控输送有益试剂的装置，该装置由（i）包含至少两层的芯组成，其中至少一层包含有益试剂和在水合时形成微细凝胶珠的聚合物，并且至少一层，其包含在水合时形成微观凝胶珠的聚合物; 和（ii）不渗透的不溶性涂层，其粘附并包围芯并且包含提供用于微细凝胶珠的水合和释放的区域的孔。

7. 发明授权

US4886668A Multiparticulate controlled porosity osmotic pump 失效
标题翻译：多粒度控制孔隙渗透泵
公开(公告)号：US4886668A
公开(公告)日：1989-12-12
申请号：US100676
申请日：1987-09-24
申请人： John L. Haslam , Gerald S. Rork
发明人： John L. Haslam , Gerald S. Rork
IPC分类号： A61K9/00 , A61K31/55
CPC分类号： A61K9/0004 , A61K31/55
摘要： The instant invention is directed to a multiparticulate osmotic pump, for the controlled release of diltiazem L-malate to an environment of use, said pump comprising:(I) a carrier medium which does not maintain its integrity in the environment of use;(II) a multiple of tiny osmotic pump elements each comprising:(A) a core comprises diltiazem L-malate and an effective buffering amount of sodium bitartrate surrounded by(B) a rate controlling water insoluble wall, having a fluid permeability of 6.96.times.10.sup.-18 to 6.96.times.10.sup.-14 cm.sup.3 sec/g and a reflection coefficient of less than 0.5, prepared from:(i) a polymer permeable to water but impermeable to solute and(ii) 0.1 to 60% by weight, based on the total weight of (i) and (ii), of at least one pH insensitive pore forming additive dispersed throughout said wall,wherein the total amount of diltiazem L-malate in all of the osmotic pump elements is a therapeutically effective amount.
摘要翻译：本发明涉及一种多颗粒渗透泵，用于将地尔硫卓L-苹果酸盐控制释放到使用环境中，所述泵包括：（I）在使用环境中不保持其完整性的载体介质; （II）多个微小的渗透泵元件，每个包含：（A）核心包括地尔硫卓L-苹果酸盐和有效缓冲量的由（B）速率控制水不溶性壁包围的硼酸酒石酸钠，其流体渗透性为6.96×10 -18至6.96×10 14 cm 3 / g和反射系数小于0.5，由以下因素制备：（i）可渗透水但不溶于溶质的聚合物，和（ii）基于总计的0.1-60重量％分散在整个壁上的至少一种pH不敏感的形成孔的添加剂的（i）和（ii）的重量，其中所有渗透泵元件中的地尔硫卓L-苹果酸盐的总量是治疗有效量。

8. 发明授权

US4880631A Controlled porosity osmotic pump 失效
标题翻译：可控孔隙渗透泵
公开(公告)号：US4880631A
公开(公告)日：1989-11-14
申请号：US100665
申请日：1987-09-24
申请人： John L. Haslam , Gerald S. Rork
发明人： John L. Haslam , Gerald S. Rork
IPC分类号： A61K9/00 , A61K31/55
CPC分类号： A61K9/0004 , A61K31/55
摘要： The instant invention is directed to an osmotic pump, for the controlled release of diltiazem L-malate to an environment of use, said pump comprising:(A) a core which comprises a therapeutically effective amount of diltiazem L-malate and an effective buffering amount of sodium bitartrate surrounded by(B) a rate controlling water insoluble wall, having a fluid permeability of 6.96.times.10.sup.-18 to 6.96.times.10.sup.-14 cm.sup.3 sec/g and a reflection coefficient of less than 0.5, prepared from:(i) a polymer permeable to water but impermeable to solute and(ii) 0.1 to 60% by weight, based on the total weight of (i) and (ii), of at least one pH insensitive pore forming additive dispersed throughout said wall.
摘要翻译：本发明涉及渗透泵，用于将地尔硫卓L-苹果酸盐控制释放到使用环境中，所述泵包括：（A）核心，其包含治疗有效量的地尔硫卓L-苹果酸盐和有效缓冲量由（B）速率控制水不溶性壁包围的酒石酸氢钠，其流体渗透性为6.96×10-18至6.96×10-14厘米3秒/克，反射系数小于0.5，由以下物质制备：（i）聚合物可渗透水，但不溶于溶质，和（ii）基于（i）和（ii）总重量的0.1至60重量％的分散在所述壁上的至少一种pH不敏感的成孔添加剂。

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