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1. 发明申请

WO2004004684A8 CONTROLLED-RELEASE PHARMACEUTICAL FORMULATIONS 审中-公开
标题翻译：控制释放药物制剂
公开(公告)号：WO2004004684A8
公开(公告)日：2004-12-29
申请号：PCT/IB0302877
申请日：2003-06-26
申请人： PFIZER PROD INC , BERCHIELLI ALFRED , DAUGHERITY PATRICK DAVID , SHAMBLIN SHERI LYNN , THOMBRE AVINASH GOVIND , WATERMAN KENNETH CRAIG
发明人： BERCHIELLI ALFRED , DAUGHERITY PATRICK DAVID , SHAMBLIN SHERI LYNN , THOMBRE AVINASH GOVIND , WATERMAN KENNETH CRAIG
IPC分类号： A61K9/00 , A61K9/22 , A61K31/4433
CPC分类号： A61K31/4433 , A61K9/0004
摘要： The invention provides controlled release pharmaceutical formulations having a coated core with the core comprising a drug-containing composition and a waterswellable composition, each occupying essentially separate regions within the core. The drug-containing composition comprises a PDE4D inhibitor, or a pharmaceutically acceptable salt thereof, preferably (R)-2-[4-({[2-(benzo[1,3]dioxol-5-yloxy)-pyridine-3carbonyl]-amino}-methyl)-3-fluoro-phenoxy]-propionic acid, or a pharmaceutically acceptable salt thereof, or 2-(4-fluorophenoxy)-N-[4-(1-hydroxy-1-methyl-ethyl)benzyl]-nicotinamide, or a pharmaceutically acceptable salt thereof, and a drug entraining agent. The coating around the core is water-permeable, water-insoluble, and has at least one delivery port therethrough. The invention further provides methods of reducing the nausea and emetic effects of PDE4D inhibitors, and controlled-release formulations having improved PDE4D inhibitor in vivo and in vitro profiles.
摘要翻译：本发明提供具有包衣核心的控释药物制剂，其核心包含含药物的组合物和每个占据核心内基本上分开的区域的可饮用水的组合物。含有药物的组合物包含PDE4D抑制剂或其药学上可接受的盐，优选（R）-2- [4 - （{[2-（苯并[1,3]二氧杂环戊烯-5-基氧基） - 吡啶-3-羰基] - 氨基} - 甲基）-3-氟 - 苯氧基] - 丙酸或其药学上可接受的盐，或2-（4-氟苯氧基）-N- [4-（1-羟基-1-甲基 - 乙基）苄基 ] - 烟酰胺或其药学上可接受的盐，以及药物吸入剂。芯周围的涂层是透水的，不溶于水的，并且具有至少一个通过其的输送口。本发明还提供减少PDE4D抑制剂的恶心和止吐作用的方法，以及具有改善的PDE4D抑制剂的体内和体外外观特征的控制释放制剂。

2. 发明申请

WO0147498A2 HYDROGEL-DRIVEN LAYERED DRUG DOSAGE FORM 审中-公开
标题翻译：氢化驱动剂层剂量形式
公开(公告)号：WO0147498A2
公开(公告)日：2001-07-05
申请号：PCT/IB0001871
申请日：2000-12-13
申请人： PFIZER PROD INC , CURATOLO WILLIAM JOHN , FERGIONE MICHAEL BRUCE , ROY MICHAEL CHRISTOPHER , THOMBRE AVINASH GOVIND , WATERMAN KENNETH CRAIG , APPEL LEAH ELIZABETH , BEYERINCK RONALD ARTHUR , CHIDLAW MARK BRIAN , FRIESEN DWAYNE THOMAS , SUPPLEE DANIELLE
发明人： CURATOLO WILLIAM JOHN , FERGIONE MICHAEL BRUCE , ROY MICHAEL CHRISTOPHER , THOMBRE AVINASH GOVIND , WATERMAN KENNETH CRAIG , APPEL LEAH ELIZABETH , BEYERINCK RONALD ARTHUR , CHIDLAW MARK BRIAN , FRIESEN DWAYNE THOMAS , SUPPLEE DANIELLE
IPC分类号： A61K9/26 , A61K9/00 , A61K9/22 , A61K9/36 , A61K31/135 , A61K47/10 , A61K47/12 , A61K47/26 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/38 , A61P3/04 , A61P15/00 , A61P15/10 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/30 , A61P43/00
CPC分类号： A61K9/0004 , A61K31/135 , Y10S514/951
摘要： A controlled release dosage form for sertraline has a core comprising a sertraline-containing composition and a water-swellable composition wherein the water-swellable composition is in a separate region within the core. A coating around the core is water-permeable, water-insoluble, and has at least one delivery port therethrough. In one embodiment, the dosage form releases sertraline to the use environment at an average rate of 6 to 10 wt.% per hour from the second to the twentieth hour after introduction to a use environment and less than about 25 wt.% for the first two hours and at least 70 wt.% by the twelfth hour, where the percentages correspond to the mass of drug released from the tablet divided by the total mass of drug originally present in the tablet. In another embodiment, the dosage form releases less than about 25 wt.% of sertraline to the use environment by the second hour after introduction of the dosage form to the use environment, and delivers at least 25 wt.% from the eighth to the twenty-fourth hour.
摘要翻译：舍曲林的控制释放剂型具有包含含舍曲林组合物和水溶胀性组合物的核心，其中水溶胀性组合物在核心内的分离区域中。芯周围的涂层是透水的，不溶于水的，并且具有至少一个通过其的输送口。在一个实施方案中，剂型在引入使用环境后的第二至第二十小时以平均速率以每小时6至10重量％的平均速率将舍曲林释放至使用环境，并且对于第一个，小于约25重量％两小时至少70重量％，其中百分比对应于从片剂释放的药物的质量除以最初存在于片剂中的药物的总质量。在另一个实施方案中，在将剂型引入使用环境后第二小时，剂型释放小于约25重量％的舍曲林至使用环境，并将至少25重量％从第八次释放到二十第四小时

3. 发明申请

WO2006024949A3 CONTROLLED RELEASE DOSAGE FORMS COMBINING IMMEDIATE RELEASE AND SUSTAINED RELEASE OF LOW-SOLUBILITY DRUG 审中-公开
标题翻译：控制释放剂量形式结合立即释放和持续释放低溶解性药物
公开(公告)号：WO2006024949A3
公开(公告)日：2006-05-04
申请号：PCT/IB2005002825
申请日：2005-08-19
申请人： PFIZER PROD INC , APPEL LEAH ELIZABETH , FRIESEN DWAYNE THOMAS , HERBIG SCOTT MAX , THOMBRE AVINASH GOVIND
发明人： APPEL LEAH ELIZABETH , FRIESEN DWAYNE THOMAS , HERBIG SCOTT MAX , THOMBRE AVINASH GOVIND
IPC分类号： A61K9/20 , A61K9/50 , A61K31/496
CPC分类号： A61K9/209 , A61K9/2031 , A61K9/2081 , A61K9/2846
摘要： A controlled release dosage form comprises an immediate release portion and an enteric coated sustained release core.
摘要翻译：控释剂型包含立即释放部分和肠溶衣缓释核心。

4. 发明申请

WO2004009283A3 PHARMACEUTICAL LASER DRILLING SYSTEM WITH MEANS FOR CHECKING THE CORRECT ORIENTATION OF EACH DOSAGE 审中-公开
标题翻译：具有检查每个剂量的正确方向的手段的药物激光钻孔系统
公开(公告)号：WO2004009283A3
公开(公告)日：2004-04-22
申请号：PCT/IB0303133
申请日：2003-07-11
申请人： PFIZER PROD INC , CARRUTHERS MARK SAMUEL , THOMBRE AVINASH GOVIND , CRAIG CHRISTOPHER DONAVAN , MILLARD DOUGLAS LEE , NEWBOLD DAVID DIXON , SPENCE KENNY RAY
发明人： CARRUTHERS MARK SAMUEL , THOMBRE AVINASH GOVIND , CRAIG CHRISTOPHER DONAVAN , MILLARD DOUGLAS LEE , NEWBOLD DAVID DIXON , SPENCE KENNY RAY
IPC分类号： A61J3/06 , A61J3/00 , B23K26/04 , B23K26/08 , B23K26/14 , B23K26/38 , B23K26/42 , A61K9/00 , A61K9/20 , B07C5/342 , B07C5/36 , B65G47/256
CPC分类号： B23K26/032 , A61J3/005 , A61J2205/20 , B23K26/04 , B23K26/0648 , B23K26/0665 , B23K26/0838 , B23K26/142 , B23K26/1462 , B23K26/1476 , B23K26/382 , B23K26/40 , B23K2201/35
摘要： A laser drilling system (10) forms an opening in the coating of a pharmaceutical dosage form and includes an orientation check assembly to check the correct orientation of each dosage form before the laser drilling is performed, a debris removal assembly to reduce buildup of and reduce exposure to drilling debris and a quality control assembly to verify that the opening formed conforms to predetermined specifications. The orientation check assembly comprises first and second link conveyors, one first color sensor (52) located adjacent the first link conveyor and generating a signal representative of the color of the pharmaceutical dosage form, and a rejection station located along said first link conveyor for ejecting said dosage form in response to said signal generated by said color sensor (52).
摘要翻译：激光钻孔系统（10）在药物剂型的涂层中形成开口，并且包括在进行激光钻孔之前检查每个剂型的正确取向的取向检查组件，用于减少积聚和减少的碎屑去除组件暴露于钻屑和质量控制组件，以验证形成的开口符合预定规格。定向检查组件包括第一和第二连杆输送机，位于第一连杆输送机附近的一个第一颜色传感器（52），并产生代表药物剂型的颜色的信号，以及位于沿着所述第一连杆输送机排出的排出台所述剂型响应由所述颜色传感器（52）产生的所述信号。

5. 发明申请

WO2005053650A8 AZITHROMYCIN DOSAGE FORMS WITH REDUCED SIDE EFFECTS 审中-公开
标题翻译： AZITHROMYCIN剂型减少副作用
公开(公告)号：WO2005053650A8
公开(公告)日：2005-12-01
申请号：PCT/IB2004001654
申请日：2004-05-14
申请人： PFIZER PROD INC , HAGEN TIMOTHY ARTHUR , HERBIG SCOTT MAX , LO JULIAN BELKNAP , THOMBRE AVINASH GOVIND , APPEL LEAH ELIZABETH , CREW MARSHALL DAVID , FRIESEN DWAYNE THOMAS , LYON DAVID KEITH , MCCRAY SCOTT BALDWIN , WEST JAMES BLAIR
发明人： HAGEN TIMOTHY ARTHUR , HERBIG SCOTT MAX , LO JULIAN BELKNAP , THOMBRE AVINASH GOVIND , APPEL LEAH ELIZABETH , CREW MARSHALL DAVID , FRIESEN DWAYNE THOMAS , LYON DAVID KEITH , MCCRAY SCOTT BALDWIN , WEST JAMES BLAIR
IPC分类号： C07H17/00 , A61K9/00 , A61K9/16 , A61K9/20 , A61K31/7052 , A61K47/02 , A61K47/14 , A61K47/18 , A61K47/44 , A61P31/04
CPC分类号： A61K9/1611 , A61K9/143 , A61K9/1617 , A61K9/1623 , A61K9/1635 , A61K9/1641 , A61K9/1694 , A61K9/2009 , A61K9/2013 , A61K9/2031 , A61K31/7052
摘要： An oral dosage form comprising azithromycin and an effective amount of an alkalizing agent. Preferably, said oral dosage form comprises an effective amount of an alkalizing agent and an azithromycin multiparticulate wherein said multiparticulate comprises azithromycin, a mixture of glyceryl monobehenate, glyceryl dibehenate and glyceryl tribehenate, and a poloxamer. Typically, the oral dosage form includes any suitable oral dosing means such as a powder for oral suspension, a unit dose packet or sachet, a tablet or a capsule.Additionally disclosed is an oral suspension comprising azithromycin, an effective amount of an alkalizing agent and a vehicle. Preferably, the azithromycin is in multiparticulate form wherein said multiparticulate comprises azithromycin, a mixture of glyceryl monobehenate, glyceryl dibehenate and glyceryl tribehenate,and a poloxamer. Also disclosed is a method for reducing gastrointestinal side effects, associated with administering azithromycin to a mammal, comprising contiguously administering azithromycin and an effective amount of alkalizing agent to said mammal wherein the frequency of gastrointestinal side effects is lower than that experienced by administering an equal dose of azithromycin without said alkalizing agent.Further disclosed is a method of treating a bacterial or protozoal infection in a mammal in need thereof comprising contiguously administering to said mammal a single dose of an oral dosage form wherein said oral dosage form comprises azithromycin and an effective amount of an alkalizing agent.Additionally disclosed are azithromycin multiparticulates comprising azithromycin, a surfactant; and a pharmaceutically acceptable carrier.
摘要翻译：包含阿奇霉素和有效量的碱化剂的口服剂型。优选地，所述口服剂型包含有效量的碱化剂和阿奇霉素多颗粒，其中所述多颗粒包含阿奇霉素，单山嵛酸甘油酯，二苯乙酸甘油酯和枸橼酸甘油酯和泊洛沙姆的混合物。通常，口服剂型包括任何合适的口服给药方式，例如用于口服悬浮液的粉末，单位剂量包或小药囊，片剂或胶囊。另外公开的是包含阿奇霉素，有效量的碱化剂和一辆车。优选地，阿奇霉素是多颗粒形式，其中所述多颗粒包括阿奇霉素，甘油单山嵛酸甘油酯，二苯甲酸甘油酯和枸橼酸甘油酯和泊洛沙姆的混合物。还公开了一种减少与向哺乳动物施用阿奇霉素相关的胃肠道副作用的方法，包括向所述哺乳动物连续施用阿奇霉素和有效量的碱化剂，其中胃肠道副作用的频率低于施用相等剂量的阿奇霉素。没有所述碱化剂的阿奇霉素的进一步公开是一种在有需要的哺乳动物中治疗细菌或原生动物感染的方法，其包括向所述哺乳动物连续施用单剂量的口服剂型，其中所述口服剂型包含阿奇霉素和有效量的碱性试剂。另外公开了包含阿奇霉素，表面活性剂的阿奇霉素多颗粒; 和药学上可接受的载体。

6. 发明申请

WO0211702A3 HYDROGEL-DRIVEN DRUG DOSAGE FORM 审中-公开
标题翻译： HYDROGEL-DRIVEN DRUG剂型
公开(公告)号：WO0211702A3
公开(公告)日：2002-11-28
申请号：PCT/IB0101390
申请日：2001-08-03
申请人： PFIZER PROD INC , APPEL LEAH ELIZABETH , BABCOCK WALTER C , BEYERINCK RONALD ARTHUR , CHIDLAW MARK BRIAN , CURATOLO WILLIAM JOHN , FRIESEN DWAYNE THOMAS , HERBIG SCOTT MAX , THOMBRE AVINASH GOVIND
发明人： APPEL LEAH ELIZABETH , BABCOCK WALTER C , BEYERINCK RONALD ARTHUR , CHIDLAW MARK BRIAN , CURATOLO WILLIAM JOHN , FRIESEN DWAYNE THOMAS , HERBIG SCOTT MAX , THOMBRE AVINASH GOVIND
IPC分类号： A61K9/00 , A61K9/20 , A61K9/22 , A61K9/24 , A61K31/135 , A61K31/353 , A61K31/4178 , A61K31/4422 , A61K31/496 , A61K31/519 , A61K31/5377 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/16 , A61K47/26 , A61K47/30 , A61K47/34 , A61K47/36 , A61K47/38 , A61K47/42
CPC分类号： A61K9/0004 , A61K9/2077 , A61K9/2086 , A61K9/209
摘要： A controlled release dosage form has a coated core with the core comprising a drug-containing composition and a water-swellable composition, each occupying separate regions within the core. The coating around the core is water-permeable, water-insoluble and has at least one delivery port therethrough. A variety of geometric arrangements are disclosed.
摘要翻译：控释剂型具有涂覆的核心，其核心包含含药物的组合物和水溶胀性组合物，每个组合物占据核心内的分开的区域。芯周围的涂层是透水的，不溶于水的，并且具有至少一个通过其的输送口。公开了各种几何布置。

7. 发明专利

CA2537413A1 SUSTAINED RELEASE DOSAGE FORMS OF ZIPRASIDONE 未知
公开(公告)号：CA2537413A1
公开(公告)日：2005-03-10
申请号：CA2537413
申请日：2004-08-31
申请人： SHAMBLIN SHERI L , FRIESEN DWAYNE THOMAS , HERBIG SCOTT MAX , WATERMAN KENNETH C , SHANKER RAVI MYSORE , BABCOCK WALTER CHRISTIAN , SMITHEY DANIEL TOD , SUTTON STEVEN C , THOMBRE AVINASH GOVIND , LYON DAVID KEITH , APPEL LEAH ELIZABETH , AHMED IMRAN
发明人： SHAMBLIN SHERI L , FRIESEN DWAYNE THOMAS , HERBIG SCOTT MAX , WATERMAN KENNETH C , SHANKER RAVI MYSORE , BABCOCK WALTER CHRISTIAN , SMITHEY DANIEL TOD , SUTTON STEVEN C , THOMBRE AVINASH GOVIND , LYON DAVID KEITH , APPEL LEAH ELIZABETH , AHMED IMRAN
IPC分类号： A61K9/20 , A61K9/00 , A61K9/16 , A61K9/22 , A61K9/28 , A61K9/52 , A61K31/496
摘要： A sustained release solid oral dosage from for treatment of a psychotic disorder, for example schizophrenia, in a mammal is provided, which oral dosage from comprises ziprasidone in an amount effective in treating said psychotic disorder and a pharmaceutically acceptable carrier.

8. 发明专利

AR046811A1 FORMAS DE DOSIFICACION ORAL DE ZIPRASIDONA DE LIBERACION SOSTENIDA 未知
公开(公告)号：AR046811A1
公开(公告)日：2005-12-28
申请号：ARP040103123
申请日：2004-08-31
申请人： AHMED IMRAN , HERBIG SCOTT MAX , FRIESEN DWAYNE THOMAS , BABCOCK WALTER CHRISTIAN , LYON DAVID KEITH , SUTTON STEVEN C , SHAMBLIN SHERI L , THOMBRE AVINASH GOVIND , SHANKER RAVI MYSORE , APPEL LEAH ELIZABETH , SMITHEY DANIEL TOD , WATERMAN KENNETH C
发明人： AHMED IMRAN , BABCOCK WALTER CHRISTIAN , HERBIG SCOTT MAX , SHAMBLIN SHERI L , SMITHEY DANIEL TOD , THOMBRE AVINASH GOVIND , FRIESEN DWAYNE THOMAS , LYON DAVID KEITH , SHANKER RAVI MYSORE , SUTTON STEVEN C , WATERMAN KENNETH C , APPEL LEAH ELIZABETH
IPC分类号： A61K9/00 , A61K9/16 , A61K9/20 , A61K9/52 , A61K31/496 , A61K9/22 , A61K9/28 , A61P25/18
摘要： Forma de dosificación oral sólida de ziprasidona de liberación sostenida para el tratamiento de un trastorno psicótico, por ejemplo, esquizofrenia, en un mamífero. Reivindicación 1: Un forma de dosificación oral de liberación sostenida que comprende una cantidad farmacéuticamente efectiva de ziprasidona y un medio de liberación sostenida para liberar por lo menos una parte de dicha ziprasidona, en donde después de la administración para alcanzar un estado estable, dicha forma de dosificación proporciona una concentración de ziprasidona en sangre mínima (Cmin) en estado estable de por lo menos 20 ng/ml y una concentración de ziprasidona en sangre máxima (Cmax) en estado estable de menos de 330 ng/ml.

9. 发明申请

WO2005020929A3 SUSTAINED RELEASE DOSAGE FORMS OF ZIPRASIDONE 审中-公开
标题翻译： ZIPRASIDONE的持续释放剂型
公开(公告)号：WO2005020929A3
公开(公告)日：2005-08-25
申请号：PCT/US2004028304
申请日：2004-08-31
申请人： AHMED IMRAN , APPEL LEAH ELIZABETH , BABCOCK WALTER CHRISTIAN , FRIESEN DWAYNE THOMAS , HERBIG SCOTT MAX , LYON DAVID KEITH , SHAMBLIN SHERI L , SHANKER RAVI MYSORE , SMITHEY DANIEL TOD , SUTTON STEVEN C , THOMBRE AVINASH GOVIND , WATERMAN KENNETH C
发明人： AHMED IMRAN , APPEL LEAH ELIZABETH , BABCOCK WALTER CHRISTIAN , FRIESEN DWAYNE THOMAS , HERBIG SCOTT MAX , LYON DAVID KEITH , SHAMBLIN SHERI L , SHANKER RAVI MYSORE , SMITHEY DANIEL TOD , SUTTON STEVEN C , THOMBRE AVINASH GOVIND , WATERMAN KENNETH C
IPC分类号： A61K9/00 , A61K9/16 , A61K9/20 , A61K9/52 , A61K31/496 , A61K9/22 , A61K9/28
CPC分类号： A61K9/1617 , A61K9/0004 , A61K9/1652 , A61K9/2018 , A61K9/2027 , A61K9/2031 , A61K9/2054 , A61K9/2077 , A61K9/2081 , A61K9/209 , A61K9/2846 , A61K9/5047 , A61K31/496 , A61K31/4965
摘要： A sustained release solid oral dosage from for treatment of a psychotic disorder, for example schizophrenia, in a mammal is provided, which oral dosage from comprises ziprasidone in an amount effective in treating said psychotic disorder and a pharmaceutically acceptable carrier.
摘要翻译：提供了用于治疗哺乳动物精神障碍例如精神分裂症的持续释放固体口服剂量，其口服剂量包含治疗所述精神障碍有效量的齐拉西酮和药学上可接受的载体。

10. 发明专利

JP2000229846A RELEASE CONTROL TYPE DOSAGE FORM 失效
公开(公告)号：JP2000229846A
公开(公告)日：2000-08-22
申请号：JP2000033132
申请日：2000-02-10
申请人： PFIZER PROD INC
发明人： REA ELIZABETH APPEL , CURATOLO WILLIAM JOHN , HERBIG SCOTT MAX , JAMES ALAN SHRIVER NIGHTINGALE , THOMBRE AVINASH GOVIND
IPC分类号： A61K9/22 , A61K9/00 , A61K9/14 , A61K9/16 , A61K9/26 , A61K9/50 , A61K9/52 , A61K31/135 , A61K31/137 , A61K31/17 , A61K31/36 , A61K31/404 , A61K31/44 , A61K31/497 , A61K31/505 , A61K31/517 , A61K31/522 , A61K47/32 , A61K47/34 , A61K47/38
摘要： PROBLEM TO BE SOLVED: To obtain a release control type dosage form having respectively specific core and coating to provide improved medicine bioavailability to deliver a medicine having poor solubility and short half-life of exclusion. SOLUTION: This dosage form comprises a core 12 composed of a penetrating agent and a poor soluble medicine, and a coating 18 around the core 12 having substantial water permeability. In the core 12, the medicine is in the form of a solid dispersed matter in a dispersed polymer, and at least most of the medicine is noncrystalline. The coating 18 contains at least one delivery boat 19 and controls the water inflow from an aqueous use environment to the core 12 to push out at least part of the core 12 to the above environment through the boat 19. During release of the above-mentioned medicine, the coating 18 has insolubility and non-erodibility.

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