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1. 发明申请

WO2005051358A1 COMPOSITION AND METHOD FOR ENHANCING BIOAVAILABILITY 审中-公开
标题翻译：提高生物利用度的组合物和方法
公开(公告)号：WO2005051358A1
公开(公告)日：2005-06-09
申请号：PCT/US2004/037927
申请日：2004-11-12
申请人： ALZA CORPORATION , DONG, Liang, C. , POLLOCK-DOVE, Crystal , HAN, Jasmine
发明人： DONG, Liang, C. , POLLOCK-DOVE, Crystal , HAN, Jasmine
IPC分类号： A61K9/16
CPC分类号： A61K9/1611 , A61K9/2009 , A61K9/2027 , A61K9/2054
摘要： The present invention relates to compositions and methods for enhancing the bioavailability of beneficial agents with low water solubility.
摘要翻译：本发明涉及用于增强具有低水溶性的有益药剂的生物利用度的组合物和方法。

2. 发明申请

WO2009137827A2 CONTROLLED RELEASE OF N-ACETYLCYSTEINE (NAC) FOR REDUCTION OF SYSTEMIC AND/OR VASCULAR INFLAMMATION 审中-公开
标题翻译：控制释放N-乙酰胆碱（NAC）以减少系统性和/或血管炎
公开(公告)号：WO2009137827A2
公开(公告)日：2009-11-12
申请号：PCT/US2009/043435
申请日：2009-05-11
申请人： TIARA PHARMACEUTICALS, INC. , ARAD, Yadon , DONG, Liang, C.
发明人： ARAD, Yadon , DONG, Liang, C.
IPC分类号： A61K31/198
CPC分类号： A61K9/4808 , A61K9/2077 , A61K9/2081 , A61K9/209 , A61K9/5078 , A61K31/198 , A61K31/366 , A61K45/06 , A61K2300/00
摘要： The present invention provides a controlled-release composition which provides a therapeutically effective plasma concentration of N-acetylcysteine over prolonged period of time. The present invention also includes the use of the controlled-release composition, either alone or in combination with at least one additional active agent, for reduction of vascular inflammation marker and treatment of diseases, conditions, and/or symptoms associated with systemic and/or vascular inflammation in a patient. Furthermore, the present invention provides a process of making granules comprising N-acetylcysteine, or a salt, solvate, prodrug, and/or analog thereof.
摘要翻译：本发明提供了一种控制释放组合物，其在延长的时间段内提供治疗有效的N-乙酰半胱氨酸的血浆浓度。本发明还包括单独或与至少一种另外的活性剂组合的控释组合物用于减少血管炎症标志物以及治疗与全身和/或其他疾病相关的疾病，病症和/或症状的用途。患者血管炎症。此外，本发明提供了制备包含N-乙酰半胱氨酸或其盐，溶剂合物，前药和/或类似物的颗粒的方法。

3. 发明申请

WO1995003823A1 THERAPEUTIC COMPOSITIONS COMPRISING A POLYPEPTIDE 审中-公开
标题翻译：包含多肽的治疗组合物
公开(公告)号：WO1995003823A1
公开(公告)日：1995-02-09
申请号：PCT/US1994008560
申请日：1994-07-29
申请人： ALZA CORPORATION
发明人： ALZA CORPORATION , YANG, Heechung , NGUYEN, Vu, Anh , DONG, Liang, C. , WONG, Patrick, S.-L.
IPC分类号： A61K38/27
CPC分类号： A61K38/27 , A61K9/1617 , A61K38/28 , A61K47/12 , A61K47/44
摘要： The present invention is directed to a pharmaceutical formulation of a therapeutic polypeptide together with a permeation-enhancing mixture of sodium salicylate and an oil to provide enhanced absorption of the polypeptide through the wall of the gastrointestinal tract, and particularly of the colon, after oral administration, the amount of oil being from about 10 wt % to about 30 wt %, preferably from about 15 wt % to about 25 wt %, of the total formulation and the amount of sodium salicylate being from about 70 wt % to about 90 wt %, preferably from about 75 wt % to about 85 wt %, of the total formulation. The polypeptide may be non-lyophilized. The pharmaceutical formulation is characterized as a solid, which provides a convenient and improved format for handling and storage and for the preparation of oral dosage forms (such as pills, capsules and delivery vessels) containing a homogeneous mixture of ingredients.
摘要翻译：本发明涉及治疗性多肽的药物制剂以及水杨酸钠和油的渗透增强混合物，以在口服给药之后通过胃肠道的壁，特别是结肠壁增强吸收多肽，油的量为总制剂的约10重量％至约30重量％，优选约15重量％至约25重量％，水杨酸钠的量为约70重量％至约90重量％，优选约75重量％至约85重量％。多肽可以是非冻干的。药物制剂的特征在于固体，其提供用于处理和储存的方便和改进的形式，以及用于制备含有均匀成分混合物的口服剂型（例如丸剂，胶囊和递送容器）。

4. 发明申请

WO2004041246A1 PHARMACEUTICAL FORMULATION PROVIDING AN INCREASED BIOVAILABILITY OF HYDROPHOBIC DRUGS 审中-公开
标题翻译：提供增加潜在药物生物利用度的药物制剂
公开(公告)号：WO2004041246A1
公开(公告)日：2004-05-21
申请号：PCT/US2003/034703
申请日：2003-10-31
申请人： ALZA CORPORATION
发明人： DONG, Liang, C. , ZHAO,Ruiping , WONG, Patrick, S., L.
IPC分类号： A61K9/00
CPC分类号： A61K31/57 , A61K9/0004 , A61K9/1075 , A61K9/146
摘要： The present invention provides a drug formulation comprising a hydrophobic drug, an oil phase and a surfactant and a dosage form. The drug formulation works to increase the bioavailability of hydrophobic drugs delivered to the gastro-intestinal tract ("GI tract") of a desired subject. The drug formulation of the present invention is formulated as a self-emuslifying nanosuspension, which forms an emulsion in-situ upon introduction to an aqueous environment. The dosage form of the present invention may be formed using various different materials and may be configured to deliver the drug formulation of the present invention to the GI tract of a subject using any desired mechanism. A controlled release dosage form according to the present invention may be designed to deliver the drug formulation of the present invention at a desired rate over a desired period of time. If designed as a controlled release dosage form, the dosage form of the present invention may be an osmotic dosage form.
摘要翻译：本发明提供了包含疏水性药物，油相和表面活性剂以及剂型的药物制剂。药物制剂用于增加递送至所需受试者的胃肠道（“胃肠道”）的疏水性药物的生物利用度。将本发明的药物制剂配制成自发性纳米悬浮液，其在引入水性环境中时就地形成乳状液。本发明的剂型可以使用各种不同的材料形成，并且可以被配置为使用任何期望的机制将本发明的药物制剂递送到受试者的胃肠道。可以设计根据本发明的控释剂型，以期望的速率在期望的时间段内递送本发明的药物制剂。如果设计为控释剂型，本发明的剂型可以是渗透剂型。

5. 发明申请

WO2003053401A3 FORMULATION AND DOSAGE FORM FOR INCREASING ORAL BIOAVAILABILITY OF HYDROPHILIC MACROMOLECULES 审中-公开
公开(公告)号：WO2003053401A3
公开(公告)日：2003-07-03
申请号：PCT/US2002/041031
申请日：2002-12-18
申请人： ALZA CORPORATION
发明人： DONG, Liang, C. , WONG, Patrick, S., L. , NGUYEN, Vu, A. , YUM, Si-Hong , CHAO, Anthony, C. , DADDONA, Peter, E.
IPC分类号： A61K9/00
摘要： The present invention includes a formulation and dosage form for enhancing the bioavailability of orally administered hydrophilic macromolecules. The formulation of the present invention includes a permeation enhancer, a hydrophilic macromolecule, and a carrier that exhibits in-situ gelling properties, such as nonionic surfactant. The formulation of the present invention is delivered within the GI tract as a liquid having at least some affinity for the surface of the GI mucosal membrane. Once released, it is believed that the liquid formulation spreads across one or more areas of the surface of the GI mucosal membrane, where the carrier of the formulation then transitions into a biodhesive gel in-situ. As a bioadhesive gel, the formulation of the present invention present the hydrophilic macromolecule and the permeation enhancer at the surface of the GI mucosal membrane at concentrations sufficient to increase absorption of the hydrophilic macromolecule through the GI mucosal membrane over a period of time. The dosage form of the present invention incorporates the formulation of the present invention and may be designed to provide the controlled release of the formulation within the GI tract over a desired period of time.

6. 发明申请

WO2003053401A2 FORMULATION AND DOSAGE FORM FOR INCREASING ORAL BIOAVAILABILITY OF HYDROPHILIC MACROMOLECULES 审中-公开
标题翻译：制剂和剂型用于增加水解大分子的口服生物利用度
公开(公告)号：WO2003053401A2
公开(公告)日：2003-07-03
申请号：PCT/US2002/041031
申请日：2002-12-18
申请人： ALZA CORPORATION
发明人： DONG, Liang, C. , WONG, Patrick, S., L. , NGUYEN, Vu, A. , YUM, Si-Hong , CHAO, Anthony, C. , DADDONA, Peter, E.
IPC分类号： A61K9/00
CPC分类号： A61K9/1274 , A61K9/0004 , A61K9/4858 , A61K9/4891 , A61K31/727
摘要： The present invention includes a formulation and dosage form for enhancing the bioavailability of orally administered hydrophilic macromolecules. The formulation of the present invention includes a permeation enhancer, a hydrophilic macromolecule, and a carrier that exhibits in-situ gelling properties, such as nonionic surfactant. The formulation of the present invention is delivered within the GI tract as a liquid having at least some affinity for the surface of the GI mucosal membrane. Once released, it is believed that the liquid formulation spreads across one or more areas of the surface of the GI mucosal membrane, where the carrier of the formulation then transitions into a biodhesive gel in-situ. As a bioadhesive gel, the formulation of the present invention present the hydrophilic macromolecule and the permeation enhancer at the surface of the GI mucosal membrane at concentrations sufficient to increase absorption of the hydrophilic macromolecule through the GI mucosal membrane over a period of time. The dosage form of the present invention incorporates the formulation of the present invention and may be designed to provide the controlled release of the formulation within the GI tract over a desired period of time.
摘要翻译：本发明包括用于增加口服给药的亲水性大分子的生物利用度的制剂和剂型。本发明的制剂包括渗透促进剂，亲水性大分子和表现出原位胶凝性的载体，如非离子表面活性剂。本发明的制剂在胃肠道内作为对GI粘膜表面具有至少一些亲和性的液体递送。一旦释放，据信液体制剂在GI粘膜表面的一个或多个区域上扩散，其中制剂的载体然后原位转变成生物胶凝胶。作为生物粘附凝胶，本发明的制剂在足以在一段时间内通过GI粘膜增加亲水性大分子的吸收的浓度，在GI粘膜的表面存在亲水性高分子和渗透促进剂。本发明的剂型包含本发明的制剂，并且可以设计成在期望的时间段内提供制剂在胃肠道内的受控释放。

7. 发明申请

WO1995006460A1 DISPENSER CONTAINING HYDROPHOBIC AGENT 审中-公开
标题翻译：含有疏水剂的分配器
公开(公告)号：WO1995006460A1
公开(公告)日：1995-03-09
申请号：PCT/US1994009709
申请日：1994-08-31
申请人： ALZA CORPORATION
发明人： ALZA CORPORATION , DONG, Liang, C. , ESPINAL, Steven, D. , WONG, Patrick, S.-L. , GUITTARD, George, V. , HAMEL, Lawrence, G.
IPC分类号： A61K09/00
CPC分类号： A61K9/0004 , A61K9/2013 , A61K9/2054
摘要： The present invention is directed to a formulation for the delivery of hydrophobic active agents to a fluid environment of use while avoiding aggregation of the hydrophobic agents in the environment, the formulation comprising a hydrophobic active agent in an amount of 50 wt% (percent by weight) or greater together with polyoxyethylene 40 stearate and a disintegrant. The present invention is also directed to an improvement in a fluid-activated delivery device (10) wherein the delivery device includes a housing (12) defining an internal compartment (14), an active agent formulation (15) in the compartment, exit means (13) in the housing (12) for delivering the active agent formulation (15) from the delivery device, a fluid-activated expandable driving member (16) in the compartment, optionally a partition layer between the active agent formulation (15) and the driving member (16), and optionally a lubricant subcoat (18); wherein the improvement comprises an active agent formulation (15) comprising a hydrophobic active agent in an amount of 50 wt% (percent by weight) or greater together with polyoxyethylene 40 stearate and a disintegrant.
摘要翻译：本发明涉及用于将疏水性活性剂递送至使用的流体环境的制剂，同时避免疏水剂在环境中的聚集，所述制剂包含50重量％（重量百分比）的疏水性活性剂）或更大，与聚氧乙烯40硬脂酸酯和崩解剂一起。本发明还涉及流体激活的输送装置（10）的改进，其中输送装置包括限定内部隔室（14）的壳体（12），隔室中的活性剂制剂（15），出口装置（13），用于从所述输送装置输送活性剂制剂（15），所述隔室中的流体活化的可膨胀驱动构件（16），任选地在所述活性剂制剂（15）和驱动构件（16）和任选的润滑剂底涂层（18）; 其中所述改进包括活性剂制剂（15），其包含50重量％（重量百分比）以上的疏水性活性剂以及聚氧乙烯40硬脂酸酯和崩解剂。

8. 发明申请

WO2003053400A1 FORMULATION & DOSAGE FORM FOR THE CONTROLLED DELIVERY OF THERAPEUTIC AGENTS 审中-公开
标题翻译：用于治疗药物控制的配方和剂型
公开(公告)号：WO2003053400A1
公开(公告)日：2003-07-03
申请号：PCT/US2002/040763
申请日：2002-12-19
申请人： ALZA CORPORATION
发明人： DONG, Liang, C. , WONG, Patrick, S., L. , ESPINAL, Steve, D. , NGUYEN, Vu, A.
IPC分类号： A61K9/00
CPC分类号： A61K9/0014 , A61K9/0004 , A61K9/1274 , A61K47/12 , A61K47/44
摘要： The present invention includes a formulation and controlled release dosage form that enable the controlled release of therapeutic agents showing reduced absorption in the lower gastrointestinal tract. The formulation of the present invention includes a therapeutic agent that exhibits greater absorption in the upper GI tract than in the lower GI tract and a permeation enhancer, which serves to increase absorption of the therapeutic agent in the lower GI tract. The formulation of the present invention further includes a carrier that allows the formulation to transition to a bioadhesive gel in situ after the formulation is dispensed within the GI tract and has had some opportunity to reach the surface of the GI mucosal membrane. The bioadhesive gel formed by the formulation of the present invention works to present effective concentrations of both the therapeutic agent and the permeation enhancer at the surface of the GI mucosal membrane over a period. The controlled release dosage form of the present invention is designed to deliver the formulation of the present invention at a desired release rate or release rate profile over a desired period of time.
摘要翻译：本发明包括使得能够控制释放在下胃肠道中显示减少的吸收的治疗剂的制剂和控释剂型。本发明的制剂包括在上GI道中比在下GI道中显示更大吸收的治疗剂和渗透促进剂，其用于增加治疗剂在下GI道中的吸收。本发明的制剂还包括载体，其允许制剂在制剂分配在胃肠道内之后就地转移到生物粘附凝胶上并具有到达GI粘膜的表面的一些机会。通过本发明的制剂形成的生物粘附凝胶用于在一段时间内提供GI粘膜表面上的治疗剂和渗透促进剂的有效浓度。本发明的控制释放剂型被设计成在所需的时间段内以期望的释放速率或释放速率曲线递送本发明的制剂。

9. 发明申请

WO1996025922A3 BANDED PROLONGED RELEASE ACTIVE AGENT DOSAGE FORM 审中-公开
公开(公告)号：WO1996025922A3
公开(公告)日：1996-08-29
申请号：PCT/US1996001848
申请日：1996-02-09
申请人： ALZA CORPORATION
发明人： ALZA CORPORATION , WONG, Patrick, S.-L. , EDGREN, David, Edmil , DONG, Liang, C. , FERRARI, Vincent, J.
IPC分类号： A61K09/20

10. 发明申请

WO1996013248A1 INJECTION-MOLDED DOSAGE FORM 审中-公开
标题翻译：注射剂型剂型
公开(公告)号：WO1996013248A1
公开(公告)日：1996-05-09
申请号：PCT/US1995013619
申请日：1995-10-20
申请人： ALZA CORPORATION
发明人： ALZA CORPORATION , DONG, Liang, C. , WONG, Patrick, S.-L. , POLLOCK, Crystal , FERRARI, Vincent, Joseph
IPC分类号： A61K09/00
CPC分类号： C08L67/04 , A61K9/0004 , A61K9/2095 , A61K47/34 , A61K47/38 , B01D71/48 , C08L1/284 , C08L71/02 , C08L2666/26 , C08L2666/02 , C08L71/00 , C08L2666/18
摘要： A dosage form is disclosed comprising an injection-molded housing member free of organic solvents.
摘要翻译：公开了一种剂型，其包括不含有机溶剂的注塑外壳构件。

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