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1. 发明申请

US20100331387A1 LYOPHILIZED PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译： LYOPHILIZED药物组合物
公开(公告)号：US20100331387A1
公开(公告)日：2010-12-30
申请号：US12676755
申请日：2008-09-18
申请人： Thitiwan Buranachokpaisan , Wenlei Jiang , Wei-Qin Tong , Joseph Lawrence Zielinski , Jiahao Zhu , Hans-Peter Zobel
发明人： Thitiwan Buranachokpaisan , Wenlei Jiang , Wei-Qin Tong , Joseph Lawrence Zielinski , Jiahao Zhu , Hans-Peter Zobel
IPC分类号： A61K31/4045
CPC分类号： A61K31/4045 , A61K9/0019 , A61K9/0095 , A61K9/19
摘要： Pharmaceutical compositions that include a poorly water-soluble therapeutic compound, an aqueous solvent, an chelator/antioxidant, a buffer or buffer component, and a bulking agent. The pharmaceutical compositions can be orally ingested or administered parenterally. The pharmaceutical compositions can further be lyophilized to form a pharmaceutically acceptable cake that can be administered orally, e.g., as a solid oral dosage form; or reconstituted and administered parenterally, e.g. as a single i.v. bolus or iv infusion, or administered orally, e.g. as a drink solution.
摘要翻译：包含难溶于水的治疗化合物，水性溶剂，螯合剂/抗氧化剂，缓冲剂或缓冲剂组分以及填充剂的药物组合物。药物组合物可以口服摄取或肠胃外给药。药物组合物可以进一步冻干以形成可以口服给药的药学上可接受的蛋糕，例如作为固体口服剂型; 或重组和肠胃外给药，例如作为一个i.v. 推注或静脉输注，或口服给药，例如作为饮料溶液。

2. 发明申请

US20100056500A1 Stable Parenteral Formulation 审中-公开
标题翻译：稳定的肠胃外制剂
公开(公告)号：US20100056500A1
公开(公告)日：2010-03-04
申请号：US12514514
申请日：2007-11-20
申请人： Thitiwan Buranachokaisan , Wenlei Jiang , Wei-Qin Tong
发明人： Thitiwan Buranachokaisan , Wenlei Jiang , Wei-Qin Tong
IPC分类号： A61K31/5513 , A61P31/12
CPC分类号： A61K9/0019 , A61K9/19 , A61K47/40
摘要： The present invention relates to pharmaceutical formulations of benzodiazepine compounds which are active against Respiratory Syncytial Virus (RSV) suitable for parenteral administration.
摘要翻译：本发明涉及对适合肠胃外给药的呼吸道合胞病毒（RSV）有活性的苯并二氮杂类化合物的药物制剂。

3. 发明申请

US20080286352A1 Liposome Compositions 审中-公开
标题翻译：脂质体组合物
公开(公告)号：US20080286352A1
公开(公告)日：2008-11-20
申请号：US12065134
申请日：2006-08-31
申请人： Saran Kumar , Wenlei Jiang , Jorg Ogorka , Jia-ai Zhang
发明人： Saran Kumar , Wenlei Jiang , Jorg Ogorka , Jia-ai Zhang
IPC分类号： A61K9/127 , A61K31/66 , A61P43/00
CPC分类号： A61K9/1272 , A61K31/41 , A61K31/663
摘要： A method of liposome-based therapy for a mammalian subject is disclosed. The method uses liposomes and/or liposomes with outer surfaces that contain an affinity moiety effective to bind specifically to a biological surface at which the therapy is aimed, and a hydrophilic polymer coating. The hydrophilic polymer coating is made up of polymer chains covalently linked to surface lipid components. After a desired liposome biodistribution is achieved, the affinity agent binds to the target surface and helps internalize the liposomes.
摘要翻译：公开了一种哺乳动物受试者基于脂质体的治疗方法。该方法使用具有外表面的脂质体和/或脂质体，所述外表面含有有效结合治疗所针对的生物表面的亲和部分和亲水性聚合物涂层。亲水聚合物涂层由与表面脂质组分共价连接的聚合物链组成。在实现所需的脂质体生物分布后，亲和剂结合靶表面并有助于脂质体内化。

4. 发明申请

US20080182909A1 METHODS FOR STABILIZING BIOLOGICALLY ACTIVE AGENTS ENCAPSULATED IN BIODEGRADABLE CONTROLLED-RELEASE POLYMERS 审中-公开
标题翻译：用于稳定可生物降解控制释放聚合物中生物活性剂的方法
公开(公告)号：US20080182909A1
公开(公告)日：2008-07-31
申请号：US11863088
申请日：2007-09-27
申请人： Steven P. Schwendeman , Gaozhong Zhu , Hanne Bentz , Jeffrey A. Hubbell , Wenlei Jiang , Anna Shenderova , Jichao Kang
发明人： Steven P. Schwendeman , Gaozhong Zhu , Hanne Bentz , Jeffrey A. Hubbell , Wenlei Jiang , Anna Shenderova , Jichao Kang
IPC分类号： A61K47/30
CPC分类号： A61K9/1647 , A61K9/0019 , A61K47/02
摘要： Methods for reducing or inhibiting the irreversible inactivation of water-soluble biologically active agents in biodegradable polymeric delivery systems which are designed to release such agents over a prolonged period of time, such as PLGA delivery systems are provided. The method comprises preparing PLGA delivery systems whose microclimate, i.e. the pores where the active agent resides, uniformly or homogenously maintain a pH of between 3 and 9, preferably between 4 and 8, more preferably between 5 and 7.5 during biodegradation. Depending on the size of the delivery system, and the initial bulk permeability of the polymer, this result is achieved by (a) incorporating a water-soluble carrier into the delivery system, (b) incorporating a select basic additive (or antacid) into the delivery system, (c) incorporating both a water soluble carrier and a select basic additive into the delivery system, (d) adding a pore forming molecule for increasing the rate of release of low molecular weight monomers and oligomers into the delivery system, (e) using a PLGA polymer with reduced glycolide content, i.e. PLGA with from 100% to 75% lactide and 0 to 25% glycolide) (f) using a microencapsulation method that yields a more extensive pore-network, e.g. oil-in-oil emulsion-solvent extraction as opposed to water-in-oil-in water-solvent evaporation method, and (g) combinations thereof.
摘要翻译：提供了用于减少或抑制在可生物降解的聚合物递送系统中的水溶性生物活性剂的不可逆失活的方法，其被设计为在长时间内释放这些试剂，例如PLGA递送系统。该方法包括制备PLGA递送系统，其微生物即活性剂所在的孔在生物降解过程中均匀或均匀地保持3至9之间，优选4至8，更优选5至7.5之间的pH。根据输送系统的尺寸和聚合物的初始体积渗透性，该结果通过（a）将水溶性载体引入输送系统来实现，（b）将选择的碱性添加剂（或抗酸剂）掺入递送系统，（c）将水溶性载体和选择性碱性添加剂并入输送系统中，（d）添加成孔分子，以将低分子量单体和低聚物的释放速率提高到递送系统中（ e）使用具有降低的乙交酯含量的PLGA聚合物，即具有100％至75％丙交酯和0至25％乙交酯的PLGA）（f）使用产生更广泛孔隙网络的微胶囊化方法，例如油包水乳液 - 溶剂萃取相对于水包油型水溶剂蒸发法，和（g）它们的组合。

5. 发明授权

US06743446B2 Methods for stabilizing biologically active agents encapsulated in biodegradable controlled-release polymers 失效
标题翻译：用于稳定包封在可生物降解的控释聚合物中的生物活性剂的方法
公开(公告)号：US06743446B2
公开(公告)日：2004-06-01
申请号：US09738961
申请日：2000-12-15
申请人： Steven P. Schwendeman , Gaozhong Zhu , Hanne Bentz , Jeffrey A. Hubbell , Wenlei Jiang , Anna Shenderova , Jichao Kang
发明人： Steven P. Schwendeman , Gaozhong Zhu , Hanne Bentz , Jeffrey A. Hubbell , Wenlei Jiang , Anna Shenderova , Jichao Kang
IPC分类号： A61K914
CPC分类号： A61K9/1647 , A61K9/0019 , A61K47/02
摘要： Methods for reducing or inhibiting the irreversible inactivation of water-soluble biologically active agents in biodegradable polymeric delivery systems which are designed to release such agents over a prolonged period of time, such as PLGA delivery systems are provided. The method comprises preparing a PLGA delivery systems whose microclimate, i.e. the pores where the active agent resides, uniformly or homogenously maintain a pH of between 3 and 9, preferably between 4 and 8, more preferably between 5 and 7.5 during biodegradation. Depending on the size of the delivery system, and the initial bulk permeability of the polymer, this result is achieved by (a) incorporating a water-soluble carrier into the delivery system, (b) incorporating a select basic additive (or antacid) into the delivery system, (c) incorporating both a water soluble carrier and a select basic additive into the delivery system, (d) adding a pore forming molecule for increasing the rate of release of low molecular weight monomers and oligomers into the delivery system, (e) using a PLGA polymer with reduced glycolide content, i.e. PLGA with from 100% to 75% lactide and 0 to 25% glycolide) (f) using a microencapsulation method that yields a more extensive pore-network, e.g. oil-in-oil emulsion-solvent extraction as opposed to water-in-oil-in water-solvent evaporation method, and (g) combinations thereof.
摘要翻译：提供了用于减少或抑制在可生物降解的聚合物递送系统中的水溶性生物活性剂的不可逆失活的方法，其被设计为在长时间内释放这些试剂，例如PLGA递送系统。该方法包括制备PLGA递送系统，其微生物即活性剂所在的孔在生物降解过程中均匀或均匀地保持在3至9之间，优选4至8之间，更优选5至7.5的pH。根据输送系统的尺寸和聚合物的初始体积渗透性，该结果通过（a）将水溶性载体引入输送系统来实现，（b）将选择的碱性添加剂（或抗酸剂）掺入递送系统，（c）将水溶性载体和选择性碱性添加剂并入输送系统中，（d）添加成孔分子，以将低分子量单体和低聚物的释放速率提高到递送系统中（ e）使用具有降低的乙交酯含量的PLGA聚合物，即具有100％至75％丙交酯和0至25％乙交酯的PLGA）（f）使用产生更广泛孔隙网络的微胶囊化方法，例如油包水乳液 - 溶剂萃取相对于水包油型水溶剂蒸发法，和（g）它们的组合。

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