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    Bioadhesive drug delivery system with enhanced gastric retention
    14.
    发明申请
    Bioadhesive drug delivery system with enhanced gastric retention 审中-公开
    生物粘附药物递送系统具有增强的胃滞留

    公开(公告)号：US20050064027A1

    公开(公告)日：2005-03-24

    申请号：US10498661

    申请日：2002-12-13

    Applicant: Jules Jacob ,  Edith Mathiowitz ,  David Enscore ,  Marcus Schestopol

    Inventor： Jules Jacob ,  Edith Mathiowitz ,  David Enscore ,  Marcus Schestopol

    IPC: A61K9/30 ,  A61K9/00 ,  A61K9/16 ,  A61K9/20 ,  A61K9/48 ,  A61K9/50 ,  A61K9/52 ,  A61K31/522 ,  A61K45/00 ,  A61K47/04 ,  A61K47/36 ,  A61K47/42 ,  A61P31/12 ,  A61P31/20 ,  A61P33/00 ,  A61P35/00

    CPC classification number: A61K9/0065 ,  A61K9/501 ,  A61K9/5026 ,  A61K9/5031 ,  A61K9/5073

    Abstract: Bioadhesive macrosphere delivery systems (“BDDS”) having prolonged gastric retention time due to bioadhesion rather than physical density or size are described. In general, the macrospheres have diameters that are greater than 200 microns, more preferably greater than 500 microns. The bioadhesive macrospheres are released in the stomach where they reside in close proximity to the gastric mucosa for a prolonged period of time. Increased residence of BDDS in the upper GI can lead to increased systemic absorption of drug in the preferred site of systemic absorption, namely the upper GI tract (upper to mid-jejunum). The BDDS may be engineered either as a capsule with drug delivery controlled by a diffusion-limited membrane or degradable shell, or as a solid matrix system with drug delivery controlled by a combination of diffusion and polymer degradation kinetics.

    Abstract translation: 描述了由于生物粘附而不是物理密度或大小而具有延长的胃停留时间的生物粘附大球传递系统（“BDDS”）。 通常，大球的直径大于200微米，更优选大于500微米。 生物粘附的大球在胃中被释放，其中它们靠近胃粘膜存在一段较长的时间。 增加BDDS在上GI中的居住可导致药物在全身吸收的优选部位，即上胃肠道上（上至中空）中的全身吸收增加。 BDDS可以被设计为具有由扩散限制膜或可降解壳控制的药物递送的胶囊，或者作为具有由扩散和聚合物降解动力学的组合控制的药物递送的固体基质体系。

    Polymeric gene delivery system
    16.
    发明授权
    Polymeric gene delivery system 失效
    聚合物基因传递系统

    公开(公告)号：US06620617B2

    公开(公告)日：2003-09-16

    申请号：US09815807

    申请日：2001-03-23

    Applicant: Edith Mathiowitz ,  Yong Shik Jong ,  Kim Boekelheide

    Inventor： Edith Mathiowitz ,  Yong Shik Jong ,  Kim Boekelheide

    IPC: C12N1500

    CPC classification number: A61K9/1647 ,  A61K9/1272 ,  A61K9/2027 ,  A61K48/00

    Abstract: A means for obtaining efficient introduction of exogenous genes into a patient, with long term expression of the gene, is disclosed. The gene, under control of an appropriate promoter for expression in a particular cell type, is encapsulated or dispersed with a biocompatible, preferably biodegradable polymeric matrix, where the gene is able to diffuse out of the matrix over an extended period of time, for example, a period of three to twelve months or longer. The matrix is preferably in the form of a microparticle such as a microsphere (where the gene is dispersed throughout a solid polymeric matrix) or microcapsule (gene is stored in the core of a polymeric shell), a film, an implant, or a coating on a device such as a stent. The size and composition of the polymeric device is selected to result in favorable release kinetics in tissue. The size is also selected according to the method of delivery which is to be used, typically injection or administration of a suspension by aerosol into the nasal and/or pulmonary areas. The matrix composition can be selected to not only have favorable degradation rates, but to be formed of a material which is bioadhesive, to further increase the effectiveness of transfer when administered to a mucosal surface.

    Abstract translation: 公开了一种用于获得有效引入外源基因到患者中的方法，其具有该基因的长期表达。 在特定细胞类型中用于表达的适当启动子的控制下的基因用生物相容的，优选可生物降解的聚合物基质包封或分散，其中基因能够在延长的时间段内扩散出基质，例如 ，期限为三至十二个月或更长。 基质优选为微粒，例如微球（其中基因分散在整个固体聚合物基质中）或微胶囊（基因存储在聚合物壳的核心中），膜，植入物或涂层 在诸如支架的装置上。 选择聚合物装置的尺寸和组成以在组织中产生有利的释放动力学。 还根据要使用的递送方法选择大小，通常通过气雾剂将悬浮液注射或施用于鼻和/或肺部区域。 可以选择基质组合物不仅具有良好的降解速率，而且由生物粘附的材料形成，以进一步提高施用于粘膜表面时转移的有效性。

    Multiwall polymeric microcapsules from hydrophilic polymers
    17.
    发明授权
    Multiwall polymeric microcapsules from hydrophilic polymers 失效
    来自亲水聚合物的多壁聚合物微胶囊

    公开(公告)号：US06528035B1

    公开(公告)日：2003-03-04

    申请号：US09707440

    申请日：2000-11-06

    Applicant: Edith Mathiowitz ,  Jules S. Jacob ,  Donald E. Chickering, III ,  Kathleen Jo Leach

    Inventor： Edith Mathiowitz ,  Jules S. Jacob ,  Donald E. Chickering, III ,  Kathleen Jo Leach

    IPC: B32B516

    CPC classification number: B01J13/04 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/1694 ,  A61K9/5036 ,  A61K9/5052 ,  A61K9/5089 ,  B29K2003/00 ,  Y10S514/963 ,  Y10S514/965 ,  Y10T428/2984 ,  Y10T428/2985 ,  Y10T428/2989 ,  Y10T428/2991

    Abstract: Two or more hydrophilic polymers that are not soluble in each other at a particular concentration and temperature, but which have a positive spreading coefficient in solution, are used to form multi-layered polymeric microspheres. The multi-layer microspheres produced by the method are distinguished by extremely uniform dimensioned polymer layers and actual incorporation of a substance to be delivered into the polymer layers. In the preferred embodiment of the method, two polymers are dissolved in an aqueous solvent, the substance to be incorporated is dispersed or dissolved in the polymer solution, the mixture is suspended in an organic solvent or polymer/water mixture and stirred, and the solvent is slowly evaporated, creating microspheres with an inner core formed by one polymer and an outer layer formed by the second polymer.

    Abstract translation: 在特定浓度和温度下彼此不溶的但在溶液中具有正扩散系数的两种或更多种亲水性聚合物用于形成多层聚合物微球体。 通过该方法制备的多层微球的特征在于非常均匀的尺寸聚合物层和实际掺入待输送到聚合物层中的物质。 在该方法的优选实施方案中，将两种聚合物溶解在水性溶剂中，将待加入的物质分散或溶解在聚合物溶液中，将混合物悬浮在有机溶剂或聚合物/水混合物中并搅拌，并将溶剂 缓慢蒸发，产生具有由一种聚合物形成的内芯和由第二聚合物形成的外层的微球。

    Preparation of multiwall polymeric microcapsules from hydrophilic polymers
    18.
    发明授权
    Preparation of multiwall polymeric microcapsules from hydrophilic polymers 失效
    从亲水聚合物制备多壁聚合物微胶囊

    公开(公告)号：US06511749B1

    公开(公告)日：2003-01-28

    申请号：US08990365

    申请日：1997-12-15

    Applicant: Edith Mathiowitz ,  Jules S. Jacob ,  Donald E. Chickering, III ,  Kathleen Jo Pekarek

    Inventor： Edith Mathiowitz ,  Jules S. Jacob ,  Donald E. Chickering, III ,  Kathleen Jo Pekarek

    IPC: B32B1502

    CPC classification number: B01J13/04 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/1694 ,  A61K9/5036 ,  A61K9/5052 ,  A61K9/5089 ,  B29K2003/00 ,  Y10S514/963 ,  Y10S514/965 ,  Y10T428/2984 ,  Y10T428/2985 ,  Y10T428/2989 ,  Y10T428/2991

    Abstract: Two or more hydrophilic polymers that are not soluble in each other at a particular concentration and temperature, but which have a positive spreading coefficient in solution, are used to form multi-layered polymeric microspheres. The multi-layer microspheres produced by the method are distinguished by extremely uniform dimensioned polymer layers and actual incorporation of a substance to be delivered into the polymer layers. In the preferred embodiment of the method, two polymers are dissolved in an aqueous solvent, the substance to be incorporated is dispersed or dissolved in the polymer solution, the mixture is suspended in an organic solvent or polymer/water mixture and stirred, and the solvent is slowly evaporated, creating microspheres with an inner core formed by one polymer and an outer layer formed by the second polymer.

    Abstract translation: 在特定浓度和温度下彼此不溶的但在溶液中具有正扩散系数的两种或更多种亲水性聚合物用于形成多层聚合物微球体。 通过该方法制备的多层微球的特征在于非常均匀的尺寸聚合物层和实际掺入待输送到聚合物层中的物质。 在该方法的优选实施方案中，将两种聚合物溶解在水性溶剂中，将待加入的物质分散或溶解在聚合物溶液中，将混合物悬浮在有机溶剂或聚合物/水混合物中并搅拌，并将溶剂 缓慢蒸发，产生具有由一种聚合物形成的内芯和由第二聚合物形成的外层的微球。

    Methods and compositions for enhancing the bioadhesive properties of polymers using organic excipients
    19.
    发明授权
    Methods and compositions for enhancing the bioadhesive properties of polymers using organic excipients 失效
    使用有机赋形剂增强聚合物生物粘合性能的方法和组合物

    公开(公告)号：US06156348A

    公开(公告)日：2000-12-05

    申请号：US135248

    申请日：1998-08-17

    Applicant: Camila A. Santos ,  Jules S. Jacob ,  Benjamin A. Hertzog ,  Gerardo P. Carino ,  Edith Mathiowitz

    Inventor： Camila A. Santos ,  Jules S. Jacob ,  Benjamin A. Hertzog ,  Gerardo P. Carino ,  Edith Mathiowitz

    IPC: B82B1/00 ,  A61K9/16 ,  A61K9/51 ,  A61K9/50 ,  A61F2/02 ,  A61K47/30

    CPC classification number: A61K9/5138 ,  A61K9/1641 ,  A61K9/1647 ,  A61K9/5153

    Abstract: Methods and compositions are provided for enhancing the bioadhesive properties of polymers used in drug delivery systems. The bioadhesive properties of a polymer are enhanced by incorporating an anhydride oligomer into the polymer to enhance the ability of the polymer to adhere to a tissue surface such as a mucosal membrane. Anhydride oligomers which enhance the bioadhesive properties of a polymer include oligomers synthesized from dicarboxylic acid monomers, preferably those found in Krebs glycolysis cycle, especially fumaric acid. The oligomers can be incorporated within a wide range of polymers including proteins, polysaccharides and synthetic biocompatible polymers. In one embodiment, anhydride oligomers can be incorporated within polymers used to form or coat drug delivery systems, such as microspheres, which contain a drug or diagnostic agent. The oligomers can either be solubilized and blended with the polymer before manufacture or else used as a coating with polymers over existing systems. The polymers, for example in the form of microspheres, have improved ability to adhere to mucosal membranes, and thus can be used to deliver a drug or diagnostic agent via any of a range of mucosal membrane surfaces including those of the gastrointestinal, respiratory, excretory and reproductive tracts.

    Abstract translation: 提供了用于增强药物递送系统中使用的聚合物的生物粘合性质的方法和组合物。 聚合物的生物粘合性能通过将酸酐低聚物引入聚合物来增强聚合物粘附到组织表面如粘膜的能力。 增强聚合物生物粘合性能的酸酐低聚物包括由二羧酸单体合成的低聚物，优选在克雷伯糖酵解循环中发现的那些，特别是富马酸。 低聚物可以掺入宽范围的聚合物中，包括蛋白质，多糖和合成的生物相容性聚合物。 在一个实施方案中，酸酐低聚物可以掺入用于形成或涂覆药物递送系统的聚合物，例如含有药物或诊断剂的微球体。 寡聚物可以在制造之前溶解并与聚合物共混，或者在现有体系中用作具有聚合物的涂层。 聚合物，例如以微球形式，具有改善粘附于粘膜的能力，因此可用于通过任何一种粘膜膜表面（包括胃肠道，呼吸道，排泄物）的粘膜递送药物或诊断剂 和生殖道。

    Pure polyanhydride from dicarboxylic acid and coupling agent
    20.
    发明授权
    Pure polyanhydride from dicarboxylic acid and coupling agent 失效
    来自二羧酸和偶联剂的纯聚酐

    公开(公告)号：US4916204A

    公开(公告)日：1990-04-10

    申请号：US80332

    申请日：1987-07-31

    Applicant: Abraham J. Domb ,  Robert S. Langer ,  Eyal Ron ,  Steven Giannos ,  Rohit Kothari ,  Edith Mathiowitz

    Inventor： Abraham J. Domb ,  Robert S. Langer ,  Eyal Ron ,  Steven Giannos ,  Rohit Kothari ,  Edith Mathiowitz

    IPC: A61K31/335 ,  A61K31/365 ,  A61K31/39 ,  C08G67/04 ,  C08G69/08 ,  C08G69/10

    CPC classification number: A61K31/335 ,  A61K31/365 ,  A61K31/39 ,  C08G67/04 ,  C08G69/08 ,  C08G69/10 ,  Y10S514/863

    Abstract: A method for synthesizing polyanhydrides in solution using coupling agents and a removable acid acceptor to effect a one-step polymerization of dicarboxylic acids. As used in the method, these coupling agents include phosgene, diphosgene, and acid chlorides. Insoluble acid acceptors include insoluble polyamines and crosslinked polyamines such as polyethyleneimine and polyvinylpyridine and inorganic bases such as K.sub.2 CO.sub.3, Na.sub.2 CO.sub.3, NaHCO.sub.3, and CaCO.sub.3. The only byproduct formed is a removable hydrochloric acid-acid acceptor.Examples are provided of the polymerization of highly pure polyanhydrides using phosgene, diphosgene or an acid chloride as the coupling agent, in combination with either an insoluble acid acceptor or a soluble acid acceptor in a solvent wherein the polymerization byproduct or polymer is insoluble.A particularly important application of these polyanhydrides is in the formation of drug delivery devices containing bioactive compounds. The method is also useful in the polymerization of dicarboxylic acids including heat liable dipeptides of glutamic or aspartic acid.

    Abstract translation: 使用偶联剂和可除去的酸受体在溶液中合成聚酐以进行二羧酸的一步聚合的方法。 如该方法所用，这些偶联剂包括光气，双光气和酰氯。 不溶性酸受体包括不溶性多胺和交联聚胺如聚乙烯亚胺和聚乙烯吡啶以及无机碱如K 2 CO 3，Na 2 CO 3，NaHCO 3和CaCO 3。 形成的唯一副产物是可除去的盐酸酸受体。 提供了使用光气，双极光或酰氯作为偶联剂的高纯度聚酐与在溶剂中的不溶性酸受体或可溶性酸受体组合的聚合反应，其中聚合副产物或聚合物是不溶的。 这些多酸酐的特别重要的应用是形成含有生物活性化合物的药物递送装置。 该方法也可用于二羧酸的聚合，包括谷氨酸或天冬氨酸的热应答二肽。

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