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1. 发明申请

US20060141041A1 METHODS AND COMPOSITIONS FOR THE TARGETED DELIVERY OF BIOLOGICALLY ACTIVE AGENTS 失效
标题翻译：用于有针对性地提供生物活性剂的方法和组合物
公开(公告)号：US20060141041A1
公开(公告)日：2006-06-29
申请号：US10342448
申请日：2003-01-14
申请人： Mark Tracy , David Scher
发明人： Mark Tracy , David Scher
IPC分类号： A61K38/21 , A61K38/20 , A61K38/19 , A61K9/14
CPC分类号： A61K9/1647 , Y02A50/411 , Y02A50/423
摘要： The present invention relates to a sustained release composition for the targeted delivery of biologically active agents to specific tissues and cells. The composition comprises microparticles containing a biocompatible polymer, a water-soluble polymer and a biologically active agent. In one embodiment, the biologically active agent is an antigen or an immunomodulator. In another embodiment, the biologically is a labile agent. The microparticles have a number median diameter of greater than 20 microns upon administration. The water-soluble polymer is present in the sustained released composition in at least about 20% of the dry weight of the microparticle. the sustained release composition provides for the dissolution of the water-soluble polymer of the composition upon hydration, at a much greater rate than the degradation of the biocompatible polymer. This variance is solubility generates pseudo-microparticles which have a number median diameter which is substantially smaller than the size of the administered microparticles. The pseudo-microparticles can be engulfed by antigen presenting cells of the immune system, or absorbed by the Peyer's patches in the gut.
摘要翻译：本发明涉及用于将生物活性剂靶向递送至特定组织和细胞的持续释放组合物。该组合物包含含有生物相容性聚合物，水溶性聚合物和生物活性剂的微粒。在一个实施方案中，生物活性剂是抗原或免疫调节剂。在另一个实施方案中，生物学上是不稳定剂。微粒在给药时的中值直径大于20微米。水溶性聚合物以至少约20％的微粒干重存在于持续释放的组合物中。持续释放组合物提供组合物的水溶性聚合物在水合时以比生物相容性聚合物降解更大的速率溶解。这种方差是溶解度产生具有基本上小于施用的微粒尺寸的数字中值直径的假微粒。伪微粒可以被免疫系统的抗原呈递细胞吞噬，或被肠道中的派耶氏斑块吸收。

2. 发明申请

US20050260272A1 Method of forming microparticles that include a bisphosphonate and a polymer 审中-公开
标题翻译：形成包含二膦酸盐和聚合物的微粒的方法
公开(公告)号：US20050260272A1
公开(公告)日：2005-11-24
申请号：US11122796
申请日：2005-05-05
申请人： Maria Figueiredo , Rajesh Kumar , Maura Maloney , Kristin Prinn , David Scher , Gregory Troiano , Thean Yeoh , Stephen Zale
发明人： Maria Figueiredo , Rajesh Kumar , Maura Maloney , Kristin Prinn , David Scher , Gregory Troiano , Thean Yeoh , Stephen Zale
IPC分类号： A61K9/14 , A61K9/16 , A61K9/19 , A61K9/50 , A61K31/66 , A61K31/675 , B01J13/02 , B01J13/04 , C08L23/08
CPC分类号： A61K9/1647 , A61K9/1641 , A61K9/1694 , A61K9/19 , C08L23/08 , C08L23/0815 , C08L2205/02 , C08L2666/06
摘要： Microparticles that include a bisphosphonate and a polymer are produced by a method that includes forming a water-in-oil emulsion by mixing an aqueous solution of the bisphosphonate with a combination of a biocompatible polymer and a polymer solvent. At least one aqueous liquid can be mixed with the water-in-oil emulsion to form a water-in-oil-in-water emulsion and to extract the polymer solvent from the polymer, thereby forming the microparticles. Methods of treating a patient in need of therapy include administering the microparticles described to the patient. In one embodiment, the microparticles are formulated for the sustained release of the bisphosphonate.
摘要翻译：包括二膦酸盐和聚合物的微粒通过包括通过将二膦酸盐的水溶液与生物相容性聚合物和聚合物溶剂的组合混合形成油包水乳液的方法来制备。可以将至少一种含水液体与油包水乳液混合以形成水包油包水乳液，并从聚合物中提取聚合物溶剂，从而形成微粒。治疗需要治疗的患者的方法包括将所描述的微粒给予患者。在一个实施方案中，将微粒配制成二膦酸盐的持续释放。

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