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    • 9. 发明申请
    • HIGH-THROUGHPUT FABRICATION OF MICROPARTICLES
    • 高通量微波炉的制造
    • WO2007078765A2
    • 2007-07-12
    • PCT/US2006047519
    • 2006-12-13
    • MASSACHUSETTS INST TECHNOLOGYLITTLE STEVEN RANDERSON DANIEL GLANGER ROBERT S
    • LITTLE STEVEN RANDERSON DANIEL GLANGER ROBERT S
    • C08G77/42
    • A61K9/1647A61K9/1694
    • The optimatization of microparticle formulations has become increasingly difficult given the numerous parameters (e.g., polymer, polymer blend, agent to be delivered, particle size, pharaceutical excipients) that can be varied in preparing microparticles. The high-throughput fabrication of microparticles based on the double emulsion/solvent evaporation technique is therefore a breakthrough in screening and optimizing microparticle formulations for particular characteristics. This new system allows for the preparation of multiple (e.g., over 20, over 50, over 100, over 500, etc.) microparticle formulations in parallel. The system involves the formation of an emulsion containing aqueous bubbles with the payload in an organic phase containing the polymer or polymer blend being used for the microparticles. This first emulsion is then transferred to a larger aqueous phase, and a second water- in-oil-in water emulsion is formed. The organic solvent is then removed, and the resulting particles are optionally washed and/or freeze dried. The resulting microparticles are similar or better than microparticles prepared using the traditional one formulation at a time approach. The high-throughput fabrication of microparticles is particularly useful in optimizing microparticles formulations for drug delivery.
    • 鉴于在制备微粒中可以变化的许多参数(例如,聚合物,聚合物共混物,待递送的试剂,粒径,药物赋形剂),微粒制剂的优化变得越来越困难。 因此,基于双重乳液/溶剂蒸发技术的微粒的高通量制造是筛选和优化微粒制剂以获得特定特征的突破。 该新系统允许并行制备多个(例如,超过20个,超过50个,超过100个,超过500个等等)微粒制剂。 该系统包括在含有用于微粒的聚合物或聚合物共混物的有机相中形成含有水泡的含水气泡。 然后将该第一乳液转移到较大的水相中,并形成第二水包油包水乳液。 然后除去有机溶剂,任选地将所得颗粒洗涤和/或冷冻干燥。 所得到的微粒类似于或优于使用传统的一种制剂在一段时间内制备的微粒。 微粒的高通量制造特别可用于优化用于药物递送的微粒制剂。