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    • 2. 发明授权
    • Sustained-release preparation of physiologically active polypeptide and production thereof
    • 生理活性多肽的缓释制剂及其制备
    • US06482864B1
    • 2002-11-19
    • US09319023
    • 1999-05-28
    • Yutaka YamagataMasafumi MisakiSusumu Iwasa
    • Yutaka YamagataMasafumi MisakiSusumu Iwasa
    • A61K4732
    • A61K9/1647A61K38/27Y10S514/964
    • A method for producing a sustained-release preparation, which comprises dispersing a physiologically active polypeptide into an organic solvent solution of a biodegradable polymer and removing the organic solvent, wherein the polypeptide is a powder obtained by lyophilizing an aqueous solution of the polypeptide which solution has a water-miscible organic solvent and/or a volatile salt; which improves the ease of handling of the physiologically active polypeptide powder in the process for producing the preparation; which makes it possible to industrially produce the sustained-release preparation in large scale; which provides a sustained-release preparation showing high and stable concentration of the active component in blood in long term, low initial release ratio of the physiologically active polypeptide, and high entrapment ratio of the polypeptide into the sustained-release preparation.
    • 一种缓释制剂的制备方法,其包括将生理活性多肽分散到生物可降解聚合物的有机溶剂溶液中并除去有机溶剂,其中所述多肽是通过将多肽溶液冻干得到的粉末 水混溶性有机溶剂和/或挥发性盐; 这提高了在制备该制剂的过程中易于处理生理活性多肽粉末; 这使得可以大规模地工业生产缓释制剂; 其提供持续释放制剂,其显示出高生产活性多肽的长期,低的初始释放比例以及所述多肽进入缓释制剂的高滞留比,从而高效稳定血液中活性成分的浓度。