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    • 2. 发明授权
    • Entrapment or microencapsulation of drugs in a polyhydroxyalkanoate
formed by enzyme synthesis
    • 通过酶合成形成的聚羟基链烷酸酯中的药物的包封或微胶囊化
    • US6146665A
    • 2000-11-14
    • US150019
    • 1998-09-09
    • Robert H. MarchessaultDusica MaysingerGeoffrey Alan Ralph Nobes
    • Robert H. MarchessaultDusica MaysingerGeoffrey Alan Ralph Nobes
    • A61K9/16A61K9/50C12P7/62A61K9/14C12N11/04
    • A61K31/7048A61K9/1647A61K9/5031C12P7/625
    • A hydrophilic or lipophilic drug is entrapped or microencapsulated in a polyhydroxyalkanoate homopolymer or copolymer. The homopolymer or copolymer is synthesized in an aqueous medium containing a dissolved hydrophilic drug by in vitro enzyme polymerization of a hydroxyalkanoate Coenzyme A monomer to form microporous granules entrapping the drug. The enzyme may be a polyhydroxyalkanoate synthase, and the monomer may be 3-hydroxybutyryl Coenzyme A or 3-hydroxyvalerate Coenzyme A. The monomer is produced by reaction of a carboxylic acid group of a hydroxyalkanoic acid with a thiol group of Coenzyme A. To microencapsulate a lipophilic drug, droplets of oil containing a lipophilic drug are formed dispersed in an aqueous medium such as in the form of an oil-in-water emulsion. The polyhydroxyalkanoate homopolymer or copolymer is formed in the aqueous medium by the enzyme polymerization to form microcapsules having a core of oil containing the drug. The granules or microcapsules containing the drug may be dried.
    • 亲水或亲脂性药物被包埋或微胶囊化在聚羟基链烷酸酯均聚物或共聚物中。 均聚物或共聚物在含有溶解的亲水性药物的水性介质中通过羟基链烷酸酯辅酶A单体的体外酶聚合形成包埋该药物的微孔颗粒。 该酶可以是聚羟基链烷酸酯合成酶,单体可以是3-羟基丁酰辅酶A或3-羟基戊酸酯辅酶A.单体是通过羟基链烷酸的羧酸基团与辅酶A的硫醇基团的反应制备的。为了将微囊化 形成亲水性药物,含有亲脂性药物的油滴分散在水性介质中,例如以水包油乳液的形式。 通过酶聚合在水性介质中形成聚羟基链烷酸酯均聚物或共聚物,以形成含有药物核心的微胶囊。 可以干燥含有药物的颗粒或微胶囊。
    • 3. 发明授权
    • Diblock copolymer and use thereof in a micellar drug delivery system
    • 二嵌段共聚物及其在胶束药物递送系统中的用途
    • US06469132B1
    • 2002-10-22
    • US09563380
    • 2000-05-03
    • Adi EisenbergDusica MaysingerChristine Allen
    • Adi EisenbergDusica MaysingerChristine Allen
    • C08G6308
    • C08G63/664
    • The present invention relates to diblock copolymers and more particularly to polycaprolactone-b-polyethylene oxide (PCL-b-PEO) diblock copolymers used in micellar systems, for delivering a biologically active agent to a site. There is provided a diblock copolymer compound comprising a hydrophilic block and a hydrophobic block, the hydrophilic block comprising a polyethylene oxide (PEO) polymer, the hydrophobic block comprising a polycaprolactone (PCL) polymer, the PCL polymer comprising a number of caprolactone monomers selected from 5 to 150, the PEO polymer comprising a number of ethylene oxide monomers selected from 30 to 100. The diblock copolymer compound of the present invention may be used to form a micellar delivery system for delivering biologically active agents such as lipophilic drugs to sites such as the central nervous system. The hydrophobic reservoir obtained enables a larger amount of agent to be incorporated therein, with a slower release and without the damaging effects that such high doses would induce with known delivery systems.
    • 本发明涉及二嵌段共聚物,更具体地涉及用于胶束体系中的聚己内酯-b-聚环氧乙烷(PCL-b-PEO)二嵌段共聚物,用于将生物活性剂递送至位点。 提供包含亲水嵌段和疏水嵌段的二嵌段共聚物化合物,所述亲水性嵌段包含聚环氧乙烷(PEO)聚合物,所述疏水嵌段包含聚己酸内酯(PCL)聚合物,所述PCL聚合物包含多个选自以下的己内酯单体 5至150,PEO聚合物包含多个选自30至100的环氧乙烷单体。本发明的二嵌段共聚物化合物可用于形成胶束递送系统,用于将生物活性剂如亲脂性药物递送至诸如 中枢神经系统。 获得的疏水性储存容器可以加入更多量的药剂,其释放较慢,并且不会产生这种高剂量可以用已知递送系统诱导的破坏作用。