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    • 4. 发明申请
    • MICROPARTICLE COMPRISING CROSS-LINKED POLYMER
    • 包含交联聚合物的微晶
    • US20100291116A1
    • 2010-11-18
    • US12679132
    • 2008-09-26
    • Aylvin Jorge Angelo Athanasius DiasBartholomeus Johannes Margretha PlumAudrey PetitTristan Handels
    • Aylvin Jorge Angelo Athanasius DiasBartholomeus Johannes Margretha PlumAudrey PetitTristan Handels
    • A61K47/30C08G67/00B32B1/00A61K38/02A61K39/00A61K31/7088C08G73/00C08G75/00A61K31/573A61P31/00
    • A61K9/1641A61K9/5031Y10T428/2982Y10T428/2998
    • Microparticle comprising a cross-linked polymer comprising (a) a cross-linker comprising two or more radically polymerizable groups, preferably selected from the group consisting of alkenes, sulfhydryl (SH), thioic, unsaturated esters, unsaturated urethanes, unsaturated ethers, and unsaturated amides; (b) a monofunctional reactive diluent comprising maximum one unsaturated C—C bond represented by the formula R0—C(R1)═CHR2 Formula (I) wherein —R0 is chosen depending on the structure of a selected active agent (c) to be loaded into the microparticle and is chosen to have a structure that when combined with the other components of the microparticle provides a higher affinity of the selected active agent (c) for the microparticle; —each R1 is chosen from hydrogen and substituted and unsubstituted, aliphatic, cycloaliphatic and aromatic hydrocarbon groups which groups optionally contain one or more moieties selected from the group of ester moieties, ether moieties, thioester moieties, thioether moieties, carbamate moieties, thiocarbamate moieties, amide moieties and other moieties comprising one or more heteroatoms, in particular one or more heteroatoms selected from S, O, P and N, each R5 in particular independently being chosen from the group of hydrogen and substituted and unsubstituted alkyl groups, which alkyl groups optionally contain one or more heteroatoms, in particular one or more heteroatoms selected from P, S, O and N; —each R2 is chosen from hydrogen, —COOCH3, —COOC2H5, —COOC3H7, and —COOC4H9.
    • 包含交联聚合物的微粒包括(a)包含两个或更多个可自由基聚合基团的交联剂,优选选自烯烃,巯基(SH),硫代,不饱和酯,不饱和氨基甲酸酯,不饱和醚和不饱和醚 酰胺 (b)单官能反应性稀释剂,其包含由式R 0 -C(R 1)= CHR 2式(I)表示的最大一个不饱和C-C键,其中-R 0根据所选活性剂(c)的结构选择 加入到微粒中并被选择为具有当与微粒的其它组分组合时提供所选择的活性剂(c)对于微粒的较高亲合力的结构; - 每个R 1选自氢和取代和未取代的脂族,脂环族和芳族烃基,这些基团任选地含有一个或多个选自酯部分,醚部分,硫酯部分,硫醚部分,氨基甲酸酯部分,硫代氨基甲酸酯部分, 酰胺部分和包含一个或多个杂原子,特别是一个或多个选自S,O,P和N的杂原子的其它部分,每个R 5特别地独立地选自氢和取代和未取代的烷基,该烷基任选地 含有一个或多个杂原子,特别是一个或多个选自P,S,O和N的杂原子; - 每个R 2选自氢,-COOCH 3,-COOC 2 H 5,-COOC 3 H 7和-COOC 4 H 9。