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    • 1. 发明授权
    • 고체분산체 및 그 제조방법
    • 고체분산체및그제조방법
    • KR100676298B1
    • 2007-01-30
    • KR1020050078006
    • 2005-08-24
    • 씨제이 주식회사
    • 노현정김택로조청일고동현김태형서혜란조일환김창주
    • A61K31/4196
    • A solid dispersion is provided to show improved dissolution rate of a medicine, and improved stability of the dissolution rate according to passing of the storage time. The solid dispersion containing a compound represented by the formula(1) is prepared by dispersing a mixture consisting of a water-soluble polymer selected from the group consisting of poloxamer, polyethylene glycol, polyvinylpyrrolidone, copolymer of vinylpyrrolidone and vinyl acetate, and a mixture thereof, a surfactant having more than 10 of HLB, and the compound of the formula(1) in a strong disintegrating agent selected from the group consisting of crosscamellose sodium, sodium starch glycolate, crosspovidone, pre-gelatinized starch and a mixture thereof or a mixture consisting of the strong disintegrating agent and a pharmaceutically acceptable excipient. In the formula(1), R1 is C3-6 cycloalkyl, C3-6 cycloalkenyl, phenyl, C1-6 alkyl, C1-6 haloalky, C1-6 alkoxy, C1-6 haloalkoxy, phenyl substituted by at least one selected from the group consisting of halogen, amino, monoalkylamino, dialkylamino, nitro and cyano, styrenyl, C1-6 alkoxy styrenyl, and pyridyl, R2 is methyl or amino, and each A, B, C and D is independently C or N. Regarding the total weight of the dispersion, 0.1-10 wt.% of the water soluble polymer and 0.1-10 wt.% of the surfactant are contained.
    • 提供固体分散体以显示药物的溶解速率提高,并且随着储存时间的过去而改善溶解速率的稳定性。 含有由式(1)表示的化合物的固体分散体通过将由选自泊洛沙姆,聚乙二醇,聚乙烯吡咯烷酮,乙烯基吡咯烷酮和乙酸乙烯酯的共聚物及其混合物的水溶性聚合物组成的混合物 中,具有超过10的HLB的表面活性剂,和式(1)的在选自由crosscamellose钠,淀粉羟乙酸钠,交联聚维所组成的组中选择的强崩解剂的化合物中,预胶化淀粉和它们的混合物或混合物 由强力崩解剂和药学上可接受的赋形剂组成。 在式(1)中,R1是C3-6环烷基,C3-6环烯基,苯基,C1-6烷基,C1-6卤代烷基,C1-6烷氧基,C1-6卤代烷氧基,被选自 选自卤素,氨基,单烷基氨基,二烷基氨基,硝基和氰基,苯乙烯,C 1-6烷氧基苯乙烯基和吡啶基的基团,R 2是甲基或氨基,且每个A,B,C和d独立地是C或N.关于总 包含分散体的重量,0.1-10重量%的水溶性聚合物和0.1-10重量%的表面活性剂。