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    • 1. 发明公开
    • 실로스타졸의 제어방출 제제 및 그 제조방법
    • 含有西兰坦的控制释放制剂及其制备方法
    • KR1020080076382A
    • 2008-08-20
    • KR1020070016221
    • 2007-02-15
    • (주)아모레퍼시픽주식회사 에스트라
    • 박진우신광현빈성아이혁배준호전도용
    • A61K9/22A61K31/4709
    • A61K9/0065A61K9/2031A61K9/2054A61K31/4709
    • A controlled-release preparation containing cilostazol is provided to improve absorption rate of cilostazol in small intestine and reduce side effects such as headache by staying in stomach for a long time and slowly releasing cilostazol, and enhance compliance of patient by reducing dosage frequency. A controlled-release preparation contains 10-80 wt.% of cilostazol or its pharmaceutically acceptable salt, 0.1-50 wt.% of solubilizer, 5-80 wt.% of swelling agent, 0.5-50 wt.% of swelling speed-controller and 0.1-50 wt.% of gas-generating material. A method for preparing the controlled-release preparation containing cilostazol comprises the steps of: mixing cilostazol or its pharmaceutically acceptable salt, solubilizer, swelling agent, swelling speed-controller and gas-generating material; granulating the mixture; and filling the granulates in capsules or tabletting the granulates.
    • 提供含有西洛他唑的控释制剂,以提高西洛他唑在小肠中的吸收率,并通过长时间停留在胃中并缓慢释放西洛他唑,减少头痛的副作用,并通过降低剂量频率增强患者的依从性。 控释制剂含有10-80重量%的西洛他唑或其药学上可接受的盐,0.1-50重量%的增溶剂,5-80重量%的溶胀剂,0.5-50重量%的溶胀速度控制剂 和0.1-50重量%的气体发生材料。 制备含有西洛他唑的控释制剂的方法包括以下步骤:将西洛他唑或其药学上可接受的盐,增溶剂,溶胀剂,溶胀速度控制器和产气材料混合; 制粒混合物; 并将颗粒填充在胶囊中或压制颗粒。
    • 2. 发明公开
    • 실로스타졸의 제어방출 제제 및 그 제조방법
    • 含有西兰坦的控制释放制剂及其制备方法
    • KR1020080076440A
    • 2008-08-20
    • KR1020070016352
    • 2007-02-16
    • (주)아모레퍼시픽주식회사 에스트라
    • 박진우신광현권민정배준호전도용
    • A61K9/10A61K9/16
    • A61K9/2054A61K9/1635A61K9/1652A61K9/1694A61K9/205A61K9/2077A61K31/4709
    • A controlled-release preparation containing cilostazol is provided to minimize side effects such as headache due to immediate release of cilostazol, and improve compliance of patient by maintaining effective blood concentration of cilostazol and reducing dosage frequency. A controlled-release preparation contains 10-80 wt.% of cilostazol or its pharmaceutically acceptable salt, 0.1-50 wt.% of solubilizer and 5-80 wt.% of erodible hydrogel-forming material selected from polyethylene oxide, hydroxyalkylcellulose, hydroxypropylalkylcellulose, polyvinylalcohol, polyvinylpyrrolidone, sodium carboxymethylcellulose, propyleneglycol alginate, carbopol, sodium alginate, xanthan gum, locust bean gum, cellulose gum, gellan gum, tragacanth gum, karaya gum, guar gum, acacia gum and a mixture thereof. A method for preparing the controlled-release preparation containing cilostazol comprises the steps of: (1) mixing cilostazol or its pharmaceutically acceptable salt with solubilizer and granulating the mixture by solid dispersion to prepare solubilized drug granules; and (2) mixing the solubilized drug granules with erodible hydrogel-forming material and granulating the mixture.
    • 提供含有西洛他唑的控释制剂以最小化由于西洛他唑立即释放引起的头痛等副作用,并通过维持西洛他唑有效血药浓度和降低剂量频率来提高患者的依从性。 控释制剂含有10-80重量%的西洛他唑或其药学上可接受的盐,0.1-50重量%的增溶剂和5-80重量%的可溶性水凝胶形成材料,其选自聚环氧乙烷,羟烷基纤维素,羟丙基烷基纤维素, 聚乙烯醇,聚乙烯吡咯烷酮,羧甲基纤维素钠,藻酸丙二醇酯,聚羧乙烯,藻酸钠,黄原胶,刺槐豆胶,纤维素胶,结冷胶,黄蓍胶,刺梧桐胶,瓜尔胶,阿拉伯树胶及其混合物。 制备含有西洛他唑的控释制剂的方法包括以下步骤:(1)将西洛他唑或其药学上可接受的盐与增溶剂混合并通过固体分散体制粒混合物以制备溶解的药物颗粒; 和(2)将溶解的药物颗粒与可侵蚀的水凝胶形成材料混合并将混合物制粒。