会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 2. 发明申请
    • CELLULOSE DERIVATIVES FOR INHIBITING CRYSTALLIZATION OF POORLY WATER-SOLUBLE DRUGS
    • 用于抑制不溶性水溶性药物结晶的纤维素衍生物
    • WO2013106433A1
    • 2013-07-18
    • PCT/US2013/020835
    • 2013-01-09
    • VIRGINIA TECH INTELLECTUAL PROPERTIES, INC.PERDUE RESEARCH FOUNDATION
    • EDGAR, Kevin, J.LI, BinTAYLOR, LynneILEVBARE, GraceWILLIAMS, Stephanie, M.LIU, Haoyu
    • A61K47/38A61K47/30A61K9/08A61K31/70
    • A61K47/38A61K9/146A61K31/05A61K31/352A61K31/357A61K31/40A61K31/427A61K31/536A61K31/70C08B3/00
    • The present invention relates to the fields of chemistry and pharmaceuticals. Embodiments of the invention provide cellulose esters useful for inhibiting solution crystallization of drugs. Specific polymers of the invention include cellulose esters of formula (I) : wherein n of the ω-carboxyalkanoyl group, Formula (II), is 3, 4, 6, or 8 to provide a ω-carboxyalkanoyl group chosen from succinoyl, glutaroyl, adipoyl, sebacyl, and suberyl groups; and wherein R is chosen from : a hydrogen atom; and an alkanoyl group chosen from acetyl, propionyl, butyryl, valeroyl, hexanoyl, nonanoyl, decanoyl, lauroyl, palmitoyl, and stearoyl groups; wherein there is a total degree of substitution of the alkanoyl group and the ω-carboxyalkanoyl group of at least 2.0; and wherein the polymer comprises m repeating units where n = 1 to 1,000,000, or 10 to 100,000, or 100 to 1,000, such as 1 to 6,000. Embodiments further include compositions comprising cellulose esters and poorly water-soluble drugs, which compositions exhibit greater solubility and stability in solution as compared to the drugs alone. Drugs that can be used in combination with such polymers include but are not limited to ritonavir, efavirenz, etravirine, celecoxib, clarithromycin, curcumin, ellagic acid, quercetin, naringenin, and resveratrol. Methods for making and using the compounds and compositions are also included within the scope of the invention.
    • 本发明涉及化学和药物领域。 本发明的实施方案提供了可用于抑制药物溶液结晶的纤维素酯。 本发明的具体聚合物包括式(I)的纤维素酯:其中式(II)的ω-羧基烷酰基中的n为3,4,6或8,以提供选自琥珀酰基,戊酰基, 己二酰基,癸二酰基和辛二酸基; 并且其中R选自:氢原子; 和选自乙酰基,丙酰基,丁酰基,戊酰基,己酰基,壬酰基,癸酰基,月桂酰基,棕榈酰基和硬脂酰基的烷酰基; 其中烷酰基和ω-羧基烷酰基的总取代度为至少2.0; 并且其中所述聚合物包含m个重复单元,其中n = 1至1,000,000,或10至100,000,或100至1,000,如1至6,000。 实施方案还包括包含纤维素酯和水溶性差的药物的组合物,与单独的药物相比,该组合物在溶液中表现出更大的溶解度和稳定性。 可以与这些聚合物组合使用的药物包括但不限于利托那韦,依法韦仑,依伐维林,塞来昔布,克拉霉素,姜黄素,鞣花酸,槲皮素,柚皮苷和白藜芦醇。 制备和使用化合物和组合物的方法也包括在本发明的范围内。