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    • 96. 发明申请
    • Pullulan-containing powder, process for producing the same and use thereof
    • 含有支链淀粉的粉末,其制造方法及其用途
    • US20040197410A1
    • 2004-10-07
    • US10484216
    • 2004-01-20
    • Toshiyuki SugimotoToshio Miyake
    • C12P019/04A61K009/14C08B037/00
    • C08J3/12A23L29/274A23P20/20A61K8/0212A61K8/11A61K8/73A61Q5/02A61Q17/04A61Q19/00A61Q19/02C08B37/0018C08J3/14C08J2305/00C08K5/15C08L5/00C08L5/16C08L2666/26
    • The object of the present invention is to overcome conventional demerits of pullulan powders prepared by conventional techniques, i.e., they could not be homogeneously mixed with non-reducing saccharides composed of glucose units when mixed together, and the resulting mixtures do not easily dissolve in water; and to provide a pullulan-containing powder with an improved rate of water dissolution, as well as to provide preparations and uses thereof. The present invention solves the above object by providing a pullulan-containing powder which uniformly comprises pullulan as a main ingredient and a non-reducing saccharide, and their process and uses; wherein the pullulan-containing powder is prepared by the steps of preparing a solution dissolving pullulan and a non-reducing saccharide homogeneously, pulverizing the solution, and collecting the resulting pullulan-containing powder. The powder has an improved rate of water dissolution, while retaining satisfactory resistance to humidity without fear of causing separation between the pullulan and the non-reducing sccharide.
    • 本发明的目的是克服通过常规技术制备的支链淀粉粉末的常规缺点,即当它们混合在一起时不能与由葡萄糖单元组成的非还原性糖类均匀混合,并且所得混合物不容易溶于水 ; 并提供具有改善的水溶解速率的含支链淀粉的粉末,以及提供其制备和用途。 本发明通过提供均匀地包含支链淀粉作为主要成分和非还原性糖的支链淀粉粉末及其工艺和用途来解决上述目的。 其中含有支链淀粉的粉末通过以下步骤制备:均匀地制备溶解支链淀粉和非还原性糖的溶液,粉碎溶液,并收集所得的含支链淀粉粉末。 粉末具有提高的水溶解速率,同时保持令人满意的耐湿性,而不用担心在支链淀粉和非还原性螯合剂之间分离。
    • 100. 发明授权
    • Camptothecin derivatives
    • 喜树碱衍生物
    • US5892043A
    • 1999-04-06
    • US773182
    • 1996-12-27
    • Kenji TsujiharaTakayuki KawaguchiSatoshi OkunoToshiro Yano
    • Kenji TsujiharaTakayuki KawaguchiSatoshi OkunoToshiro Yano
    • A61K47/48C08B37/00C08B37/02C07D471/00
    • C08B37/0018A61K47/4823A61K47/48338C08B37/0021
    • A camptothecin derivative comprising a compound of the formula �I!: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is --X.sub.n --Alk.sub.m --R.sup.6, and the other two are H, alkyl or halogen, or (B) adjacent two groups combine to form alkylene, and one of the carbon atoms of said alkylene group is substituted by --X.sub.n --Alk.sub.m --R.sup.6, and the remaining three groups are H, alkyl or a halogen, and one or two --CH.sub.2 -- of the alkylene in (A) or (B) may optionally be replaced by --O--, --S-- or --NH--, X is --O-- or --NH--, Alk is alkylene, R.sup.6 is --NH.sub.2, ##STR2## or --OH, m and n are both 0 or 1, or m is 1 and n is 0, which camptothecin compound is bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof. Said camptothecin derivatives show enhanced antitumor activities but few side effects and are useful as a medicament.
    • 包含式[I]化合物的喜树碱衍生物:其中R 1,R 2,R 3,R 4和R 5是(A)相邻的两个基团结合形成亚烷基,或两者都是H,并且其中之一 其余三个为-Xn-Alkm-R6,另外两个为H,烷基或卤素,或(B)相邻的两个基团结合形成亚烷基,所述亚烷基的一个碳原子被-Xn- Al-C-R6,其余三个基团是H,烷基或卤素,并且(A)或(B)中亚烷基的一个或两个-CH 2可以任选地被-O - , - S-或-NH - ,X为-O-或-NH-,Alk为亚烷基,R6为-NH2,或IMA为-OH,m和n均为0或1,或m为1,n为0,喜树碱化合物为 通过氨基酸或肽或其药学上可接受的盐与具有羧基的多糖结合。 所述喜树碱衍生物显示出增强的抗肿瘤活性,但副作用很少,可用作药物。