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DRUG PREPARATION HAVING IMPROVED IN VIVO TOLERANCE

机译:体内耐受性得到改善的药物制备

摘要

PROBLEM TO BE SOLVED: To obtain the subject preparation useful for the treatment of malignant tumor, inflammatory disease and autoimmune disease by modifying a drug preparation, thereby improving the in vivo tolerance of an active compound in therapeutic use and, in some case, increasing the drug effect. SOLUTION: The objective drug preparation is prepared by including a glycosyl-Y-[-C(=Y)-X]p -W(R)n -X-C(=Y)-active compound (glycosyl is an enzymatically cleavable polysaccharide, etc.; W is an aromatic group, etc.; R is H, methyl, etc.; (p) is 0 or 1; (n) is an integer; X and Y are each O, NH, etc.; the active compound is a biologically active compound linked through hydroxyl group, etc., especially anthracycline, preferably doxorubicin, etoposide, vindesine, vinblastine, etc.), a sugar and/or a sugar alcohol (glucose, mannose, fructose, etc.), a pharmacologically permissible carrier and optionally a bivalent ion (Ca, Mg, Fe, etc.).
机译:要解决的问题:通过修饰药物制剂来获得可用于治疗恶性肿瘤,炎性疾病和自身免疫性疾病的主题制剂,从而提高治疗性用途中活性化合物的体内耐受性,并在某些情况下提高药物的活性。药物作用。解决方案:通过包含糖基-Y-[-C(= Y)-X] p -W(R)n -XC(= Y)活性化合物(糖基是可酶切的多糖等)制备目标药物制剂;; W是芳香族基团等; R是H,甲基等;(p)是0或1;(n)是整数; X和Y分别是O,NH等;活性化合物是通过羟基等连接的生物活性化合物,尤其是蒽环类,优选阿霉素,依托泊苷,长春地辛,长春碱等),糖和/或糖醇(葡萄糖,甘露糖,果糖等),在药理上允许的载体和可选的二价离子(Ca,Mg,Fe等)。

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