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Use of biodegradable microspheres for the delivery of a anticancer agent for the treatment of glioblastoma

机译:可生物降解的微球在递送抗癌剂中治疗胶质母细胞瘤的用途

摘要

Biodegradable microspheres are prepared by dispersing an anticancer agent in an organic solvent with vigorous stirring, addi polymer, mixing with an aqueous phase to form an emulsion. The organic solvent is extracted by addition of water and the suspens of microspheres is filtered off. Biodegradable microspheres are prepared by dispersing an anticancer agent in an organic solvent with vigorous stirring, add a polymer, mixing with an aqueous phase to form an emulsion. The organic solvent is extracted by addition of water and the suspens of microspheres is filtered off. The organic solvent used is preferably dichloromethane, and the mixing is effected at around 2 degrees C. The polymer is preferably poly(d,l-lactic acid/glycolic acid), (PLAGA) equal quantities of the two acids being used i the copolymerization. The anticancer agent is hydrophilic and /or does not cross the blood brain barrier. It may be a 5-fluorour (5-FU), platinum derivatives, taxanes, gemcitabine, VP16, mitomycin, idoxuridine, topoisomerase 1 inhibitors, nitroso ureas, methotrexate, bleomycin, adriamycin, cytoxan, vincristin, and immunomodulating cytokins. Independent claims cover the use of these suspensions as medicines to be used simultaneously, sequentially, or separately t radiotherapy to treat glioblastomas, the microspheres being injected into the into the parenchymatous space and increasing the l span of the patient by at least 90 weeks, preferably at least 160 weeks.
机译:通过在剧烈搅拌下将抗癌剂分散在有机溶剂中,添加聚合物,与水相混合以形成乳液来制备可生物降解的微球。通过添加水萃取有机溶剂,并将微球的悬浮液滤出。通过在剧烈搅拌下将抗癌剂分散在有机溶剂中,添加聚合物,与水相混合以形成乳液,来制备可生物降解的微球。通过添加水萃取有机溶剂,并将微球的悬浮液滤出。所使用的有机溶剂优选为二氯甲烷,并且混合在约2℃下进行。聚合物优选为聚(d,1-乳酸/乙醇酸),(PLAGA)在共聚合中使用的两种酸的量相等。 。该抗癌剂是亲水的和/或不穿过血脑屏障。它可能是5-氟尿嘧啶(5-FU),铂衍生物,紫杉烷类,吉西他滨,VP16,丝裂霉素,异氧尿苷,拓扑异构酶1抑制剂,亚硝基尿素,甲氨蝶呤,博来霉素,阿霉素,cytoxan,vincristin和免疫调节细胞因子。独立权利要求涵盖将这些混悬液用作在放疗中同时,顺序或分别用于治疗胶质母细胞瘤的药物的用途,将微球体注射到实质性空间中,并使患者的跨度至少延长90周,最好是至少160周。

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