首页> 外国专利> NANO-MICELLAR PREPARATION OF ANTHRACYLCLINE ANTITUMOR ANTIBIOTICS ENCAPSULATED BY THE PHOSPHATIDE DERIVATIZED WITH POLYETHYLENE GLYCOL

NANO-MICELLAR PREPARATION OF ANTHRACYLCLINE ANTITUMOR ANTIBIOTICS ENCAPSULATED BY THE PHOSPHATIDE DERIVATIZED WITH POLYETHYLENE GLYCOL

机译:聚乙烯醇衍生的磷脂包裹的蒽环类抗微生物剂的纳米胶体制备

摘要

The present invention provides a nano-micellar preparation of anthracycline antitumor antibiotics for intravenous injection, which comprises a therapeutically effective amount of anthracycline antitumor antibiotics, a phosphatide derivatized with polyethylene glycol, together with pharmaceutically acceptable adjuvants. The preparation is prepared by encapsulating the medicament with a nano-micelle to obtain the nano-micellar preparation of anthracycline antitumor antibiotics for injection. The anthracycline antitumor antibiotics and the phosphatide derivatized with polyethylene glycol form a nano-micelle with a highly homogeneous particle size. In the micelle, the hydrophobic core of encapsulated medicament is surrounded by polyethylene glycol molecules to form a hydrophilic protective layer, so that the medicament is prevented from contacting with the enzymes and other protein molecules in blood and being recognized and phagocytozed by reticuloendothelial system in the body, and the circulation time in vivo of the micelle is prolonged.
机译:本发明提供了用于静脉注射的蒽环类抗肿瘤抗生素的纳米胶束制剂,其包含治疗有效量的蒽环类抗肿瘤抗生素,被聚乙二醇衍生的磷脂以及药学上可接受的佐剂。通过将药物用纳米胶囊封装以获得用于注射的蒽环类抗肿瘤抗生素的纳米胶束制剂来制备制剂。蒽环类抗肿瘤抗生素和被聚乙二醇衍生的磷脂形成粒径均一的纳米胶束。在胶束中,被包封药物的疏水核被聚乙二醇分子包围,形成亲水性保护层,从而防止了药物与血液中的酶和其他蛋白质分子接触,并被网状内皮系统识别和吞噬。体内,胶束的体内循环时间延长。

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