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本文描叙了一种新型水溶性药物传递系统的制备与特点。包括白蛋白微球体(平均直径为1μ)含有超细度磁性粒子、磁铁和原型药物羟基柔毛霉素。外部用一个有适当强度的磁场能将静脉注射的磁性微球体局限于体内所要达到的靶位。这种化疗药物部位特异的传递,使得希望药物在体内达到的部位有最大浓度, 比一般全身给药需要的剂量小并可减少其毒性。微球体的制备——(1)热稳定化的微球体:制备一种每毫升含人血清白蛋白(Ⅰ)250 mg,~(125)碘-牛血清白蛋白(Ⅱ)0.02ml,大部分纯化的羟基柔毛霉素(Ⅲ)32mg 和直径为10～20nm 的磁性粒子(Ⅳ)72mg 的水混悬液。将这种混悬液0.5ml 一份份加至30ml 棉子油中,所得乳剂用超声波处理,在4°匀化1分钟,再将此匀化物逐滴加至100ml 预热至110～
This article describes the preparation and characteristics of a novel water-soluble drug delivery system. Including albumin microspheres (average diameter of 1μ) containing ultrafine magnetic particles, magnets and the prototype drug hydroxy daunorubicin. External use of a magnetic field with appropriate intensity can be intravenous injection of magnetic microspheres confined to the body to reach the target site. The site-specific delivery of this chemotherapeutic drug results in the maximum concentration of drug that is expected to reach the body in vivo, which is less than the dose required for general systemic administration and reduces its toxicity. Preparation of Microspheres- (1) Thermo Stabilized Microspheres: A solution of 250 mg of human serum albumin (I) per ml, 0.02 ml of ~ (125) iodine-bovine serum albumin An aqueous suspension of 32 mg of the purified hydroxyactamycin (III) and 72 mg of a magnetic particle (IV) having a diameter of 10 to 20 nm was suspended. 0.5 ml of this suspension is added in one portion to 30 ml of cottonseed oil, the resulting emulsion is sonicated and homogenized at 4 ° for 1 minute, and this homogenate is added dropwise to a mixture of 100 ml preheated to 110 -