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本文报告了高三尖杉酯碱多相脂质体(139-5号)的处方设计、制备工艺及抗肿瘤和临床前药理研究结果。139—5号中加入免疫促进剂,制备工艺采用熔融法。小鼠尾静脉注射给药,剂量为1.0mg/kg 时对 L_(615)和 S_(180)的抑制率分别为37.3—57.4%和50.0—72.3%;剂量为0.75mg/kg 时,对 S_(180)的抑制率为34.1-50.9%;均高于其水溶液对照组。小鼠尾静脉和腹腔一次给药的 LD_(50)分别为3.53mg/kg 和2.44mg/kg。家兔耳静脉连续给药15天,高剂量(0.30mg/kg/day)对造血功能有一定抑制作用,观察到可逆性肝细胞变性,其它脏器未发现明显病变。
This article reports on the formulation design, preparation process, and anti-tumor and preclinical pharmacological studies of homoharringtonine multiphasic liposomes (139-5). No. 139-5 added immune booster, the preparation process using the melting method. When mice were given tail vein injection, the inhibitory rates of L_ (615) and S_ (180) were 37.3–57.4% and 50.0–72.3% at a dose of 1.0 mg/kg, respectively; at a dose of 0.75 mg/kg, S_ The inhibition rate of (180) was 34.1-5.9%; both were higher than the aqueous control group. LD 50 in the tail vein and intraperitoneal administration of mice were 3.53 mg/kg and 2.44 mg/kg, respectively. The rabbit ear vein was continuously administered for 15 days. High dose (0.30 mg/kg/day) had a certain inhibitory effect on hematopoietic function, and reversible hepatocyte degeneration was observed. No other lesions were found in other organs.