5-氟尿嘧啶两种不同制剂急性毒性比较

Comparison of acute toxicity of two different preparations of 5-fluorouracil

目的 比较 5 氟尿嘧啶 ( 5 Fu)两种不同制剂急性毒性的差异。方法 采用静脉注射 (iv)、腹腔注射 (ip)两种途径 ,观察小鼠给予包封有 5 Fu的GalCer脂质体或 5 Fu注射剂后所产生的毒性反应和死亡情况 ,计算半数致死量(LD50 )。结果 iv 5 FuGalCer脂质体和iv 5 Fu的LD50 分别为 2 70 .1、189.6mg/kg ;其 95 %可信区间分别为 2 2 2 .0～32 7.5、14 4 .7～ 2 4 7.6mg/kg。ip 5 FuGalCer脂质体和ip 5 Fu的LD50 分别为 380 .2和 2 5 7.7mg/kg ;其 95 %可信区间分别为 310 .6～ 4 6 1.1和 2 13.1～ 35 2 .5mg/kg。 5 FuGalCer脂质体和 5 Fu相比 ,两种制剂的iv、ip给药途径的LD50 差异均有显著性。结论 5 FuGalCer脂质体急性毒性小于 5 Fu。

Objective To compare acute toxicity of two different preparations of 5 flurouracil(5 Fu). Methods Toxic reaction and number of death of mice injected 5 Fu liposome made of Gosylceramide (5 Fu Galcer liposome) and 5 Fu injection intravenously (iv) or intraperitoneally (ip) was observed and median lethal dose (LD 50 ) was calculated. Results LD 50 of 5 FU Galcer liposome and 5 Fu given via iv was 270 1 and 189 6 mg/kg, and its 95% confident interval was 222 0～327 5 and 144 7～247 6 mg/kg. LD 50 of 5 Fu Galcer liposome and 5 Fu injection given via ip was 380 2 and 275 7 mg/kg respectively, and its 95% confident interval was 310 6～461 61 and 213 1～352 5 mg/kg respectively. Conclusion The acute toxicity of 5 Fu Galcer liposome is lower than that of 5 Fu injection.