磷霉素钙原料药及杂质的细胞毒性考察  

Cytotoxicity of Fosfomycin Calcium Raw Material and its Impurity

作　　者：陶磊 徐静 曹玉 戴震 马志 Tao Lei;Xu Jing;Cao Yu;Dai Zhen;Ma Zhi(Nanjing Institute for Food and Drug Control,Nanjing 211198,China)

机构地区：[1]南京市食品药品监督检验院,南京211198

出　　处：《中国药师》2021年第8期590-593,共4页China Pharmacist

摘　　要：目的:考察磷霉素钙原料药及主要杂质的细胞毒性。方法:不同浓度的磷霉素钙原料药及主要杂质作用于人源肝脏细胞(L02)以及肠上皮细胞(Ncm460)一定时间后,计算相对增殖率(RGR)并记录细胞形态的变化。结果:磷霉素钙原料药(4 mmol·L^(-1))对L02和Ncm460细胞的RGR分别为54.5%和60.9%;杂质A对细胞的RGR分别为101.8%和94.7%。光镜结果显示,给予磷霉素钙原料药作用一定时间后,L02和Ncm460细胞出现不同程度的变圆、浮起、胞膜皱缩等形态学改变;且随着药物作用时间的延长,形态变化进一步加剧。然而,给予相同浓度的杂质A处理后,细胞的生长速度和形态均未发生明显的改变。结论:与原料药相比,同等浓度条件下杂质A对两种细胞均表现为极轻或无细胞毒作用。Objective:To evaluate the cytotoxicity of fosfomycin calcium raw material and its impurity.Methods:The relative proliferation rate(RGR)of human liver cells(L02)and human intestinal epithelial cells(Ncm460)were calculated and cell morphology were recorded after treated with different concentrations of fosfomycin calcium raw material and its main impurity.Results:The RGR of fosfomycin calcium raw material(4 mmol·L^(-1))on L02 and Ncm460 cells was 54.5%and 60.9%,respectively,and the RGR of impurity A on L02 and Ncm460 cells was 101.8%and 94.7%,respectively.The results of morphology under a light microscope showed that L02 and Ncm460 cells had different morphologic changes,such as rounded,floating and membrane shrinkage after treated with calcium fosfomycin raw material for a certain time.With the prolongation of drug action time,the morphological changes were further intensified.However,the growth rate and morphology of cells did not change significantly after treated with the same concentration of impurity A.Conclusion:Compared with fosfomycin calcium raw material at the same concentration,impurity A shows extremely mild or no cytotoxic effect on both types of cells.

关 键 词：磷霉素钙 杂质A 细胞毒性 

分 类 号：R965.3[医药卫生—药理学]