聚乙二醇400介导的多西他赛脂肪乳剂与多西他赛注射液的稀释稳定性研究  

Stability comparison between a novel polyethylene glycol mediated lipid nanoemulsion of docetaxel and docetaxel injection saline dilutions

作　　者：张广军[1] 林玲 陈丽娜[1] 高保安[1,2] 陈建明[1,2] 

机构地区：[1]第二军医大学药剂学教研室,上海200433 [2]天士力帝益药业有限公司,江苏淮安223002

出　　处：《药学实践杂志》2015年第2期119-121,175,共4页Journal of Pharmaceutical Practice

基　　金：上海市纳米专项(12nm0501000)

摘　　要：目的建立多西他赛的含量测定方法;考察自制的聚乙二醇（PEG）400介导的多西他赛脂肪乳剂与市售的多西他赛注射液稀释液的稳定性。方法建立高效液相色谱法测定含量;在室温条件下采用膜过滤法,以过滤液的含量、pH值以及过滤前的粒径为指标,考察PEG400介导的多西他赛脂肪乳剂与市售的多西他赛注射液的稀释液随时间变化的稳定性。结果多西他赛在1~256μg/ml的浓度范围内线性关系良好,回归方程：Y=21.199 X＋20.488,r=0.999 9;自制PEG400介导的多西他赛脂肪乳剂分散液,室温下24h内过滤液的含量、pH值以及过滤前的粒径均未见明显变化。观察市售多西他赛注射液的生理盐水稀释液,2h发现有药物析出,过滤液含量明显下降。结论自制PEG400介导的多西他赛脂肪乳剂的分散稳定性远优于市售多西他赛注射液的生理盐水稀释液,大大提高了临床用药的安全性。Objective To establish HPLC method to detect docetaxel and compare the stability of a novel polyethylene glycol mediated lipid nanoemulsion of docetaxel with docetaxel injection saline dilutions .Methods HPLC method was estab‐lished to detect docetaxel concentration .The stability of a novel polyethylene glycol mediated lipid nanoemulsion of docetaxel and docetaxel saline dilutions were investigated by drug concentration pH value and particle size using membranes filtration method .Results The linear range of docetaxel was 1‐256 μg/ml ,regression equation was Y=21 .199X＋20 .488 ,r=0 .999 9 . The drug concentration pH value and particle size of polyethylene glycol mediated lipid nanoemulsion of docetaxel was stable at room temperature in 24 hours .However the docetaxel injection saline dilutions was discovered drug precipitation in about two hours after preparation and the drug concentration was significant decreased in the filtration of docetaxel injection saline dilu‐tions .Conclusion The novel polyethylene glycol mediated lipid nanoemulsion of docetaxel was a new stable docetaxel formula‐tion and significantly increased the safety in clinical .

关 键 词：聚乙二醇400 多西他赛脂肪乳剂 多西他赛注射液 稀释稳定性 

分 类 号：R944.1[医药卫生—药剂学]