摘要
合成了不同重均分子质量(M_w)的聚乙二醇-聚丙交酯嵌段共聚物,用以制备紫杉醇聚合物胶束。采用一种基于透析适配器的流通池法,检测所得胶束的体外释放行为,并考察透析膜的种类和截留分子量(MWCO)、流通池流速、样品池中玻璃珠用量、胶束样品浓度对体外释放结果的影响,同时用所建立的方法检测自制紫杉醇胶束、市售注射液和脂质体的体外释放行为。结果显示,透析膜的种类和MWCO对胶束的体外释放具有一定影响;不同流速以及玻璃珠不同用量对释放度测定结果影响不大;但样品浓度对检测结果有显著影响。采用本法检测时,不同剂型紫杉醇的体外释放行为具有明显区别;而不同M_w聚合物制得胶束的体外释放行为只在释放初期具有微小差异。
The poly(ethylene glycol)-poly(DL-lactide) block copolymers with different of molecular weight(M_w) values were synthesized to prepare the paclitaxel polymeric micelles.A flow-through cell method based on dialysis adapter for in vitro release testing of paclitaxel polymeric micelles was established,and the influences of type and molecular weight cut-off(MWCO) of dialysis membrane,flow rate of flow through cell,amount of glass beads placed in cell and sample concentration on in vitro release behavior of paclitaxel from the prepared micelles were investigated.Moreover,this method was adopted to testing the release of paclitaxel-loaded preparations,namely the self-made micelles and the commercial injection and liposomes.The results showed that the type and MWCO of the dialysis membrane had a certain effect on the in vitro release of the micelles;both flow rate and amount of glass beads had little effect on the release results;but the sample concentration had a significant effect on the test results.The release behaviors of different dosage forms of paclitaxel tested by this method were quite different,while there were only slight differences among the micelles with different M_W polymers in the early stage of release.
作者
尚萍萍
郝贵周
郑华
陈小伟
张贵民
SHANG Pingping;HAO Guizhou;ZHENG Hua;CHEN Xiaowei;ZHANG Guimin(Shandong Engineering Research Center of Complex Injectables,Shandong Newtime Pharmaceutical Co.,Ltd.,Linyi 273400)
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2020年第9期1172-1177,共6页
Chinese Journal of Pharmaceuticals
基金
山东省重大科技创新工程——注射用紫杉醇聚合物胶束的研制(2018CXGC1408)。
关键词
体外释放
透析适配器
紫杉醇
聚合物胶束
流通池法
in vitro release
dialysis adapter
paclitaxel
polymeric micelle
flow-through cell method
