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Study on preparation process of artesunate polylactic acid microspheres
PAN Xu-wang1， WANG Wei2， FANG Hong-ying1， WANG Fu-gen1， CAI Zhao-bin1*
（1. Preparation Room of Hangzhou Xixi Hospital， Hangzhou ， China；
2. Pharmaceutical Department， Zhejiang Provincial People's Hospital， Hangzhou ， China）
[Abstract] This study aims to investigate the preparation process and in vitro release behavior of artesunate polylactic acid microspheres， in order to prepare an artesunate polylactic acid（PLA） administration method suitable for hepatic arterial embolization. With PLA as the material and polyvinyl alcohol（PVA） as the emulsifier， O/W emulsion/solvent evaporation method was adopted to prepare artesunate polylactic acid microspheres， and optimize the preparation process. With drug loading capacity， encapsulation efficiency and particle size as indexes， a single factor analysis was made on PLA concentration， PVA concentration， drug loading ratio and stirring velocity. Through an orthogonal experiment， the optimal processing conditions were determined as follows： PLA concentration was 9.0%， PVA concentration was 0.9%， drug loading ratio was 1∶2 and stirring velocity was 1 000 r·min-1. According to the verification of the optimal process， microsphere size， drug loading and entrapment rate of artesunate polylactic acid microspheres were （101.7±0.37）μm，（30.8±0.84）%，（53.6±0.62）%， respectively. The results showed that the optimal process was so reasonable and stable that it could lay foundation for further studies.
[Key words] artesunate； polylactic acid microsphere； preparation process； orthogonal design； release in vitro
doi：10.4268/cjcmm