吡喹酮缓释植入剂的研制

目的以两种不同分子量的聚(乳酸-羟基乙酸)为载体,采用熔融挤出法制备吡喹酮缓释植入剂。方法采用GPC和DSC分别考察了挤出前后载体的分子量、分子量分布及热性能变化,检测了植入剂的含量均匀度及体外释放度。结果挤出后载体的分子量降低,分子量分布变窄,Tg略有下降;植入剂的平均含量为98.72%,RSD值为0.88%,含量均匀度符合药典要求;0～15 d内体外日释放量平缓上升,15～24 d内出现暴释现象,24 d时,累积释放度达100%。结论熔融挤出法制备吡喹酮-PLGA缓释植入剂可行,所制植入剂起到了缓释的作用,缓药期达24 d。

Study on release implant of praziquantel

Objective To prepare the release implants of praziquantel by melt extrusion using PLGA with two kinds of different molecular weight as a carrier.Methods The changes of molecular weight,molecular weight distribution and thermal properties of the carrier before and after extrusion were investigated by GPC and DSC,respectively.The determination and in vitro release rate of implants were also tested by HPLC.Results The molecular weight and Tg of carrier was decreased,and the molecular weight distribution was narrowed after extrusion.The average content of implants was 98.72%,and RSD was 0.88%.The content uniformity of implants conformed to the standard of Chinese Pharmacopoeia.In vitro daily release of the implants reposefully increased in 0 ～ 15 days,however,a burst release occurred in 15 ～ 24 days.The cumulative release rate arrived 100% at 24th day.Conclusion The hot-melting extrusion method was feasible to prepare praziqantel-PLGA implants,and the implants can release to 24 days.