马来酸阿塞那平微球的制备及体外释放研究

摘要

Objective:To prepare asenapine maleate (ASM)-loaded microspheres,and evaluate their in vitro characteristics.Methods:ASM microspheres were prepared by O/W emulsion-solvent evaporation method.The effects of different polymers on microspheres were investigated.Results:ASM microspheres prepared with PLGA 75/25 were spherical and smooth.The particle size was 83.54 μm,the encapsulation efficiency was 86.39％,and the drug loading was 12.19％.The release of ASM was completed at a constant or nearly constant speed within 40 days,and the zero-order release curve was as follows:Y =0.022 63X + 0.111 45,r =0.986 2.Conclusion:ASM microspheres prepared by emulsion-solvent evaporation method PLGA 75/25 can sustainedly release ASM in vitro for 40 days,which may achieve long-term therapeutic effect and improve the bioavailability.%目的:制备马来酸阿塞那平(asenapine maleate,ASM)缓释微球,并对其进行体外评价.方法:采用O/W乳化-溶剂挥发法制备ASM微球,研究不同聚合物材料对微球的影响.结果:以PLGA 75/25作为载体制备的ASM微球,球形完整,表面光滑,其粒径为83.54 μm,包封率为86.39％,载药量为12.19％,可在40 d内均速或接近均速地释放,其零级释放拟合曲线为:Y=0.022 63X +0.111 45,r=0.9862.结论:通过乳化-溶剂挥发法所制备的ASM微球在体外可在40 d内持续缓慢释药,以达到长期治疗效果且提高药物的生物利用度,减少给药次数,提高患者顺应性.