马来酸阿塞那平微球的制备及体外释放研究

Preparation and in vitro release of asenapine maleate-loaded microspheres

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83.54μm,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=0.986 2。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。

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 corn speed within 40 days, and the zero-order release curve was as follows： Y = Conclusion ： release ASM ASM micro in vitro for sph 40 eres prepared by emulsion-solvent evaporation pleted at a consta 0. 022 63X ＋ 0. 1 method PLGA 75 nearly constant 5,r=0.9862. can sustainedly nt or 114 /25 days, which may achieve long-term therapeutic effect and improve the bioavailability