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本研究目的在于制备新的神经激肽-1受体拮抗剂—APT011缓释注射微球,并对其理化性质、体外释放及初步稳定性进行评价.首先采用W/O/W复乳溶剂挥发法制备载药微球,并用正交设计实验优化处方工艺.显微观察结果显示该载药微球为球形,圆整度好;平均粒径为90 μm,粒径分布均匀;粉末X-衍射结果表明APT011在微球内部以无定型形式存在;DSC结果表明药物APT011与空白微球无明显相互作用.此外,载APT011微球具有明显的缓释效果,可持续释放2个月.初步稳定性结果表明在40℃和光照条件下,微球的载药量与突释效应没有明显改变.上述结果说明,载APT011微球具有优良的理化性质、缓释特性和初步稳定性,具有进入临床的潜力.“,”In the present study,we aimed to prepare sustained-release microspheres for injection of neurokinin-1 (NK-1) receptor antagonist APT011,and to evaluate their physicochemical properties,in vitro sustained-release effect and preliminary stability.APT01 1-loaded sustained-release microspheres were prepared using W/O/W double emulsion-solvent evaporation technique.The L9 (34) orthogonal experiment was used to optimize the APT011 sustained-release microsphere formulation.Microscope photographs showed that APT01 1-loaded microspheres were spherical,and the particle size was ～90 μm with uniform size distribution.XRD results indicated that APT011 existed in the microspheres in an amorphous form.DSC results showed that there was no significant interaction between APT011 and blank microspheres.APT01 1-loaded microspheres had a significant sustained-release effect,which maintained release for at least 2 months.Preliminary study results indicated that the loading content and release percentage at 0.5 h were not markedly altered below 40 ℃ and under high lighting condition.APT01 1-loaded microspheres prepared in our study exhibited excellent physicochemical properties and sustained-release characteristics and preliminary stability,demonstrating real potential for the clinical practice.