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 ...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.APT011-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 APT011-loaded microspheres were spherical,and the particle size was^90μm 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.APT011-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°C and under high lighting condition.APT011-loaded microspheres prepared in our study exhibited excellent physicochemical properties and sustained-release characteristics and preliminary stability,demonstrating real potential for the clinical practice.展开更多
文摘为确定复杂地质条件煤层群开采矿井合理生产能力,将采煤工作面煤层地质条件开采工艺性综合评价结果与计算机模拟的工作面单产相结合对工作面进行可靠的单产预测,基于工作面预测产量对可能满足矿井生产能力的多种方案进行接续方案的比较分析以得出矿井合理生产能力。以燕家河煤矿5^-1,5^-2和8煤层为研究对象,首先,对矿井未来开采的83个工作面进行开采工艺性综合评价;其次,基于综合评价结果对各工作面进行了可靠的单产预测;再次,提出了2种工作面配置方案并进行工作面接续编排;最后,分析了矿井合理生产能力。研究表明,矿井合理生产能力为180万t/a,产量波动范围为156.5-208.7万t,平均年产量为178.5万t,产量波动系数为0.114,矿井持续稳定开采25 a.
基金National Science&Technology Major Project“Key New Drug Creation and Manufacturing”(Grant No.2019ZX09201001-003-007)。
文摘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.APT011-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 APT011-loaded microspheres were spherical,and the particle size was^90μm 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.APT011-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°C and under high lighting condition.APT011-loaded microspheres prepared in our study exhibited excellent physicochemical properties and sustained-release characteristics and preliminary stability,demonstrating real potential for the clinical practice.
