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目的:制备可实现持续多巴胺能刺激治疗帕金森病的罗替戈汀缓释微球,并进行体内外评价。方法:采用O/W乳化溶剂挥发法制备微球,并对其包封率、粒径、体外释放、体内药动学等进行了考察。结果:不同高分子及组合制备的罗替戈汀微球释药特性有明显差别,采用最优处方制备的罗替戈汀微球载药量为27.0%,包封率为90.2%,平均粒径为71.5μm,扫描电镜观察结果显示,微球表面光滑圆整,体外可持续缓慢释放14 d,体内药动学结果表明,罗替戈汀微球具有明显的缓释特征,血浆浓度在给药后96 h达峰,C max为(6.27±1.32)ng·mL-1,可以检测到给药后14 d。结论:所制备的罗替戈汀微球体内可持续缓慢释药达2周,达到了预期目的。
OBJECTIVE: To prepare sustained-release microspheres of rotigotine for sustained dopaminergic stimulation of Parkinson’s disease and to evaluate in vitro and in vivo. Methods: Microspheres were prepared by O / W emulsification solvent evaporation method. The entrapment efficiency, particle size, in vitro release and pharmacokinetics were investigated. Results: The drug release characteristics of the rotigotine microspheres prepared by different polymers and combinations were significantly different. The optimal loading volume of rotigotine microspheres was 27.0%, encapsulation efficiency was 90.2%, average particle size Diameter of 71.5μm, scanning electron microscopy showed that the microspheres smooth and round surface, sustained and sustained sustained release in vitro 14 d, pharmacokinetic results show that the rotigotine microspheres with sustained release characteristics of the plasma concentration in 96 h after drug peak, C max (6.27 ± 1.32) ng · mL-1, can be detected after 14 d. Conclusion: The sustained-release sustained release drug of Rotigotine microspheres for up to 2 weeks, the desired purpose.