【作者】 张丽锋； 葛睿； 平耀东； 李青山；

【Author】 ZHANG Li-feng, GE Rui, PING Yao-dong, LI Qing-shan*(School of Pharmaceutical Science, Shanxi Medical University, Taiyuan 030001)

【机构】 山西医科大学药学院；

【摘要】 目的:制备呋喃二烯W/O/W型复乳,并进行体内外评价,为呋喃二烯的制剂设计提供研究基础。方法:采用二次乳化法制备呋喃二烯复乳,对处方进行筛选。复乳中呋喃二烯的含量、大鼠体内药物动力学特征及小鼠体内的分布均采用反相高效液相色谱法测定。结果:显微镜下观察,制得的复乳为W/O/W型,标示含量为99%±2.1%。大鼠体内的药动学呈单室模型,k=0.3468±0.0532h-1,t1/2=1.99±0.15h,Vd=1.97±0.52L;在小鼠体内分布广泛,其中心、肝、脾分布较多,脑内也有分布;结论:制得的复乳稳定性好,乳滴均匀,适合于注射给药;测定方法操作简便、准确、灵敏度高,可用于该制剂的体内外质量控制。更多还原

【Abstract】 Objective: To prepare furanodiene multiple emulsions, and evaluate the quality in vitro / vivo. Methods: Furanodiene multiple emulsions were prepared by two-step emulsification. The prescription of prime emulsions was optimized. The content of furanodiene multiple emulsions, pharmacokinetics in rats, distribution in mice were determined by RP-HPLC. Results: The type of furanodiene multiple emulsions observed by microscope, were W/O/W. Pharmacokinetics in rats was single compartment model, k=0.3468±0.0532 h-1,t1/2=1.99±0.15 h,Vd=1.97±0.52 L; Distribution in mice was wide,especially in heart, liver and spleen, also in brain. Conclusion: Furanodiene multiple emulsions were stable, and were suitable for injection; HPLC method is simple, accurate, high sensitive and can be used for the preparation of quality control in vitro/vivo.更多还原