摘要
目的研究不同密度单唾液酸四己糖神经节苷脂(monosialotetrahexosylganglioside,简称GM1)修饰乳剂比格犬体内药动学。方法制备GM1修饰密度(GM1与卵磷脂的摩尔百分比)为10%、30%和50%乳剂(GM1-CEs),并对GM1实际修饰密度进行测定。考察不同密度GM1修饰乳剂、GM1胶束与普通乳剂混合物(CEs+mGM1)比格犬体内的药动学行为。结果10%、30%和50%GM1修饰乳剂的实际修饰密度分别为7.67%、19.85%和30.01%。10%、30%和50%GM1-CEs的AUC_((0-12 h))分别是普通乳剂的1.46、2.19和2.54倍,其t_(1/2β)分别是普通乳剂的1.17、1.61和2.02倍。CE+10%mGM1、CE+30%mGM1和CE+50%mGM1的AUC_((0-12 h))分别是普通乳剂的1.05、1.10和1.19倍,其t_(1/2β)分别是普通乳剂的1.07、1.10和1.11倍。结论随GM1修饰密度增加,其修饰乳剂的循环时间延长,且未修饰于乳剂表面的GM1胶束溶液并不影响普通乳剂在比格犬体内的药动学行为。
Objective To study the pharmacokintics of emulsions coated with different GM1-surface density in Beagles.Methods 10%,30%,50% GM1-modified emulsions（GM1-CEs） were prepared and the actual GM1 modification density on emulsion surface was determined.The pharmacokintics of 10%,30%,50%GM1-CEs and the mixture of conventional emulsions and GM1 solution（CEs ＋ mGM1） were studied.Results The actual GM1 modification density of 10%,30%,50% GM1 coated emulsions were 7.67%,19.85%and 30.01%.The AUC（（0-12 h）） of 10%,30%,50%GM1-CEs were 1.46,2.19 and 2.54 fold larger than that of conventional emulsions.The t（1/2β） of 10%,30%,50%GM1-CEs were 1.17,1.61 and 2.02 fold lower than that of conventional emulsions.The AUC（（0-12 h）） of CE＋10% mGM1,CE＋30% mGM1,CE＋50%mGM1 were 1.05,1.10 and 1.19 fold larger than that of conventional emulsions.The t（1/2β） of CE ＋10%mGM1,CE ＋ 30% mGM1,CE ＋ 50% mGM1 were 1.07,1.10 and 1.11 fold lower than that of conventional emulsions.Conclusions The circulation times of GM1-modified emulsions prolong with the increase of GM1-surface density and unmodified GM1 micelles do not affect the pharmacokinetics of conventional emulsions in Beagle.
出处
《沈阳药科大学学报》
CAS
CSCD
北大核心
2017年第4期338-344,共7页
Journal of Shenyang Pharmaceutical University
基金
国家自然科学基金资助项目(81373334)
