不同密度单唾液酸四己糖神经节苷脂修饰乳剂比格犬体内药动学
发布时间:2019-01-08 17:15
【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。
[Abstract]:Objective to study the pharmacokinetics of monosialate tetrahexose ganglioside (monosialotetrahexosylganglioside, GM1) modified emulsion in Beagle dogs. Methods the modified density of GM1 (the molar ratio of GM1 to lecithin) was 10% and 50% (GM1-CEs), and the actual modified density of GM1 was determined. The pharmacokinetic behavior of GM1 modified emulsion, GM1 micelle and ordinary emulsion mixture (CEs mGM1) in Beagle dogs with different densities was investigated. Results the actual modification densities of 1030% and 50%GM1 modified emulsions were 7.6719.85% and 30.01.10, respectively. The AUC_ of 30% and 50%GM1-CEs (0-12 h) were 1.46% and 2.54 times as much as that of the ordinary emulsion, respectively, and the t _ (1 / 2 尾) of 30% and 50%GM1-CEs were 1.17 ~ 1.61 and 2.02 times as much as those of the ordinary emulsion, respectively. The AUC_ (0-12 h) of CE 30%mGM1 and CE 50%mGM1 were 1.05 ~ 1.10 and 1.19 times as much as those of ordinary emulsion, respectively, and their t _ (1 / 2 尾) were 1.07 ~ 1.10 and 1.11 times as much as that of ordinary emulsion, respectively. Conclusion with the increase of GM1 modification density, the cycle time of the modified emulsion is prolonged, and the pharmacokinetic behavior of the ordinary emulsion in Beagle dog is not affected by the GM1 micelle solution which is not modified on the surface of the emulsion.
【作者单位】: 沈阳药科大学药学院;
【基金】:国家自然科学基金资助项目(81373334)
【分类号】:R965
[Abstract]:Objective to study the pharmacokinetics of monosialate tetrahexose ganglioside (monosialotetrahexosylganglioside, GM1) modified emulsion in Beagle dogs. Methods the modified density of GM1 (the molar ratio of GM1 to lecithin) was 10% and 50% (GM1-CEs), and the actual modified density of GM1 was determined. The pharmacokinetic behavior of GM1 modified emulsion, GM1 micelle and ordinary emulsion mixture (CEs mGM1) in Beagle dogs with different densities was investigated. Results the actual modification densities of 1030% and 50%GM1 modified emulsions were 7.6719.85% and 30.01.10, respectively. The AUC_ of 30% and 50%GM1-CEs (0-12 h) were 1.46% and 2.54 times as much as that of the ordinary emulsion, respectively, and the t _ (1 / 2 尾) of 30% and 50%GM1-CEs were 1.17 ~ 1.61 and 2.02 times as much as those of the ordinary emulsion, respectively. The AUC_ (0-12 h) of CE 30%mGM1 and CE 50%mGM1 were 1.05 ~ 1.10 and 1.19 times as much as those of ordinary emulsion, respectively, and their t _ (1 / 2 尾) were 1.07 ~ 1.10 and 1.11 times as much as that of ordinary emulsion, respectively. Conclusion with the increase of GM1 modification density, the cycle time of the modified emulsion is prolonged, and the pharmacokinetic behavior of the ordinary emulsion in Beagle dog is not affected by the GM1 micelle solution which is not modified on the surface of the emulsion.
【作者单位】: 沈阳药科大学药学院;
【基金】:国家自然科学基金资助项目(81373334)
【分类号】:R965
【参考文献】
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1 何丹;杨林;张景R,
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