【摘要】：目的研究不同密度單唾液酸四己糖神經(jīng)節(jié)苷脂(monosialotetrahexosylganglioside,簡稱GM1)修飾乳劑比格犬體內(nèi)藥動(dòng)學(xué)。方法制備GM1修飾密度(GM1與卵磷脂的摩爾百分比)為10%、30%和50%乳劑(GM1-CEs),并對GM1實(shí)際修飾密度進(jìn)行測定�？疾觳煌芏菺M1修飾乳劑、GM1膠束與普通乳劑混合物(CEs+mGM1)比格犬體內(nèi)的藥動(dòng)學(xué)行為。結(jié)果10%、30%和50%GM1修飾乳劑的實(shí)際修飾密度分別為7.67%、19.85%和30.01%。10%、30%和50%GM1-CEs的AUC_((0-12 h))分別是普通乳劑的1.46、2.19和2.54倍,其t_(1/2β)分別是普通乳劑的1.17、1.61和2.02倍。CE+10%mGM1、CE+30%mGM1和CE+50%mGM1的AUC_((0-12 h))分別是普通乳劑的1.05、1.10和1.19倍,其t_(1/2β)分別是普通乳劑的1.07、1.10和1.11倍。結(jié)論隨GM1修飾密度增加,其修飾乳劑的循環(huán)時(shí)間延長,且未修飾于乳劑表面的GM1膠束溶液并不影響普通乳劑在比格犬體內(nèi)的藥動(dòng)學(xué)行為。
[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.
【作者單位】： 沈陽藥科大學(xué)藥學(xué)院;
【基金】：國家自然科學(xué)基金資助項(xiàng)目(81373334)
【分類號(hào)】：R965

【參考文獻(xiàn)】

相關(guān)期刊論文 前1條

1 何丹;楊林;張景R，

本文編號(hào)：2404897