张雅雯,尹丽娜,黄夏樱,梁泽华,陈晓晓,王胜浩
ZHANG Ya-wen,YIN Li-na,HUANG Xia-ying,LIANG Ze-hua,CHEN Xiao-xiao,WANG Sheng-hao

• 1:浙江省医学科学院
• 2:浙江中医药大学药学院

摘要(Abstract)：

采用溶剂扩散法制备聚乙二醇修饰的积雪草酸(asiatic acid,AA)纳米结构脂质载体(pegylated asiatic acid loaded nanostructured lipid carriers,p-AA-NLC),以结扎肠循环模型考察其在小肠的吸收分布情况,HPLC检测健康SD大鼠灌胃给予p-AA-NLC后的胆汁药物浓度,间接评价PEG化脂质纳米粒的促口服吸收作用。结果显示,经PEG亲水性修饰的NLC在小肠黏膜的穿透能力大大提高,小肠内的转运量显著增加,大鼠体内药物排泄峰值Cmax较普通纳米粒(asiatic acid loaded nanostructured lipid carriers,AA-NLC)提高了76%,达峰时间tmax减慢,消除半衰期t1/2延长1倍,AUC0→t为AA-NLC组的1.5倍,提示AA-NLC经PEG亲水性修饰后,口服生物利用度显著提高。
A solvent diffusion method was used to prepare pegylated asiatic acid( AA) loaded nanostructured lipid carriers( p-AANLC),and the ligated intestinal circulation model was established to observe the absorption and distribution in small intestine. The concentration of AA in bile after oral administration of p-AA-NLC was detected by HPLC in healthy SD rats to indirectly evaluate the oral absorption promoting effect of PEG-modified namoparticles. The results showed that the penetration of p-AA-NLC was enhanced significantly and the transport capacity was increased greatly in small intestinal after PEG modification. As compared with the normal nanoparticles( AA-NLC),the Cmaxof the drug excretion was increased by 76%,the time to reach the peak( t_(max)) was decreased and the elimination half-life t_(1/2) was doubled in the rats after oral administration of p-AA-NLC,and the AUC_(0→t) was 1. 5 times of the AANLC group,indicating that the oral bioavailability of AA-NLC was significantly improved by hydrophilic modification of PEG.

关键词(KeyWords)： 积雪草酸;纳米结构脂质载体;聚乙二醇;口服吸收
asiatic acid;nanostructured lipid carrier;PEG;oral absorption

Abstract:

Keywords:

基金项目(Foundation):

作者(Author): 张雅雯,尹丽娜,黄夏樱,梁泽华,陈晓晓,王胜浩
ZHANG Ya-wen,YIN Li-na,HUANG Xia-ying,LIANG Ze-hua,CHEN Xiao-xiao,WANG Sheng-hao

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