去甲基斑蝥素纳米粒大鼠体肠吸收动力学研究

摘要

目的:考察去甲基斑蝥素(NCTD)及其壳聚糖纳米粒(NCTD-CS-NP)制剂的大鼠在体吸收特征与相关动力学。方法:采用大鼠在体回流试验,并用紫外分光光度法和HPLC分别测定酚红和NCTD的质量浓度;并采用在体循环法比较不同质量浓度NCTD及NCTD-CS-NP在大鼠小肠区段内的吸收规律。结果:NCTD在十二指肠、空肠、回肠、结肠的吸收速率常数(ka)分别为:0.0306,0.0278,0.0151,0.0044h-1,NCTD-CS-NP在对应肠段的ka分别为:0.0689,0.0592,0.0353,0.0095h-1;质量浓度分别为140,160,180μg/mL的NCTD小肠ka分别为:0.0499,0.0525,0.0489h-1;对应质量浓度的NCTD-CS-NPka分别为:0.0814,0.0764,0.0734h-1。结论:NCTD的质量浓度对其大鼠全肠道的吸收无显著影响,吸收呈一级动力学过程,且以肠道中上部的吸收为主,NCTD-CS-NP可有效促进药物在肠粘膜的吸收。