摘要
目的:考察难溶性一氧化氮供体药物ZLR-8大鼠在体肠吸收特征及喷雾干燥乳剂对ZLR-8肠吸收的促进作用。方法:采用大鼠在体小肠回流装置,以UV法和HPLC法分别测定酚红和ZLR-8的含量,计算ZLR-8在各肠段的吸收速率常数,考察ZLR-8浓度、肠循环液pH对肠吸收的影响,并对ZLR-8混悬液与ZLR-8喷雾干燥乳剂的肠吸收进行比较。结果:以喷雾干燥乳剂给药,大鼠十二指肠、空肠、回肠、结肠1 h后对ZLR-8的吸收百分率分别为(23.54±1.40)%,(15.95±0.09)%,(12.30±0.74)%,(3.98±0.12)%,吸收速率常数分别为(0.248 6±0.046 0),(0.143 7±0.036 0),(0.069 2±0.001 3),(0.020 8±0.000 4)h-1,各肠段吸收特性有极显著性差异。ZLR-8浓度对吸收速率常数无显著影响,但吸收量与浓度线性相关;肠循环液pH显著影响肠吸收,ZLR-8在pH5.4～7.4时有较好吸收;与混悬液相比,喷雾干燥乳剂极显著性增加大鼠肠吸收。结论:ZLR-8混悬液仅在小肠有微弱吸收,在其他肠段无明显吸收;喷雾干燥乳剂在各肠段均有明显吸收,吸收机制为被动扩散,极显著性地提高了ZLR-8的肠吸收。
Aim:To explore the in situ intestinal absorption in rats of ZLR-8,an insoluble NO-donor drug,and to compare the intestinal absorption enhancement by spray-dried emulsion.Methods:Intestine of rats was cannulated for in situ perfusion.UV and HPLC methods were used to monitor phenolsulfonphthalein and ZLR-8,respectively.The effects on ZLR-8 absorption of the intestinal segments,the concentration of ZLR-8 and the pH of the circulating perfusate were studied.The absorption of ZLR-8 suspension was compared to tha...
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2009年第4期316-320,共5页
Journal of China Pharmaceutical University
基金
国家自然科学基金资助项目(No.30271491)
江苏省自然科学基金资助项目(No.BK2002119)~~
