川陈皮素自微乳的制备及其大鼠在体肠吸收动力学  被引量:28

Preparation of nobiletin-loaded self-microemulsifying system and its absorption kinetics in rat intestines

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作  者:姚静[1] 卢韵[1] 周建平[1] 平其能[1] 

机构地区:[1]中国药科大学药剂学教研室,南京210009

出  处:《中国药科大学学报》2007年第1期35-38,共4页Journal of China Pharmaceutical University

摘  要:目的:制备川陈皮素自微乳制剂,以期提高其口服生物利用度,并研究其在大鼠小肠各部位的吸收情况。方法:测定川陈皮素自微乳的粒径、Zeta电位等理化参数,初步考察其稳定性;运用大鼠在体肠回流模型,采用HPLC法测定回流液中药物的浓度,考察药物的吸收。结果:制得的川陈皮素自微乳平均粒径为(17.9±1.5)nm,Zeta电位为-4.9mV,稳定性好。川陈皮素微乳在空肠的吸收速率最快,吸收速率常数Ka为(0.5298±0.0507)h-1;川陈皮素胶束在空肠段的吸收显著低于微乳组(P<0.05)。结论:川陈皮素自微乳制剂稳定,微乳对川陈皮素在大鼠小肠的吸收有明显的促进作用。Aim:To improve the oral bioavailability of the nobiletin, the nobiletin-loaded self-microemulsifying system was prepared and the absorption of nobiletin-loaded microemulsion in rat intestine was investigated in comparison with that of nobiletin-loaded micelle. Methods: The size, Zeta potential and stability of nobiletin-loaded selfmicroemulsifying system were investigated. In situ recirculation model was used and the concentration of nobiletin in the perfusate were determined by HPLC. Results:The particle size of the resulting microemulsion was( 17.9 ± 1.5)nm with Zeta potential of- 4.9 mV. The nobiletin-loaded self-mieroemulsifying system was stable in 6 months stored at ambient. Compared with other segments,the absorption rate constant( Ka)of(0.529 8± 0.050 7)h and the absorption percentage of nobiletin-loaded microemulsion at the jejunum were the largest. The absorption of nobiletin-loaded micelle at the jejunum was significantly lower than that of nobiletin-loaded microemulsion. Conclusion:The nobiletinloaded self-microemulsifying system is stable and might significantly improve the absorption of nobiletin in the intestinal tract.

关 键 词:川陈皮素 自微乳 在体肠回流模型 肠吸收 

分 类 号:R285[医药卫生—中药学]

 

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