双烟酸姜黄素酯纳米粒与双烟酸姜黄素酯体内转运动力学特性研究

    Study on the Transport Kinetics Character in Vivo of Double Nicotinate-curcumin Ester Nanoparticles and Nicotinate-curcumin Ester

    • 摘要: 目的 提高双烟酸姜黄素酯的生物利用度,考察双烟酸姜黄素酯是否代谢为姜黄素。方法 以新西兰家兔为试验对象,采用口服给予双烟酸姜黄素酯纳米粒与双烟酸姜黄素酯原料药后,在不同时间点采血,HPLC测定血中双烟酸姜黄素酯、姜黄素等成分含量,计算体内药物转运动力学参数AUC,比较两者的差别。结果 采用统计矩法中的零阶矩法计算AUC,原料药的AUC平均值为(354.835±8.660)μg·L-1·h,而纳米粒的AUC平均值为(883.335±16.37)μg·L-1·h。纳米粒的AUC是原料药AUC的2.486倍。可知纳米粒与原料药相比显著提高了生物利用度;血中未检测到姜黄素。结论 双烟酸姜黄素酯制成纳米粒可显著提高双烟酸姜黄素酯的生物利用度;双烟酸姜黄素酯在体内没有代谢为姜黄素。

       

      Abstract: OBJECTIVE To evaluate bioavailability and whether dual nicotinate-curcumin ester is metabolized to curcumin of this nanoparticles in comparison with dual nicotinate-curcumin ester. METHODS New Zealand rabbits were selected as experiment object, blood samples were collected at different intervals after the dual nicotinate-curcumin ester nanoparticles and dual nicotinate-curcumin ester crude drug was given. The content of dual nicotinate-curcumin ester, curcumin in the blood were detected by HPLC. The AUC of transport kinetics character in vivo was calculated. The difference between nanoparticles and crude drug was compared. RESULTS The AUC was calculated by zeroth moment in the rosenblueth method, the AUC average value of crude drug was (354.835±8.660)μg·L-1·h while the nanoparticles was (883.335±16.37) μg·L-1·h. The value of nanoparticles was 2.486 times of crude drug. It was obvious that bioavailability could be improved by nanoparticles compared to crude drug. Curcumin in the blood were not detected. CONCLUSION The bioavailability of dual nicotinate-curcumin ester crude drug can be improved by made into nanoparticles. Dual nicotinate-curcumin ester is not metabolized to curcumin in vivo.

       

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