[关键词]
[摘要]
目的 考察吴茱萸-姜黄素碱纳米粒(evodiamine-curcumin nanoparticles,ECNP)在大鼠体内的药动学特征,探讨姜黄素(CUR)对吴茱萸碱(EVO)生物利用度的影响。方法 采用溶剂挥发法制备ECNP,大鼠分别ig给予ECNP、吴茱萸碱姜黄素混合物(MEC)、EVO后,在不同时间点于眼底静脉采血,采用HPLC法测定血浆中EVO的质量浓度。结果 ECNP、MEC和游离EVO组EVO的AUC0~t分别为(3 197.74±81.64)、(1 387.73±39.42)、(928.08±54.84)μg·h/L。其中,MEC组的AUC0~t为游离EVO组的1.50倍;ECNP组的AUC0~t分别为游离EVO组和MEC组的3.45倍和2.30倍。结论 CUR与EVO配伍能促进EVO的口服吸收,制备成纳米粒制剂后进一步提高EVO在大鼠体内的口服生物利用度。
[Key word]
[Abstract]
Objective To investigate the in vivo pharmacokinetic characteristics of evodiamine-curcumin nanoparticles (ECNP), and to discuss the influence of curcumin (CUR) to the bioavailability of evodiamine (EVO). Methods ECNP were prepared by solvent evaporation method. Rats were orally given ECNP. After administration, blood samples were collected from the retinal venous plexus of SD rats at different time points. And the blood concentration of EVO was determined by HPLC. Results The AUC0-t of ECNP, mixture of evodiamine and curcumin (MEC) and free EVO were (3 197.74 ± 81.64) μg·h/L, (1 387.73 ± 39.42) μg·h/L, and (928.08 ± 54.84) μg·h/L, respectively. The AUC0-t of MEC was 1.50 times as free EVO. The AUC0-t of ECNP was 3.45 and 2.30 times as EVO and MEC, respectively. Conclusion The absorption of EVO in rats was promoted with CUR, and nanoparticles can further improve the oral bioavailability of EVO in rats.
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[基金项目]
重庆市科委资助项目(csct2015jcyjBX0027)