雷洛昔芬纳米乳的大鼠口服吸收和小鼠组织分布研究

发布时间：2018-11-19 13:56

【摘要】：目的:研究灌胃(ig)给予雷洛昔芬(raloxifene,RAL)混悬剂(suspensions)和纳米乳(nanoemulsion,NE)后,大、小鼠口服吸收及小鼠组织分布特性。方法:大鼠静脉注射(iv)RAL溶液(10 mg·kg~(-1)),大、小鼠ig给予RAL混悬剂和纳米乳(60 mg·kg~(-1)),于给药后不同时间点取得大、小鼠血样及小鼠组织样品,HPLC法测定生物样品中RAL浓度,比较混悬剂和纳米乳ig给药后的口服吸收参数和组织分布特点。结果:口服吸收研究中,与混悬剂组相比,雷洛昔芬纳米乳(RAL-NE)在大、小鼠体内的AUC和Cmax均增大;小鼠组织分布研究中,2种制剂中的RAL在肺中的药物分布较高;脾的AUC和Cmax提高最为明显,而肝的AUC和Cmax2种制剂相比几乎没有差别。结论:与混悬剂相比,RAL-NE可以在一定程度上提高RAL的生物利用度;RAL制成纳米乳后体内靶向性发生了一定的改变,对脾具有明显的靶向性。
[Abstract]:Aim: to study the characteristics of oral absorption and tissue distribution of raloxifene (raloxifene,RAL) suspension (suspensions) and nano-emulsion (nanoemulsion,NE) in rats and mice after oral administration of (ig). Methods: rats were injected intravenously with (iv) RAL solution (10 mg kg~ (-1), ig was given RAL suspension and nano-emulsion (60 mg kg~ (-1),) at different time points after administration), blood samples of mice and tissue samples of mice were obtained. HPLC method was used to determine the concentration of RAL in biological samples. The oral absorption parameters and tissue distribution characteristics of suspension and nano-emulsion ig were compared. Results: in the oral absorption study, compared with the suspension group, the AUC and Cmax in mice were increased, and the distribution of RAL in the lung was higher in the two preparations than in the suspension group. Spleen AUC and Cmax were significantly increased, while liver AUC and Cmax2 preparations were almost no different. Conclusion: compared with suspension, RAL-NE can improve the bioavailability of RAL to a certain extent, and the in vivo targeting of RAL nanoparticles has been changed to a certain extent, which has obvious targeting to spleen.
【作者单位】：广东药科大学
【基金】：国家自然科学基金资助项目(81573353)
【分类号】：R965

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