伏立康唑冻干亚微乳剂的大鼠体内组织分布

Tissue distribution of freeze-dried submicro-emulsion of voriconazole in rats

目的:研究自制伏立康唑亚微乳剂与市售制剂的大鼠静脉给药后的组织分布。方法:制备伏立康唑冻干亚微乳剂,按照36 mg.kg-1的给药剂量大鼠尾静脉给药,考察伏立康唑在预定时间的组织分布情况。HPLC测定大鼠血浆和各组织中伏立康唑的浓度。结果:给予2种伏立康唑制剂后,在0.5,2和8 h时大鼠各组织内药物分布接近。在脂肪、肝、心等组织内的药物浓度偏高,在肌肉、盲肠、子宫等组织内浓度相对较低。结论:大鼠给予伏立康唑亚微乳和注射用伏立康唑后,二者在大鼠体内具有类似的组织分布行为。

Objective：To study the tissue distribution of self-made and marketed freeze-dried submicro-emulsion of voriconazole in rats.Methods：Freeze-dried submicro-emulsion of voriconazole was prepared.The tissue distributions of voriconazole of the self-made and marketed preparations after intravenous administration were investigated at predetermined times at the dose of 36 mg·kg-1.The drug concentrations in plasmas and various tissues in rats were measured by high performance liquid chromatograph（HPLC）.Results：The voriconazole concentrations of the two preparations in various tissues were similar at the time of 0.5,2 and 8 h,respectively.The drug concentrations in fat,liver and heart were relatively higher than the other tissues,while the drug concentrations in muscle,caecum and uterus were lower.Conclusion：The two preparations of voriconazole showed similar tissue distribution profiles in rats after intravenous administration.