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In vitro and in vivo stability of 9-nitrocamptothecin lactone form in rats
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- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 10
- DOI:
- 10.3321/j.issn:0513-4870.2005.10.005
- Key Word:
- 9-硝基喜树碱;内酯型;HPLC;药代动力学;稳定性
Abstract： 目的考察9-硝基喜树碱内酯型在大鼠体内和离体大鼠血浆中的稳定性.方法建立利用HPLC法测定大鼠血浆中9-硝基喜树碱内酯型浓度和总浓度的方法;利用此法测定9-硝基喜树碱在离体大鼠血浆、全血及体内血浆中的内酯型比例变化以及大鼠尾静脉注射后不同时间点的内酯浓度和总浓度;并对体内外实验结果进行比较以确定影响血浆中内酯型稳定性的主要因素.结果9-硝基喜树碱内酯型在大鼠体内的稳定性显著优于体外,在体外全血中的稳定性显著优于血浆.结论血细胞具有稳定9-硝基喜树碱内酯型的作用;药物从血浆中的清除是影响体内大鼠血浆中9-硝基喜树碱内酯型比例的主要因素;9-硝基喜树碱内酯型浓度和总浓度在大鼠体内的药代动力学过程符合二室模型,而羧酸盐型浓度符合一室模型.
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