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| 9-硝基喜树碱在大鼠组织中的分布及内酯稳定性 | |
| 引用本文： | 陈军,平其能,杨希雄,蔡宝昌.9-硝基喜树碱在大鼠组织中的分布及内酯稳定性[J].中国医药工业杂志,2009,40(8). |
| 作者姓名： | 陈军 平其能 杨希雄 蔡宝昌 |
| 作者单位： | 1. 南京中医药大学药学院,江苏南京,210029;中国药科大学药学院,江苏南京,210009 2. 中国药科大学药学院,江苏南京,210009 3. 荆楚理工学院化工与药学院,湖北荆门,448000 4. 南京中医药大学药学院,江苏南京,210029 |
| 摘 要： | 考察9-硝基喜树碱(9-NC)静脉注射后在人鼠组织中的分布及内酯稳定性.建立了HPLC法间时测定组织和血浆中9-NC内酯浓度和总浓度.大鼠静脉注射9-NC溶液后测定各时间点组织中内酯浓度、总浓度和内酯比例.大多数组织中的9-NC内酯比例明显高于血浆;肝中的内酯比例最低,甚至低于血浆;血浆、肾和小肠中的内酯比例随时问延长而下降.9-NC在肝以外的组织中内酯稳定性显著优于血浆. |
| 关 键 词： | 9-硝基喜树碱 组织分布 内酯 稳定性 |
Tissue Distribution and Lactone Stability of 9-Nitrocamptothecin in Rats |
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| Authors: | CHEN Jun PING Qineng YANG Xixiong CAI Baochang |
| Abstract: | The tissue distribution and lactone stability of 9-nitrocamptothecin (9-NC) were investigated following intravenous administration of 9-NC solution to rats. The validated HPLC method was developed for determination of 9-NC lactone form (lactone 9-NC) and the total of lactone and carboxylate forms (total 9-NC) in rat tissue and plasma simultaneously. After iv administration of 9-NC solution, the concentrations of lactone and total 9-NC in rat tissues and plasma were measured. Then the lactone percentages, and the index of lactone stability were calculated. It was found that lactone 9-NC was unstable in liver and lactone percentage was even lower than that in plasma. In other tissues, however, lactone 9-NC was more stable and lactone percentages were almost all higher than that in plasma. In addition, the lactone percentage in plasma, kidney and small intestine decreased with time. Lactone 9-NC was more stable in tissues except liver than in plasma. |
| Keywords: | 9-nitrocamptothecin tissue distribution lactone stability |
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