CAJ | 학술논문

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.
고찰9-초기희수감(9-NC)정맥주사후재인서조직중적분포급내지은정성.건립료HPLC법간시측정조직화혈장중9-NC내지농도화총농도.대서정맥주사9-NC용액후측정각시간점조직중내지농도、총농도화내지비례.대다수조직중적9-NC내지비례명현고우혈장;간중적내지비례최저,심지저우혈장;혈장、신화소장중적내지비례수시문연장이하강.9-NC재간이외적조직중내지은정성현저우우혈장.
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.