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目的 本实验使用丝裂霉素 C-右旋糖酐交联物(MMC- D) ,证实其可通过改变丝裂霉素 C药代动力学特性 ,使药物宜于聚集在淋巴系统和局部用药部位。方法 将MMC- D注入到 Wistar大鼠左大腿肌肉内 ,与 MMC作对照 ,分析其药代动力学特性及淋巴组织趋向性。组织及血浆中的丝裂霉素浓度用生物检测法测定。结果 MMC- D肌注后 ,2 4h后仍有 33.5 %以结合方式存在于注射部位 ,而MMC肌注后 30 m in内消失。 MMC- D于引流的腹腔淋巴结中 2 h浓度达 185 .2 μg/ g,2 4h浓度仍为 5 5 .6 μg/ g。 MMC于淋巴结内 5 min浓度达高峰 2 3.1μg/ g,30 min内消失。MMC- D肌注后于大鼠血中测不到药物浓度 ,提示 MMC- D吸收后主要分布到血液以外的组织器官中 ,可减轻因 MMC高血浓度而产生的严重副作用。结论 本实验显示 ,MMC-D有淋巴组织分布多 ,释放缓慢 ,维持作用时间长 ,可能消除淋巴组织中的微小转移灶 ,为预防和治疗恶性肿瘤淋巴转移开辟一个新的途径
Purpose This experiment used mitomycin C-dextran cross-linkers (MMC-D), confirming that it can be adapted to the lymphatic system and topical drug sites by altering the pharmacokinetics of mitomycin C. Methods MMC-D was injected into the left thigh muscle of Wistar rats and compared with MMC to analyze its pharmacokinetics and lymphoid tissue tropism. Mitomycin concentrations in tissues and plasma were determined by bioassay. Results After MMC-D intramuscular injection, 33.5% of the MMC-D still existed at the injection site after 24 hours, while MMC disappeared within 30 minutes after intramuscular injection. The concentration of MMC-D in draining peritoneal lymph nodes reached 185.2 μg / g for 2 h and was 55.6 μg / g for 24 h. MMC in the lymph node concentration reached 5 min peak 2 3.1μg / g, disappeared within 30 min. MMC-D intramuscular injection of blood can not be measured after the drug concentration, suggesting that MMC-D absorbed mainly distributed to tissues and organs other than blood, can reduce the serious side effects caused by high blood concentration of MMC. Conclusions This study shows that MMC-D has more lymphoid tissue distribution, slow release and longer duration of maintenance, which may eliminate micrometastases in lymphoid tissues and open up a new way for the prevention and treatment of lymphatic metastasis of malignant tumors