氟尿嘧啶直肠给药与注射给药后体内组织分布比较

Comparison of Distribution in Tissues between Rectal and Injecting Administration of Fluorouracil

目的比较氟尿嘧啶(5-Fu)通过直肠用药和全身用药后在局部和全身的分布情况。方法将16例直肠癌需行手术的患者随机平均分为两组,其中一组术前1 h经直肠给予5-Fu栓400 mg,另一组术前1 h给予5-Fu400 mg静脉滴注,术中(距离给5-Fu约2 h)留取患者直肠癌组织和癌变部位上下正常组织,采用高效液相色谱法测定直肠癌组织、直肠癌上下肠壁肌肉及其引流区淋巴结和外周血液中5-Fu浓度。结果患者给予5-Fu栓后2 h癌组织中5-Fu浓度为21.68μg.-g1,上、下直肠壁肌肉中5-Fu浓度分别为13.57和15.41μg.g-1,引流区淋巴结5-Fu浓度为2.14μg.-g1,外周血液5-Fu浓度为0.068μg.g-1;静脉滴注5-Fu后2 h直肠癌组织中5-Fu浓度为4.57μg.g-1,上、下直肠壁肌肉中5-Fu浓度分别为0.074和0.064μg.g-1,引流区淋巴结5-Fu浓度为1.69μg.g-1,外周血中5-Fu浓度为0.025μg.-g1。结论直肠癌患者经直肠给予5-Fu栓剂后,局部癌组织及癌变周围组织中药物浓度较静脉滴注给予5-Fu明显提高,可更加有效地预防癌细胞在手术中的种植与转移,同时可有效降低化疗的不良反应。

Objective To study the distribution in tissues between rectal and systemic injection of 5-fluorouracil in human beings. Methods 16 patients with rectal cancer needing operation were randomly divided into two groups. One group was treated with 400 mg 5-fluorouracil suppository by rectum 1 h before operating, the other group were treated with 400 mg 5- fluorouracil by infusion lh before operating. During operation kept the normal tissues around of cancerous areas and rectal cancer tissues. The 5-fluorouraeil levels in, rectal cancer tissues and nlusele around, draining lymph node and peripheral blood were measured by HPCL. Results After treated with 5-fluorouracil suppository, the 5-fluorouracil levels in cancer tissues, in muscles up the rectal wall, down rectal walls, in draining lymph node and in peripheral blood was 21.68, 13.57, 15.41,2.14, and 0.068, respectively . The 5-fluorouraeil levels from the same areas as above after drop infusion of 5-Fu were 4.57 , 0. 074, 0. 064,1.69and 0.025μg·g^-1. Conclusion The 5-Fu levels in cancer and peripheral tissues could be significantly elevated by using than those by infusion 5-Fu. The 5-Fu suppository can more efficaciously prevent the cancer cells from implanting and transferring during the operations. Meanwhile, it can efficaciously reduce the side-effects caused by chemotherapy.