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TOPICAL APPLICATION OF WR-2721 ACHIEVES HIGH CONCENTRATIONS IN THE RECTAL WALL

机译:WR-2721的典型应用可在直肠壁中实现高浓度

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摘要

Rectal wall injury is an important treatment-related morbidity in patients treated with radiation for prostate cancer, We have undertaken this study to investigate the merits of topical intrarectal application of the radioprotective compound WR-2721. Male Copenhagen rats were injected intrarectally with 2% WR-2721 gel, At 10, 20, 30 and 40 min after application, a laparotomy was performed, and the rectum and prostate were removed. Concentrations of total WR-1065 (the active metabolite of WR-2721) were determined in these samples by an HPLC assay. While the concentration in the rectal wall tended to increase with time, it did not change substantially in the prostate. The concentration in the rectal wall was found to be significantly higher at all times, We conclude that preferential accumulation of WR-2721 in the rectal wall can be achieved by topical application, This is a promising approach to modifying rectal wall tolerance that deserves more study. (C) 1995 by Radiation Research Society [References: 19]
机译:直肠壁损伤是接受放射线治疗的前列腺癌患者中与治疗相关的重要发病率,我们进行了这项研究,以研究局部应用直肠内放射防护化合物WR-2721的优点。雄性哥本哈根大鼠经直肠内注射2%WR-2721凝胶,在应用后10、20、30和40分钟进行剖腹手术,并切除直肠和前列腺。通过HPLC测定法测定这些样品中总WR-1065(WR-2721的活性代谢产物)的浓度。尽管直肠壁中的浓度会随时间增加,但在前列腺中并未发生实质性变化。发现直肠壁中的浓度始终都显着升高。我们得出结论,通过局部应用可实现WR-2721在直肠壁中的优先积累,这是一种改善直肠壁耐受性的有前途的方法,值得进一步研究。 (C)1995年,辐射研究学会[参考文献:19]

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