PR-350的药代动力学及放射增敏作用

Pharmacokinetics and radiosensitizing effect of PR-350.

作者信息

Hirokawa K, Nakajima T, Tsumura M, Nishita T, Yamada R, Onoyama Y

机构信息

Department of Radiology, Osaka City University Medical School, Osaka, Japan.

出版信息

Radiat Med. 1997 Jan-Feb;15(1):45-9.

PMID:9134584

Abstract

PURPOSE

The in vivo pharmacokinetics and sensitizing effects of PR-350, a newly developed, highly water-soluble radiosensitizer were examined.

MATERIALS AND METHODS

C3H/HeJ mice bearing SCC-VII tumor cells were used in the experiments. Results were compared with those of PR-28 and SR-2508.

RESULTS

The intratumoral concentration of PR-350 reached the maximum value of 77.7 mg/kg 20 min after intravenous injection. The concentration in the brain was below the detection limit. The enhancement ratios of PR-350 calculated using the growth delay method were 0.9 for PR-350 at 50 mg/kg and 1.4 for PR-350 at 100 mg/kg, compared with 1.4 for SR-2508 at 100 mg/kg and 1.0 for PR-28 at 100 mg/kg.

CONCLUSION

PR-350 and SR-2508 revealed similar sensitizing effects. The side effects of PR-350 are expected to be equal to or less than those of SR-2508. PR-350 seems to be a promising radiosensitizer.

摘要

目的

研究新开发的高水溶性放射增敏剂PR - 350的体内药代动力学及增敏作用。

材料与方法

实验采用接种SCC - VII肿瘤细胞的C3H/HeJ小鼠。将结果与PR - 28和SR - 2508的结果进行比较。

结果

静脉注射后20分钟，PR - 350的瘤内浓度达到最大值77.7 mg/kg。脑内浓度低于检测限。采用生长延迟法计算，PR - 350在50 mg/kg时的增敏比为0.9，在100 mg/kg时为1.4；相比之下，SR - 2508在100 mg/kg时为1.4，PR - 28在100 mg/kg时为1.0。