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FT-207直肠栓剂在子宫颈鳞状细胞癌中的药代动力学。(II)每日剂量1克连续给药时的药代动力学

[Pharmacokinetics of FT-207 rectum suppository in squamous cell carcinoma of the uterine cervix. (II) Pharmacokinetics in continuous administration at a daily dose of 1 gram].

作者信息

Okazaki H, Hasegawa T, Endoh S, Hayashi Y, Chin N, Rin K, Nakagiri Y, Ishii Y, Fukui H, Kohno I

出版信息

Gan To Kagaku Ryoho. 1984 Apr;11(4):848-52.

PMID:6426396
Abstract

FT-207 rectum suppository at a daily dose of 1 g was repeatedly administered to patients with squamous cell carcinoma of the uterine cervix. Total doses ranged from 7 to 41 g. The following pharmacokinetic results were obtained in comparison with single administration. The blood level of FT-207 showed its peak of 35 to 37 mcg/ml at 4 hours after administration, of which half-time was 11 to 12 hours. The blood level of 5-FU showed its peak of 0.038 to 0.041 mcg/ml at 2 to 4 hours after administration, of which half time was more than 24 hours. Inter-individual differences were less than those of single administration. The level of FT-207 in tumor tissue was 14.2 mcg/g which was 15 times higher than that single administration. The level in healthy uterine cervix was 18.1 mcg/g which was 12 times higher that of single administration. The level of 5-FU in tumor tissue was 0.359 mcg/g which was 5 times than that of single administration. The level in normal tissue was 0.15 mcg/g which was 3 times higher than that of single administration. The level of 5-FU in tumor tissue was 7.8 to 8.4 times higher than that in blood. There was no difference in concentrations of both FT-207 and 5-FU between metastatic and non-metastatic lymph nodes.

摘要

对子宫颈鳞状细胞癌患者每日重复给予剂量为1g的FT - 207直肠栓剂。总剂量为7至41g。与单次给药相比,获得了以下药代动力学结果。FT - 207的血药浓度在给药后4小时达到峰值,为35至37mcg/ml,其半衰期为11至12小时。5 - FU的血药浓度在给药后2至4小时达到峰值,为0.038至0.041mcg/ml,其半衰期超过24小时。个体间差异小于单次给药。肿瘤组织中FT - 207的水平为14.2mcg/g,比单次给药时高15倍。健康子宫颈中的水平为18.1mcg/g,比单次给药时高12倍。肿瘤组织中5 - FU的水平为0.359mcg/g,是单次给药时的5倍。正常组织中的水平为0.15mcg/g,比单次给药时高3倍。肿瘤组织中5 - FU的水平比血液中的高7.8至8.4倍。转移性和非转移性淋巴结中FT - 207和5 - FU的浓度没有差异。

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