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[优福定与替加氟栓的比较药代动力学研究及妇科恶性肿瘤的II期研究]

[Comparative pharmacokinetic study between UFT and FT-207 suppo and phase II studies in gynecological malignancies].

作者信息

Hatae M, Terahara M, Hokanishi H

出版信息

Gan To Kagaku Ryoho. 1984 Nov;11(11):2386-92.

PMID:6437345
Abstract

Plasma pharmacokinetics and accumulation into tissues were comparatively examined between UFT and FT-207 suppo and 7 gynecological malignancies were treated by UFT in a phase-II study. FT-207 suppo, the maximum level was attained. After administration, UFT plasma FT reached its maximum level at 2-3 hr, but for 0.5-1 hr after administration. On the other hand, plasma 5-FU concentration reached its peak 1-2 hr or 3-4 hr after UFT administration and revealed very low levels after FT-207 suppo administration. 5-FU accumulation in normal tissue (NT) was not proportional to administered doses of UFT, but in cancerous tissue (CT) it was dependent on total UFT dose. The CT/NT ratio with respect to 5-FU concentration was 5.36 after UFT administration. The same ratio after FT-207 suppo administration was 2.63. The specificity of 5-FU accumulation into cancerous tissue after UFT administration was significantly demonstrated. According to the Evaluating Criteria for cancer chemotherapy in solid tumors by the Japanese Society for Cancer Therapy, we obtained results of PR 2, NC 2 and PD 3 using a 600 mg/day administration of UFT for 7 gynecological malignancies consisting of 6 cervical carcinomas and 1 endometrial carcinoma.

摘要

比较研究了优福定(UFT)和替加氟(FT-207)栓剂的血浆药代动力学及组织蓄积情况,并在一项II期研究中用优福定治疗了7例妇科恶性肿瘤。对于FT-207栓剂,达到了最高水平。给药后,优福定血浆中的FT在2 - 3小时达到最高水平,但给药后0.5 - 1小时内。另一方面,优福定给药后1 - 2小时或3 - 4小时血浆5-氟尿嘧啶(5-FU)浓度达到峰值,而FT-207栓剂给药后血浆5-FU浓度显示非常低。正常组织(NT)中5-FU的蓄积与优福定的给药剂量不成比例,但在癌组织(CT)中,它取决于优福定的总剂量。优福定给药后,5-FU浓度的CT/NT比值为5.36。FT-207栓剂给药后的相同比值为2.63。显著证明了优福定给药后5-FU在癌组织中蓄积的特异性。根据日本癌症治疗协会对实体瘤癌症化疗的评估标准,对于由6例宫颈癌和1例子宫内膜癌组成的7例妇科恶性肿瘤,我们采用每天600毫克优福定的给药方案,获得了2例部分缓解(PR)、2例病情稳定(NC)和3例病情进展(PD)的结果。

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