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阿那曲唑单次给药及与塞来昔布联合给药后的比较药代动力学研究。

Comparative pharmacokinetics study of anastrozole after single administration and combination with celecoxib.

作者信息

Sun Xiaoyang, Lv Mingming, Wang Binjie, Zhao Simin, Guo Ping, Wang Shixiao, Gu Liqiang, Chen Xiaohui

机构信息

a Department of Pharmaceutical Analysis , School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , PR China and.

b Baiyunshan Pharmaceutical General Factory, Guangzhou Baiyunshan Pharmaceutical Holdings Co, Ltd , Guangzhou , PR China.

出版信息

Xenobiotica. 2018 Mar;48(3):279-284. doi: 10.1080/00498254.2017.1298872. Epub 2017 Sep 14.

Abstract

1. There are numerous investigations demonstrating that the cyclooxygenase-2 (COX-2) inhibitors might enhance the efficiency of anastrozole in breast cancer. Hence, this study was conducted to investigate the comparative pharmacokinetics of anastrozole after single administration and combination with celecoxib. 2. A simple protein precipitation procedure was adopted for the sample preparation with satisfactory extraction recovery for both anastrozole and the internal standard, and then anastrozole was separated and analysed on an ACQUITY BEH UPLC C column (50 × 2.0 mm, 1.7 μm, Waters) within 2 min. The calibration curves showed good linarites (r = 0.994). Intra- and inter-day precision were within 4.93 and 13.83%, respectively. The mean extraction recoveries across QC levels were within 91.4%, and the matrix effects were within 94.5%. 3. Results showed that the method was reliable to determine anastrozole in rat plasma. Compared with rats in single administration group, no significant difference was found in the combination group. It is workable to use celecoxib combined with anastrozole in clinical therapy.

摘要
  1. 大量研究表明,环氧化酶-2(COX-2)抑制剂可能会提高阿那曲唑治疗乳腺癌的疗效。因此,本研究旨在探讨阿那曲唑单次给药及与塞来昔布联合给药后的比较药代动力学。2. 采用简单的蛋白沉淀法进行样品制备,阿那曲唑和内标物的提取回收率均令人满意,然后在ACQUITY BEH UPLC C柱(50×2.0 mm,1.7μm,沃特世)上于2分钟内分离并分析阿那曲唑。校准曲线显示出良好的线性关系(r = 0.994)。日内和日间精密度分别在4.93%和13.83%以内。各质量控制水平下的平均提取回收率在91.4%以内,基质效应在94.5%以内。3. 结果表明,该方法用于测定大鼠血浆中的阿那曲唑是可靠的。与单次给药组的大鼠相比,联合给药组未发现显著差异。塞来昔布与阿那曲唑联合用于临床治疗是可行的。

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