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금은화 추출물이 폐암치료제 gefitinib의 약물동태에 미치는 영향
구태성(Tae-Sung Koo),서숙희(Suk-Hee Seo),김성섭(Sung-Sub Kim) 대한약학회 2017 약학회지 Vol.61 No.2
The objective of this study was to estimate the potential herb drug interaction between gefitinib and Lonicera japonica (LJ) by evaluating changes in gefitinib pharmacokinetics following single and multiple oral doses of LJ in rats. Firstly, to determine basic pharmacokinetics of gefitinib, rat pharmacokinetics after 3, 10 and 30 mg/kg single intravenous and oral administration of gefitinib was executed. Secondly, single and 7-day repeated oral dose pharmacokinetics of gefitinib(10 mg/kg) after pretreatment with saline or LJ extract (500 mg/kg) were performed. In addition, the effect of fecal and urinary recovery after co-treatment with LJ and the inhibition of CYP3A4 by LJ was evaluated. Gefitinib showed dose-independent pharmacokinetics at intravenous and oral doses of 3−30 mg/kg and the pharmacokinetic parameters of gefitinib following single and multiple doses were not significantly affected by pretreatment with LJ extract. Fecal and urinary recovery of gefitinib was not significantly different between groups and LJ extract did not inhibit CYP3A4, main metabolic enzyme of gefitinib, activity until the concentration reached 300 μg/mL. These indicated that pharmacokinetics of gefitinib was not significantly affected by co-treatment with LJ extract.
Enzalutamide와 활성대사체의 동시분석법 개발 및 흰쥐에서의 활성대사체 동태 특성 규명
정종우(Jong-woo Jeong),구태성(Tae-Sung Koo) 대한약학회 2018 약학회지 Vol.62 No.2
A liquid chromatography–tandem mass spectrometric method was developed for the determination of an anti-prostate cancer drug, enzalutamide (EZT), and its active metabolite, N-desmethyl enzalutamide (NDE), in rat plasma. EZT, NDE and bicalutamide (internal standard; BCT) were extracted with ethyl acetate and separated using a column packed with octadecylsilica (5 μm, 2.1 × 50 mm) with 0.1% formic acid and methanol as the mobile phase. Detection was accomplished using MS/MS by multiple-reaction monitoring the transitions of m/z 465.1 to 209.2, 451.2 to 195.2 and 431.1 to 217.1 for EZT, NDE and BCT, respectively. The quantifiable range for the plasma samples was confirmed to be from 0.5 to 1,000 ng/ mL, and the all validation values, including the precision (coefficient of variance ≤ 11.80%) and accuracy (relative error ≤ 5.107%) of the measurements, were within the acceptable ranges given by FDA guidelines. The developed analytical method was successfully applied to characterize the kinetics of formation of the active metabolite. Considering EZT is pri-marily eliminated by hepatic metabolism in rats, the formation of NDE accounts for approximately 34% of the overall elim-ination of EZT in rats.