环丙沙星和氨芳汀之间药物相互作用的健康成人中氨芳汀药代动力学的快照

Ruth M. Ogboye, A. Adegbola, O. Bolaji, J. Soyinka
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摘要

考虑到细菌感染和疟疾感染的地理重叠,蒿甲醚/氨苯曲明和环丙沙星可同时用于治疗疟疾-伤寒合并感染。已知环丙沙星以抑制方式扰乱某些药物代谢酶的活性程度,从而能够进行药物-药物相互作用。本研究旨在评估氨苯曲明的处置以及氨苯曲明与环丙沙星之间药代动力学相互作用的程度。在两期平行药代动力学研究中,参与者给予80/480 mg蒿甲醚-氨芳碱片剂,并采血进行初步药代动力学分析。在28天的洗脱期后,参与者被分为AL组和AL- cip组。AL组接受6次标准剂量的AL,每小时12次,连续3天,而AL- cip组在开始标准剂量的AL之前,连续3天使用500毫克环丙沙星。在预定的采样点采集血液样本。采用经验证的生物分析方法测定血浆中氟苯曲明浓度,并使用WinNonlin®药代动力学软件进行药代动力学分析。平均最大血浆浓度(Cmax)为3032 μg/ml (142 ~ 6776 μg/ml)。氟苯曲明达到Cmax (tmax)的时间平均为6小时,随后缓慢清除5l /h。浓度AUC0 -∞下的总面积为111945.9 μgh/L。结果是初步的;他们证明了氟苯曲明的药代动力学与先前报道的研究一致。
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A snapshot into lumefantrine pharmacokinetics in healthy adults recruited for drug-drug interactions between ciprofloxacin and lumefantrine
Considering the geographical overlap of bacterial and malaria infection, artemether/lumefantrine and ciprofloxacin may be administered together for the treatment of malaria-typhoid co-infection. Ciprofloxacin is known to upset the degree of activities of some drug-metabolizing enzymes in an inhibitory manner, thus capable of perpetrating drug-drug interaction. This study aims to assess the disposition of lumefantrine and the extent of pharmacokinetic interactions between lumefantrine and Ciprofloxacin. Participants in a two-phase parallel pharmacokinetic study were given 80/480 mg tablets of artemether-lumefantrine, and blood samples were taken for preliminary pharmacokinetics analysis. After a washout period of 28 days, the participants were grouped into AL and AL-CIP groups. The AL group received six standard doses of AL twelve hourly for three days, while the AL-CIP group proceeded with 500 mg ciprofloxacin for three days before commencing standard doses of AL. The blood samples were collected at predetermined sampling points. The plasma concentration of lumefantrine was measured by a validated bioanalytical assay, and pharmacokinetic analysis was conducted using WinNonlin® pharmacokinetic software. The mean maximum plasma concentration (Cmax) of lumefantrine was 3032 μg/ml (142 to 6776 μg/ml range). Time for lumefantrine to reach Cmax (tmax) was on average 6 hrs followed by a slow clearance of 5 L/h. Total Area Under Concentration AUC0–∞ was 111945.9 μgh/L. The results are preliminary; they demonstrate that the pharmacokinetics of lumefantrine are consistent with those described in previously reported studies.
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