耐受性和药代动力学的新22抑制剂,HM30181,在健康韩国男性志愿者:单身,multiple-dose随机、安慰剂对照的研究。

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金正日TE,顾N, Yoon SH,曹司法院,公园公里,胫骨SG,张成泽IJ,余公里

耐受性和药代动力学的新22抑制剂,HM30181,在健康韩国男性志愿者:单身,multiple-dose随机、安慰剂对照的研究。

其他。2012年2月,34 (2):482 - 94。doi: 10.1016 / j.clinthera.2012.01.003。Epub 2012年1月28日。

PubMed ID

22284902 (在PubMed

]

文摘

背景:HM30181是口服22 (P-gp)抑制剂开发增强P-gp底物药物的口服生物利用度。目的:本研究的目的是调查的耐受性和药代动力学性质HM30181单个和多个口服后政府健康韩国男性志愿者。研究了满足监管标准在韩国市场测试产品。方法:dose-block-randomized、双盲、安慰剂对照、剂量递增研究,180 - 360年,600年,和900毫克单剂组和60 - 180,和360毫克multiple-dose组和10个科目(8活跃;每组2安慰剂)。在单剂研究中,血液和尿液样本收集120小时后药物管理局。在multiple-dose研究中,受试者接受研究药物或安慰剂每天口服一次5天。收集血液样本624小时后过去的剂量,24小时后第一个剂量评价积累指数。收集尿液样本120小时后过去的剂量。药代动力学分析使用noncompartmental执行方法。 Adverse events were collected by the spontaneous reporting of the subjects or when subjects were asked general health-related questions. RESULTS: Thirty and 70 healthy male volunteers completed the single- and multiple-dose studies, respectively. Mean (SD) age and body weight of subjects in the single administration group were 24.0 (1.8) years and 68.8 (7.4) kg, respectively, and those of the multiple administration group were 24.5 (2.6) years and 67.6 (7.7) kg, respectively. The plasma concentrations peaked at 14 to 42 hours and declined with t((1/2)) of 75.7 to 169.3 hours after single administration, and peaked at 5.5 to 8.0 hours and declined with t((1/2)) of 153.5 to 215.2 hours after multiple administrations. C(max) and area under the concentration curve within dosing intervals (AUC(tau)) increased dose dependently after single administration; however, dose-dependent increases in C(max) and AUC(tau) were not observed after multiple administrations. The fraction of drug excreted unchanged in urine was minimal, with values <0.01% in all dose groups. HM30181 accumulated after multiple administrations with an accumulation index of 4.0 to 7.4. All adverse events reported were mild in intensity; there were no serious adverse events reported. The most frequently reported adverse event was gastrointestinal disorder. CONCLUSIONS: HM30181 was well tolerated after oral administration within the dose range evaluated, with the exception of the repeated administration of 360 mg, for which gastrointestinal disorders were frequently reported. The systemic exposure of HM30181 was relatively low, and dose proportional properties of HM30181 were not observed.

DrugBank数据引用了这篇文章

药物靶点

药物	目标	类	生物	药理作用	行动
hm - 30181	22 - 1	蛋白质	人类	是的	抑制剂	细节