影响食物和酒精对口服的药物代谢动力学情况,延长释放的氢可酮配方健康志愿者。

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罗宾侬Farr SJ,罗宾逊CY,厘米

影响食物和酒精对口服的药物代谢动力学情况,延长释放的氢可酮配方健康志愿者。

中国新药杂志。2015年1月19日,7:1-9。doi: 10.2147 / CPAA.S70831。eCollection 2015。

PubMed ID

25653563 (在PubMed

]

文摘

背景:本研究的目的是评估药物,口服生物利用度,和安全的延长释放氢可酮(HC-ER)管理与食物或酒精。方法:两个单中心、非盲、随机、交叉在健康的志愿者进行了研究。在一个两期food-interaction研究中,12个受试者收到HC-ER 20毫克一夜后快速和高脂肪餐。研究中,受试在三alcohol-interaction 30 naltrexone-blocked收到HC-ER 50毫克以0%,20%或40%的酒精/橙汁溶液后一夜快。药代动力学参数来源于血浆浓度的氢可酮及其代谢产物。结果:暴露后氢可酮HC-ER 20毫克是类似于美联储和禁食状态,所评估的血浆浓度与时间曲线下的面积不时的剂量的检测浓度(AUC0-t;316.14和311.94 ng。h /毫升);相对生物利用度(Frel)为101.74%。氢可酮的差异(美联储与禁食)意味着最大血浆浓度(Cmax; 28.86 versus 22.74 ng/mL) and median time to Cmax (tmax; 6 versus 8 hours) were not clinically significant. Administration of 20% alcohol with HC-ER 50 mg did not increase systemic exposure relative to 0% alcohol (AUC0-t 878 versus 832 ng . h/mL; Frel 105%) or result in clinically meaningful changes in Cmax (51.8 versus 46.3 ng/mL) or tmax (5.44 versus 6.16 hours). Administration with 40% alcohol increased AUC0-t (1,008 ng . h/mL versus 832 ng . h/mL; Frel 120%) and Cmax (109 versus 46.3 ng/mL), and shortened tmax (2.43 versus 6.16 hours). Adverse events occurred in 10.0%, 24.1%, and 66.7% of subjects after 0%, 20%, and 40% alcohol, respectively. CONCLUSION: HC-ER can be administered without regard to meals. While there was no evidence of "dose-dumping" (an unintended, rapid release in a short time period of all or most of the hydrocodone from HC-ER), even with 40% alcohol, as with all opioids, alcohol should not be ingested while using HC-ER.

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药物

氢可酮