第一阶段,随机、交叉、开放研究的药物动力学Solriamfetol (jzp - 110)在健康成年受试者有或没有食物。

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陆Zomorodi K, Kankam M, Y

第一阶段,随机、交叉、开放研究的药物动力学Solriamfetol (jzp - 110)在健康成年受试者有或没有食物。

其他。2019年2月,41 (2):196 - 204。doi: 10.1016 / j.clinthera.2018.12.001。Epub 2018年12月28日。

PubMed ID

30598342 (在PubMed

]

文摘

目的:Solriamfetol (jzp - 110),选择性多巴胺和去甲肾上腺素再摄取抑制剂wake-promoting强劲的影响,目前正在评估睡眠的减少和改善失眠患者嗜睡症和阻塞性睡眠呼吸暂停。本研究的目的是评估的影响食物的药代动力学(PK)参数和生物利用度solriamfetol最高目的的治疗剂量在健康成年人和描述其在禁食条件下肾排泄。方法:在这个非盲、随机、交叉研究中,健康的成年受试者收到一个300毫克剂量的solriamfetol禁食条件(10 h)和美联储条件(30分钟后开始一个标准化的高脂肪、高热量的早餐),至少有一个7天,洗脱期之间的剂量。收集血液样本PK分析在这两种情况在指定时间点。收集尿液样本48 h postdose在禁食条件下。样本分析solriamfetol(血浆和尿液)和n -乙酰solriamfetol(尿液)通过使用验证质/ MS分析方法。食物的影响solriamfetol相对生物利用度研究通过对比90%置信区间(CIs)美联储的自然对数转换PK /禁食比率参数Cmax AUC0-t, AUC0-infinity的指定范围80% - -125%。安全性和耐受性也被评估。结果:共有32名受试者参加(50%女性;53.1%的黑人,46.9%的白人; mean age, 35.6 years), and 31 were included in the PK analyses. Solriamfetol was rapidly absorbed in both conditions. The 90% CIs for the fed/fasted geometric mean ratios were 89.2-98.8 for Cmax (ratio of 93.9%) and 93.8-101.5 for AUC0-infinity (ratio of 97.6%), indicating the absence of a food effect. In the fasted condition, 89.8% of solriamfetol was recovered in urine as unchanged drug over 48 h; 1.1% was excreted as a minor metabolite, N-acetyl solriamfetol. A total of 55 adverse events (AEs), all mild, were reported by 18 subjects (56.3%). The frequency and type of AEs were similar in the 2 conditions; the most common AEs (insomnia, headache, hypervigilance, decreased appetite, and nausea) were all mild in severity and resolved without treatment. IMPLICATIONS: Solriamfetol relative bioavailability was bioequivalent in the fed and fasted conditions, showing that solriamfetol can be taken without regard to meals; furthermore, tolerability was similar in both conditions. Renal excretion of unchanged drug is the primary route of elimination.

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药物

Solriamfetol