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首页> 外文期刊>Journal of drug assessment >Effects of food on the pharmacokinetics of AT-1015, a novel 5-HT_(2A) receptor antagonist
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Effects of food on the pharmacokinetics of AT-1015, a novel 5-HT_(2A) receptor antagonist

机译:食物对新型5-HT_(2A)受体拮抗剂AT-1015药代动力学的影响

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摘要

The selective 5-HT_(2A) receptor antagonist AT-1015 is being studied for its antiplatelet properties. This study aimed to determine the effect of food on AT-1015 pharmacokinetics and assess its safety and tolerability. Eight healthy male volunteers received single oral doses of 10 mg AT-1015 in a four-way crossover design. The mean area under the plasma concentration-time curve increased from 43 ng.h/ml in the fasting state to 58,60 and 54 ng.h/ml when taken 10,20 and 40 minutes after the start of a standard meal (p = 0.004 for overall treatment effect). Results for C_(max) were similar, but failed to reach statistical significance (p = 0.07). AT-1015 was safe and well tolerated. In conclusion, food increases the bioavailability of AT-1015, but the timing of the dose after the start of food is unimportant in the range 10 to 40 minutes. It is therefore recommended that AT-1015 be given after food.
机译:选择性5-HT_(2A)受体拮抗剂AT-1015的抗血小板特性正在研究中。这项研究旨在确定食物对AT-1015药代动力学的影响,并评估其安全性和耐受性。八名健康的男性志愿者在四向交叉设计中接受了10 mg AT-1015的单次口服剂量。血浆浓度-时间曲线下的平均面积从禁食状态下的43 ng.h / ml增加到标准餐开始后10,20和40分钟时摄取的58,60和54 ng.h / ml(p = 0.004(总体治疗效果)。 C_(max)的结果相似,但未达到统计学显着性(p = 0.07)。 AT-1015安全且耐受性良好。总之,食物可增加AT-1015的生物利用度,但食物开始后的给药时间在10至40分钟的范围内并不重要。因此,建议在饭后服用AT-1015。

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