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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Gemmill J D, Howie C A, Meredith P A, Kelman A W, Rasmussen H S, Hillis W S, Elliott H L

University Department of Medicine and Therapeutics, Stobhill General Hospital, Glasgow, UK.

Br J Clin Pharmacol. 1991 Oct;32(4):429-32. doi: 10.1111/j.1365-2125.1991.tb03926.x.

UK-68,798, a novel class III anti-arrhythmic agent was administered intravenously to twelve healthy volunteers in a placebo controlled, double-blind, dose-escalating study. 2. Doses of 5 and 10 micrograms kg-1 of UK-68,798 selectively and significantly prolonged the QT interval, with mean maximum changes of 35 and 107 ms respectively, without affecting other ECG intervals. 3. There were dose-related increases in AUC but clearance (23 l h-1), terminal elimination half-life (8 h) and volume of distribution (245 l) were found to be independent of dose with low levels of intra- and inter-patient variability. 4. UK-68,798 has electrophysiological effects indicative of selective class III anti-arrhythmic activity and merits further assessment in clinical studies.

在一项安慰剂对照、双盲、剂量递增研究中，对12名健康志愿者静脉注射新型III类抗心律失常药物UK-68,798。2. UK-68,798剂量为5和10微克/千克时，可选择性且显著延长QT间期，平均最大变化分别为35和107毫秒，且不影响其他心电图间期。3. 曲线下面积（AUC）随剂量增加，但清除率（23升/小时）、终末消除半衰期（8小时）和分布容积（245升）与剂量无关，患者内和患者间变异性较低。4. UK-68,798具有表明选择性III类抗心律失常活性的电生理效应，值得在临床研究中进一步评估。

Gemmill J D, Howie C A, Meredith P A, Kelman A W, Rasmussen H S, Hillis W S, Elliott H L

University Department of Medicine and Therapeutics, Stobhill General Hospital, Glasgow, UK.

Br J Clin Pharmacol. 1991 Oct;32(4):429-32. doi: 10.1111/j.1365-2125.1991.tb03926.x.

UK-68,798, a novel class III anti-arrhythmic agent was administered intravenously to twelve healthy volunteers in a placebo controlled, double-blind, dose-escalating study. 2. Doses of 5 and 10 micrograms kg-1 of UK-68,798 selectively and significantly prolonged the QT interval, with mean maximum changes of 35 and 107 ms respectively, without affecting other ECG intervals. 3. There were dose-related increases in AUC but clearance (23 l h-1), terminal elimination half-life (8 h) and volume of distribution (245 l) were found to be independent of dose with low levels of intra- and inter-patient variability. 4. UK-68,798 has electrophysiological effects indicative of selective class III anti-arrhythmic activity and merits further assessment in clinical studies.

在一项安慰剂对照、双盲、剂量递增研究中，对12名健康志愿者静脉注射新型III类抗心律失常药物UK-68,798。2. UK-68,798剂量为5和10微克/千克时，可选择性且显著延长QT间期，平均最大变化分别为35和107毫秒，且不影响其他心电图间期。3. 曲线下面积（AUC）随剂量增加，但清除率（23升/小时）、终末消除半衰期（8小时）和分布容积（245升）与剂量无关，患者内和患者间变异性较低。4. UK-68,798具有表明选择性III类抗心律失常活性的电生理效应，值得在临床研究中进一步评估。