Parker J O
Department of Medicine, Queen's University, Kingston, Ontario, Canada.
Eur Heart J. 1989 May;10 Suppl A:43-9. doi: 10.1093/eurheartj/10.suppl_a.43.
Sixteen patients with chronic, stable exercise-induced angina pectoris were studied during acute and sustained therapy with a new nitroglycerin (GTN) patch*. This patch provides a biphasic GTN release profile with therapeutic GTN plasma concentrations developing soon after application and persisting for 12h, but with low plasma concentrations during the remainder of the 24h period. This profile of GTN release was designed to avoid nitrate tolerance by providing a low nitrate period for substantial periods during each 24-h application period. In a placebo-controlled double-blind study, two GTN patches each releasing 7.5 mg GTN were applied. The active patches induced a significant decrease in systolic blood pressure and an increase in heart rate during initial application. Exercise duration to the end-point of moderate angina (P2) was increased at 4 and 8h during acute therapy and the changes during sustained therapy were similar. Thus, the Biophase GTN patch has been shown to improve exercise performance during acute therapy and, more importantly, to maintain this effect during sustained once-daily therapy.
对16例慢性、稳定型运动诱发心绞痛患者在使用新型硝酸甘油（GTN）贴剂进行急性和持续治疗期间进行了研究。这种贴剂具有双相GTN释放曲线，应用后很快就能达到治疗性GTN血浆浓度，并持续12小时，但在24小时周期的其余时间血浆浓度较低。这种GTN释放曲线的设计目的是通过在每24小时的应用周期中提供较长时间的低硝酸盐期来避免硝酸盐耐受性。在一项安慰剂对照双盲研究中，应用了两片每片释放7.5mg GTN的GTN贴剂。在最初应用时，活性贴剂导致收缩压显著降低，心率增加。在急性治疗期间的4小时和8小时，达到中度心绞痛终点（P2）的运动持续时间增加，持续治疗期间的变化相似。因此，已证明双相GTN贴剂在急性治疗期间可改善运动表现，更重要的是，在每日一次的持续治疗期间能维持这种效果。
