Van Hecken A, Juliano M L, Depré M, De Lepeleire I, Arnout J, Dynder A, Wildonger L, Petty K J, Gottesdiener K, De Hoon J N
Center for Clinical Pharmacology, University Hospital Gasthuisberg, Leuven, Belgium.
Aliment Pharmacol Ther. 2002 Sep;16(9):1683-8. doi: 10.1046/j.1365-2036.2002.01332.x.
Aspirin is widely used as an anti-thrombotic drug; however, it has been suggested that enteric-coated formulations of aspirin may be less bioavailable and less effective as anti-thrombotic agents.
To assess the effect of a formulation of enteric-coated, low-dose (81 mg) aspirin on serum generated thromboxane B2 and platelet aggregation in healthy subjects.
Twenty-four subjects participated in a double-blind, randomized, placebo-controlled, parallel-group, multiple-dose study. Twelve subjects in each of two groups received a daily oral dose of enteric-coated aspirin (81 mg) or matching placebo for 7 days. Serum thromboxane B2 and platelet aggregation (using 1 mm arachidonic acid and 1 microg/mL collagen as agonists) were measured 1-3 days prior to day 1, on day 1 (prior to therapy) and 4 h after the last dose on day 7.
After seven daily doses of enteric-coated aspirin, the mean percentage inhibition from baseline of ex vivo generated serum thromboxane B2 was 97.4%, compared with a 7.8% increase after placebo treatment. The mean percentage inhibition of arachidonic acid- and collagen-induced platelet aggregation was 97.9% and 70.9%, respectively, following enteric-coated aspirin, compared with - 1.0% and 2.7%, respectively, after placebo.
The anti-platelet effects of multiple, daily, low-dose aspirin (as assessed by inhibition of serum thromboxane B2 and platelet aggregation) are not adversely affected by enteric coating.
阿司匹林作为一种抗血栓药物被广泛使用；然而，有人提出阿司匹林的肠溶制剂作为抗血栓药物可能生物利用度较低且效果较差。
评估肠溶低剂量（81毫克）阿司匹林制剂对健康受试者血清中血栓素B2生成及血小板聚集的影响。
24名受试者参与了一项双盲、随机、安慰剂对照、平行组、多剂量研究。两组各12名受试者每日口服肠溶阿司匹林（81毫克）或匹配的安慰剂，持续7天。在第1天前1 - 3天、第1天（治疗前）以及第7天最后一剂后4小时测量血清血栓素B2和血小板聚集情况（使用1毫米花生四烯酸和1微克/毫升胶原作为激动剂）。
每日服用7剂肠溶阿司匹林后，体外生成的血清血栓素B2较基线的平均抑制百分比为97.4%，而安慰剂治疗后增加了7.8%。服用肠溶阿司匹林后，花生四烯酸和胶原诱导的血小板聚集的平均抑制百分比分别为97.9%和70.9%，而安慰剂治疗后分别为 - 1.0%和2.7%。
多次每日低剂量阿司匹林的抗血小板作用（通过抑制血清血栓素B2和血小板聚集评估）不受肠溶包衣的不利影响。
