Department of Hospital Pharmacy, Kanazawa University, Kanazawa 920-8641, Japan.
J Pharm Sci. 2011 Sep;100(9):3884-91. doi: 10.1002/jps.22602. Epub 2011 May 4.
In the initial treatment of acute myocardial infarction, it is important to administer oral low-dose acetylsalicylic acid (ASA) within 10 min of arrival at the hospital. However, ASA is supplied as an enteric-coated tablet or buffered tablet to prevent gastric irritation. Although current guidelines recommended that patients should chew their initial dose of ASA, there is little evidence as to whether this is efficacious. Therefore, we aimed to make a direct comparison of the pharmacokinetics and pharmacodynamics of ASA after ingestion of intact and chewed nonenteric-coated buffered ASA tablet (NBA) and enteric-coated ASA tablet (ECA) in a quadruple crossover study in healthy volunteers. Chewing ECA accelerated t(max) of ASA absorption, which became equivalent to that after ingestion of intact or chewed NBA. A significant decrease in serum thromboxane B(2) was observed 20 min after ingestion of chewed ECA, or intact or chewed NBA, and inhibition of platelet aggregation was also observed within 20 min. Thus, chewing of the ECA appears to result in a similar timing of ASA action to that in the case of chewed or unchewed NBA.
在急性心肌梗死的初始治疗中,重要的是在到达医院的 10 分钟内给予口服低剂量乙酰水杨酸(ASA)。然而,ASA 以肠溶衣片剂或缓冲片剂供应,以防止胃刺激。尽管目前的指南建议患者应咀嚼初始剂量的 ASA,但关于这是否有效,证据很少。因此,我们旨在通过一项在健康志愿者中进行的四重交叉研究,直接比较完整和咀嚼的非肠溶衣缓冲 ASA 片剂(NBA)和肠溶衣 ASA 片剂(ECA)后 ASA 的药代动力学和药效学。咀嚼 ECA 加速了 ASA 吸收的 t(max),使其与完整或咀嚼 NBA 后的吸收速度相当。咀嚼 ECA、完整或咀嚼 NBA 后 20 分钟观察到血清血栓素 B2 的显著下降,血小板聚集的抑制也在 20 分钟内观察到。因此,咀嚼 ECA 似乎会导致 ASA 作用的时间与咀嚼或未咀嚼 NBA 的作用时间相似。