Anttila M, Kahela P, Uotila P
Research Center, Farmos Group Ltd., Turku, Finland.
Int J Clin Pharmacol Ther Toxicol. 1988 Feb;26(2):88-92.
To compare conventional (CT) and enteric-coated (ECT) tablets of acetylsalicylic acid (ASA) six healthy adult subjects ingested one 0.5-g tablet of these formulations daily for fifteen days in a cross-over study. Significant amount of ASA was detected in peripheral blood of every subject after the ingestion of CT or ECT. The rate of absorption of ASA was faster and its peak plasma concentration was higher after the ingestion of CT. The formation of thromboxane B2 (TXB2) decreased during blood clotting concomitantly with the absorption of ASA from both formulations. The formation of TXB2 was equally and completely inhibited by CT and ECT as it decreased to 1% of the control value one day after the first dose. During treatment with a single daily dose of 0.5 g of CT or ECT, the serum level of TXB2 remained at this low level and returned to the control level gradually in two weeks after the last dose. The present study indicates that significant amount of unchanged ASA is absorbed also from ECT and that the formation of TXB2 is equally and completely inhibited with a 0.5-g daily dose of both formulations.
为比较乙酰水杨酸(ASA)的普通片剂(CT)和肠溶片剂(ECT),在一项交叉研究中,6名健康成年受试者每天服用一片0.5克的这两种制剂,持续15天。在摄入CT或ECT后,每个受试者的外周血中均检测到大量ASA。摄入CT后,ASA的吸收速度更快,其血浆峰值浓度更高。在血液凝固过程中,血栓素B2(TXB2)的形成随着两种制剂中ASA的吸收而减少。CT和ECT对TXB2的形成具有同等且完全的抑制作用,在首次给药后一天,TXB2的形成降至对照值的1%。在用每日单剂量0.5克的CT或ECT治疗期间,TXB2的血清水平保持在该低水平,并在最后一剂后两周逐渐恢复到对照水平。本研究表明,ECT中也有大量未改变的ASA被吸收,并且两种制剂每日剂量0.5克时对TXB2的形成具有同等且完全的抑制作用。