Plasma levels of aspirin following effervescent and enteric coated tablets, and their effect on platelet function

Abstract

Single doses of effervescent tablets (1200 mg) and enteric coated (EC) tablets (1300 mg and 650 mg) of acetylsalicylic acid (aspirin, ASA) were given to healthy volunteers in random order. Plasma ASA and salicylic acid (SA) levels were measured and concurrent in vitro measurements of the volunteers' platelet aggregation were carried out. The effervescent preparation resulted in peak ASA concentrations of 17-40 mg/l, achieved 20 to 30 min after a 1200 mg dose, whereas peak ASA levels of 0.01-0.37 mg/l were observed 4-6 h after a 650 mg dose of the EC preparation. With all the aggregating agents that were added to the test system maximum inhibition of platelet aggregation (about 50% of pre dose levels) was seen 1.0 h after the effervescent ASA dose, and persisted to at least 24 h, but with the EC preparation not until 24 h, at which time the degree of inhibition was also about 50% of pre-dose levels. A 1.0 g dose of sodium salicylate had no effect on in vitro platelet function. It was concluded that mean plasma levels of ASA of less than 0.25 mg/l are sufficient to depress aggregation by approximately 50%. A low dose of ASA taken daily either as effervescent ASA or EC ASA, significantly inhibits platelet aggregation and so may reduce the risk of ischaemic episodes in susceptible patients.

Commonly used fertility drugs, a diet supplement, and stress force AMPK-dependent block of stemness and development in cultured mammalian embryos

“…The 10 μM Asa dose used here was well within normal usage where normal to medium doses produce C max plasma doses of~2-200 μM [61,89]. Interestingly, it was previously reported that Asa blocks development of cultured embryos to the blastocyst stage and reduces the number of cells/embryo [90,91].…”

“…BR-DIM was used at 20 μM because this dose was used to slow growth or kill cultured prostate cancer cells [21], and a peak of~7 μM BR-DIM was reported during in vivo mouse exposure [60]. Asa (salicylate) was used at 10 μM because this is a standard plasma level after enteric pill [61] and well within the 1-3-mM levels after high-dose Asa treatment of T2D [62], and the 2-mM dose was used to show that major therapeutic levels of Asa require AMPK activity [16]. CC at 5 μM was validated in dose-response testing in other previous studies from our lab for testing AMPK effects in two-cell embryos and blastocysts and recently optimized for TSCs [41,45,63].…”

An evaluation of different doses of soluble aspirin and aspirin tablets in postoperative dental pain.

“…An alteration in gastrointestinal mobility after a general anaesthetic may contribute towards the poor efficacy that we observed after the 600 and 900 mg doses of aspirin tablets. Soluble aspirin has also been shown to be more effective than the same dose of aspirin tablets in the treatment of postoperative pain after orthopaedic surgery and general surgery (Dixit et al, 1984), and have a more pronounced effect on platelet aggregation and bleeding time (Roos-Lee et al, 1982;Proost et al, 1983 (von Graffenried & Hill, 1979).…”

Semi‐micro column high‐performance liquid chromatography with UV detection for quantification of aspirin and salicylic acid and its application to patients' sera administered with low‐dose enteric‐coated aspirin

“…An enteric-coated tablet is designed to resist disintegration in an acidic environment such as the stomach and pass it without dissolution. However, enteric-coated preparations have variable actions and incomplete absorption (Ross-Lee et al, 1982;Roberts et al, 1984;Bogentoft et al, 1978), and therefore the pharmacokinetics of enteric-coated low-dose ASA has not yet been clarified.…”