Influence of food on the absorption of acetylsalicylic acid from enteric-coated dosage forms

Abstract

The absorption of acetylsalicylic acid (ASA) from two different enteric-coated dosage forms, tablets (Premaspin) and granules (Reumyl), was studied in healthy volunteers under fasting and non-fasting conditions by following the plasma concentration and urine recovery of salicylates after single doses of ASA 1 g. Conventional tablets (Aspirin) were used as the reference. Under fasting conditions the absorption of ASA from the two different enteric-coated preparations was complete. Taken with food the enteric-coated tablets gave much lower plasma concentrations than under fasting conditions, and absorption was not complete in all subjects. In contrast, absorption from the enteric-coated granules was not influenced by the intake of food. It was concluded that enteric-coated granules of ASA permit more reproducible absorption than enteric-coated tablets.

The gastrointestinal absorption of drugs in man: a review of current concepts and methods of investigation.

“…This technique has been employed to compare the absorption of acetylsalicylic acid from enteric-coated tablets and granules in both fasting and non-fasting individuals (Bogentoft et al, 1978). When taken with food, the tablets remained in the stomach for around 4 h, probably because of the screening effect of the pylorus (see above, under Gastric emptying); under fasting conditions they were emptied in less than 1 h. In contrast, granules did not exhibit this difference.…”

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

“…Differences in concentration for SA and ASA were observed in this study, which might be influenced by the intake of food. Bogentoft et al (1978) repoterd that the absorption of ASA from an enteric-coated preparation under nonfasting conditions was later than that in fasting conditions. They determined plasma levels of SA after administration of enteric-coated tablets under fasting and non-fasting conditions.…”

“…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.…”

Minimization of Gastric Damage with Enteric-Coated Aspirin Granules Compared to Buffered Aspirin

“…Evaluation of urinary excre tion data from standard bioavailability stud ies has shown the enteric granules and plain aspirin to be equally bioavailable [18]. The small size of these granules allows them to be readily emptied from the stomach and they are protected by the enteric coat from disso lution during residence in the stomach [19]. This study shows that for acute usage, the stomach safety advantage provided by en teric coating is maintained when the delivery system is reduced from the enteric tablet to the enteric-coated granule formulation.…”