Gastrointestinal Factors in Aspirin Absorption: A Quantitative Study

doi:10.1002/jps.2600530203

Journal of Pharmaceutical Sciences

Volume 53, Issue 2, February 1964, Pages 129-134

https://doi.org/10.1002/jps.2600530203 Get rights and content

Three gastrointestinal factors influencing aspirin absorption have been selectively adjusted for quantitative measurement of their effect on the rate of salicylate absorption in humans and dogs. These are (a) gastric emptying, (b) aspirin dissolution rate, and (c) intragastric pH. Other factors such as tablet disintegration time, aspirin particle size, and intersubject variability have been eliminated or reduced where possible. The major portion of the salicylate in the blood during the first 20 minutes comes from the stomach. Impedance of gastric emptying by the use of atropine and placing the subjects in a left lateral position did not eliminate the higher plasma salicylate levels produced by the inclusion of the buffer antacids in aspirin tablets. The major effect of these antacids appears to be an acceleration of aspirin dissolution. This has been confirmed in this study by an in vivo demonstration of more rapid absorption from solutions of aspirin than from tablets. Aspirin in solution has a lower pH alone than with the inclusion of buffering antacids. Selective adjustment of the degree of aspirin and sodium salicylate ionization through the use of various buffers provided a method of study of the influence of intragastric pH on the rate of aspirin absorption. Support was obtained from dog and human studies in favor of the pH partition hypothesis that salicylates are absorbed more rapidly at low pH values.

REFERENCES (23)

E.B. Truitt et al.
Toxicol. Appl. Pharmacol.
(1960)
W.D. Paul et al.
This Journal
(1950)
J.W.E. Harrisson et al.
This Journal
(1959)
P. Sleight
Lancet
(1960)
G. Levy
This Journal
(1961)
J.I. Routh et al.
L.J. Edwards
Trans. Faraday Soc.
(1951)
P.A. Shore et al.
J. Pharmacol. Exptl. Therap.
(1957)
C.A.M. Hogben et al.
J. Pharmacol. Exptl. Therap.
(1957)
R.C. Batterman
New Engl. J. Med.
(1958)

G.A. Cronk

New Engl. J. Med.

(1958)

Cited by (16)

The absorption of aspirin is reduced after coronary artery bypass grafting
2019, Journal of Thoracic and Cardiovascular Surgery
Citation Excerpt :
However, in the present study aspirin compliance was confirmed by low TxB2 level and observed intake of aspirin. It has been known for decades that SA is more rapidly absorbed at low pH values.21 However, the gastric pH after CABG in the early postoperative period is normalized 24 hours after surgery.22
Despite treatment with the antiplatelet drug aspirin, some patients who undergo coronary artery bypass grafting (CABG) experience a thromboembolic event in the early postoperative period. The etiology of a reduced aspirin effect after CABG is still unsolved. Hence, we investigated whether patients who undergo CABG have a reduced absorption of aspirin after surgery, measured as levels of plasma salicylic acid (SA).
In total, 53 patients were included between October 2015 and May 2018. Blood samples where obtained at the day before surgery, and at the first (day 1) and second (day 2) postoperative day. A subgroup of 10 patients had additional blood samples obtained on day 1. Plasma SA was measured using liquid chromatography-electrospray-ionization tandem-mass spectrometry. Multiplate Analyzer (Roche, Roche Diagnostics, Mannheim, Germany) and VerifyNow Aspirin Test (Accumetrics, San Diego, Calif) were used to assess platelet aggregation as a measurement of the antiplatelet effect of aspirin.
A comparison of the difference in change of SA concentration between the day before surgery with day 1 and day 2 showed a significantly reduced increase in SA plasma levels after intake of aspirin at day 1 and day 2 after surgery (P < .0001), including a significantly reduced SA increase in the subgroup at 2, 3, and 4 hours after intake of aspirin. Corresponding with a reduced effect of aspirin, neither Multiplate Analyzer arachidonic acid, nor VerifyNow Aspirin Test showed a significant reduction in platelet aggregation 1 hour after intake of aspirin at day 1 (P < .0001). This also accounted for the subgroup 2, 3, and 4 hours after aspirin intake on day 1. At day 2 the same pattern as preoperatively was detected.
After CABG, the SA level and the effect of aspirin were reduced in the immediate postoperative period.
Biopharmaceutic and pharmacokinetic studies following the oral administration of sodium salicylate in oily and aqueous vehicles to rabbit
2006, International Journal of Pharmaceutics
The pharmacokinetic parameters, i.e. peak concentration (c_max); peak time (t_max); area under the curve (AUC); elimination rate constant (k); absorption rate constant (k_a); Drug clearance (cl_t), and the volume of distribution $(v_{d})$ of sodium salicylate administered in fractionated coconut oil (FCO) have been compared with that from an aqueous and glycerin vehicles using a three-way crossover study in 12 rabbits. The results of the study show that all of the pharmacokinetic parameters tested differ significantly when administered in oily rather than aqueous or glycerin vehicles. No statistically significant difference was found between any of the above mentioned parameters when comparison was made between aqueous and glycerin formulations. The results indicate that sodium salicylate is absorbed at a lower rate but to a greater extent from oily formulation. Possible reasons for these differences are discussed and is suggested, therefore, that the oily formulation might be used as a sustained release preparation.
Influence of tiemonium on the gastrointestinal absorption of aspirin
1983, International Journal of Pharmaceutics
The present study illustrates the importance of bioavailability testing whenever two active ingredients are combined in the same formulation in order to be administered simultaneously. The negative influence of the major spasmolytic drug, tiemonium, on the absorption of aspirin was demonstrated in the dog. This activity is so important that it was logical to suppose that this effect would be the same in man. In order to remove this effect, a special formulation was designed in which the two ingredients were released one after the other. Even so, an initial experiment in man gave unexpected results which were shown in an in vitro study to be due to extraneous factors connected with the preparation of the tablets. The importance of such in vitro investigations in avoiding hasty interpretation of in vivo findings is thus once again demonstrated.
Is placing a victim in the left lateral decubitus position an effective first aid intervention for acute oral poisoning? A systematic review
2019, Clinical Toxicology
Biopharmaceutics and Clinical Pharmacokinetics: An INTRODUCTION, Fourth Edition, Revised and Expanded
2017, Biopharmaceutics and Clinical Pharmacokinetics: An INTRODUCTION, Fourth Edition, Revised and Expanded
Study of improving the absorption and bioavailability of the aspirin and promethazine on the experimental animals-rabbits
2015, International Journal of Pharmaceutical Sciences Review and Research

View all citing articles on Scopus

: This investigation was supported by a grant from the Bristol-Myers Co., New York, N. Y.

View full text

Reserach ArticleGastrointestinal Factors in Aspirin Absorption: A Quantitative Study

Toxicol. Appl. Pharmacol.

This Journal

This Journal

Lancet

This Journal

Trans. Faraday Soc.

J. Pharmacol. Exptl. Therap.

J. Pharmacol. Exptl. Therap.

New Engl. J. Med.

New Engl. J. Med.

Reserach Article
Gastrointestinal Factors in Aspirin Absorption: A Quantitative Study