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Influence of Differing Analgesic Formulations of Aspirin on Pharmacokinetic Parameters

School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, NJ 08854, USA
Bayer HealthCare, 100 Bayer Blvd, Whippany, NJ 07981, USA
Bayer HealthCare, Building K56, 51368 Leverkusen, Germany
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Afzal R. Mohammed
Pharmaceutics 2015, 7(3), 188-198;
Received: 25 June 2015 / Revised: 29 July 2015 / Accepted: 29 July 2015 / Published: 3 August 2015
(This article belongs to the Special Issue Drug Metabolism and Pharmacokinetics)
Aspirin has been used therapeutically for over 100 years. As the originator and an important marketer of aspirin-containing products, Bayer’s clinical trial database contains numerous reports of the pharmacokinetics of various aspirin formulations. These include evaluations of plain tablets, effervescent tablets, granules, chewable tablets, and fast-release tablets. This publication seeks to expand upon the available pharmacokinetic information concerning aspirin formulations. In the pre-systemic circulation, acetylsalicylic acid (ASA) is rapidly converted into its main active metabolite, salicylic acid (SA). Therefore, both substances are measured in plasma and reported in the results. The 500 mg strength of each formulation was chosen for analysis as this is the most commonly used for analgesia. A total of 22 studies were included in the analysis. All formulations of 500 mg aspirin result in comparable plasma exposure to ASA and SA as evidenced by AUC. Tablets and dry granules provide a consistently lower Cmax compared to effervescent, granules in suspension and fast release tablets. Effervescent tablets, fast release tablets, and granules in suspension provide a consistently lower median Tmax compared to dry granules and tablets for both ASA and SA. This report reinforces the importance of formulation differences and their impact on pharmacokinetic parameters. View Full-Text
Keywords: clinical pharmacokinetics; pharmacokinetics; absorption; formulation; prodrugs; aspirin clinical pharmacokinetics; pharmacokinetics; absorption; formulation; prodrugs; aspirin
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Kanani, K.; Gatoulis, S.C.; Voelker, M. Influence of Differing Analgesic Formulations of Aspirin on Pharmacokinetic Parameters. Pharmaceutics 2015, 7, 188-198.

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