Influence of Differing Analgesic Formulations of Aspirin on Pharmacokinetic Parameters

Pharmaceutics

Kunal Kanani¹  Sergio C. Gatoulis²  Michael Voelker³ 

[1] School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, NJ 08854, USA; E-Mail:;Bayer HealthCare, 100 Bayer Blvd, Whippany, NJ 07981, USA;Bayer HealthCare, Building K56, 51368 Leverkusen, Germany; E-Mail:

关键词: clinical pharmacokinetics;    pharmacokinetics;    absorption;    formulation;    prodrugs;    aspirin;   

DOI  :  10.3390/pharmaceutics7030188

来源: mdpi

【 摘 要 】

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 C_max compared to effervescent, granules in suspension and fast release tablets. Effervescent tablets, fast release tablets, and granules in suspension provide a consistently lower median T_max 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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.