A Study on Pharmacokinetics of Acetylsalicylic Acid Mini-Tablets in Healthy Adult Males—Comparison with the Powder Formulation

  • Noriko Hida
    Division of Clinical Research and Development, Department of Clinical Pharmacy, School of Pharmacy, Showa University, Tokyo 142-8555, Japan
  • Taigi Yamazaki
    Division of Clinical Research and Development, Department of Clinical Pharmacy, School of Pharmacy, Showa University, Tokyo 142-8555, Japan
  • Yoshiaki Fujita
    Division of Pharmaceutics, Department of Pharmacology, Toxicology and Therapeutics, School of Pharmacy, Showa University, Tokyo 142-8555, Japan
  • Hidehiro Noda
    Pharmacy, Showa University Fujigaoka Hospital, Yokohama 227-8501, Japan
  • Takehiko Sambe
    Clinical Research Institute for Clinical Pharmacology and Therapeutics, Showa University, Tokyo 157-8577, Japan
  • Kakei Ryu
    Clinical Research Institute for Clinical Pharmacology and Therapeutics, Showa University, Tokyo 157-8577, Japan
  • Takuya Mizukami
    Clinical Research Institute for Clinical Pharmacology and Therapeutics, Showa University, Tokyo 157-8577, Japan
  • Sachiko Takenoshita
    Clinical Research Institute for Clinical Pharmacology and Therapeutics, Showa University, Tokyo 157-8577, Japan
  • Naoki Uchida
    Clinical Research Institute for Clinical Pharmacology and Therapeutics, Showa University, Tokyo 157-8577, Japan
  • Akihiro Nakamura
    Division of Pharmaceutics, Department of Pharmacology, Toxicology and Therapeutics, School of Pharmacy, Showa University, Tokyo 142-8555, Japan
  • Tsutomu Harada
    Division of Pharmaceutics, Department of Pharmacology, Toxicology and Therapeutics, School of Pharmacy, Showa University, Tokyo 142-8555, Japan

Description

<jats:p>Children with Kawasaki disease are prescribed acetylsalicylic acid powder as an antipyretic analgesic and antiplatelet agent; however, some of it remains in the mouth, leading to a bitter or sour taste. To address this issue, an in-hospital mini-tablet formulation of acetylsalicylic acid was developed. In order to use the mini-tablets safely and effectively, dissolution tests alone are not sufficient. Therefore, an open-label crossover study on six healthy participants was conducted to evaluate comparative pharmacokinetic parameters. The pharmacokinetic parameters of salicylic acid were Cmax: 4.80 ± 0.79 mg/L (powder; P), 5.03 ± 0.97 mg/L (mini-tablet; MT), AUC0–12: 18.0 ± 3.03 mg-h/L (P), 18.9 ± 4.59 mg-h/L (MT), those of acetylsalicylic acid Cmax: 0.50 ± 0.20 mg/L (P), 0.41 ± 0.24 mg/L (MT), AUC0–12: 0.71 ± 0.27 mg-h/L (P), 0.61 ± 0.36 mg-h/L (MT), with no significant differences between the mini-tablet and powder formulations. Although pharmacokinetic results obtained from adults cannot be directly applied to children, the results of this study are important for predicting pharmacokinetics. Furthermore, a formulation that can improve medication adherence in children who have difficulty taking acetylsalicylic acid powder, thus contributing to pediatric drug therapy.</jats:p>

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