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Effect of food on systemic exposure to niflumic acid following postprandial administration of talniflumate

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Abstract

Purpose

Talniflumate was designed as a prodrug of niflumic acid, a potent analgesic and anti-inflammatory drug, which is widely prescribed for treating rheumatoid diseases. The prandial effect on talniflumate absorption remains unclear; therefore, this study investigated the effect of food on the systemic exposure to niflumic acid in healthy volunteers.

Methods

Volunteers received a single 740-mg dose of talniflumate 30 min after consuming a high-fat breakfast, a low-fat breakfast, or no food (fasting condition). Plasma concentrations of both talniflumate and niflumic acid were measured using validated high-performance liquid chromatography coupled to tandem mass spectrometry.

Results

The maximum concentration of niflumic acid was 224 ± 193 ng/ml at ∼2.7 h in the fasted condition compared with 886 ± 417 ng/ml (p < 0.05) at 1.8 h and 1,159 ± 508 ng/ml (p < 0.01) at 2.2 h with the low- and high-fat meals, respectively. The mean area under the curve from zero to infinity (AUCinf) values after the low- and high-fat meals were four- and fivefold, respectively, the value while fasting (p < 0.05).

Conclusions

It is strongly recommended that talniflumate be taken after a meal to increase systemic exposure to its active metabolite. Our results suggest a reduction in the daily dosage of talniflumate when taken with food.

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Authors and Affiliations

  1. College of Pharmacy, Catholic University of Daegu, Kyoungbuk, 712–702, Korea

    Wonku Kang & Kibum Kim

  2. Department of Pharmacy, Samsung Medical Center, Seoul, Korea

    Eun-Young Kim

  3. College of Pharmacy, Chungnam National University, Daejeon, Korea

    Kwang-il Kwon

  4. Pharmaceutical Division, LG Life Sciences, Ltd, Seoul, Korea

    Jun Seok Bang

  5. College of Medicine, Kyoungpook National University, Daegu, Korea

    Young-Ran Yoon

Authors
  1. Wonku Kang
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  2. Kibum Kim
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  3. Eun-Young Kim
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  4. Kwang-il Kwon
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  5. Jun Seok Bang
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  6. Young-Ran Yoon
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Corresponding author

Correspondence to Wonku Kang.

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Kang, W., Kim, K., Kim, EY. et al. Effect of food on systemic exposure to niflumic acid following postprandial administration of talniflumate. Eur J Clin Pharmacol 64, 1027–1030 (2008). https://doi.org/10.1007/s00228-008-0524-4

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  • DOI: https://doi.org/10.1007/s00228-008-0524-4

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