University of Illinois at Chicago
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Effect of food on systemic exposure to niflumic acid following postprandial administration of talniflumate

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posted on 2024-04-15, 22:08 authored by Wonku Kang, Kibum Kim, Eun-Young Kim, Kwang-il Kwon, Jun Seok Bang, Young-Ran Yoon
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 approximately 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 (AUC(inf)) 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.



Kang, W., Kim, K., Kim, E. -Y., Kwon, K. -I., Bang, J. S.Yoon, Y. -R. (2008). Effect of food on systemic exposure to niflumic acid following postprandial administration of talniflumate. European Journal of Clinical Pharmacology, 64(10), 1027-1030.


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