Archives of Pharmacal Research

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

Pharmacokinetics of talniflumate, a prodrug of niflumic acid, following oral administration to man

  • Kim, Hyun-Ji (Department of Pharmaceutics, College of Pharmacy, Seoul National University) ;
  • Han, Yong-Hae (Department of Pharmaceutics, College of Pharmacy, Seoul National University) ;
  • Chung, Suk-Jaeng (Department of Pharmaceutics, College of Pharmacy, Seoul National University) ;
  • Lee, Min-Hwa (Department of Pharmaceutics, College of Pharmacy, Seoul National University) ;
  • Shim, Chang-Koo (Department of Pharmaceutics, College of Pharmacy, Seoul National University)
  • Published : 1996.08.01
Download PDF
⟨ Previous Next ⟩

Abstract

Plasma profile of niflumic acid following oral administration of talniflumate tablets (Somalgen) was compared to that of niflumic acid tablets in man. Plasma niflumic acid was assayed by HPLC method. Plasma niflumic acid profile from the tainiflumate tablets was similar to that from the niflumic acid tablets resulting in no differences in $AUC, C_max, t_max$ and MRT. It demonstrates that talniflumate is a prodrug of niflumic acid, and undergoes extensive first-pass biotransformation to niflumic acid. However, plasma niflumic acid concentration at 30 min after tainiflumate dosing was significantly (p<0.05) higher than that of niflumic acid dosing. The more potent analgesic activity of talniflumate than niflumic acid might be related to this higher plasma drug concentration at the earlier phase. Considering that tainiflumate is less irritant to gastrointestinal mucosa than niflumic acid, talniflumate seems to be advantageous over niflumic acid in terms of activity and side effects.

Keywords

References

  1. J. Chromatogr. v.533 High performance liquid chromatographic determination of niflumic acid in human plasma and urine Avgerinos,A.;Malamataris,S.
  2. Br. Med. J. v.290 Prolactinomas Grossman,A.;Besser,G.M.
  3. MS theis College of Pharmacy, Seoul National University Pharmacokinetics of talniflumate, a prodrug of niflumic acid, following oral administration to human Kim,H.J.
  4. J. Pharmacol. Exp. Ther. v.186 Metabolism of niflumic acid-$^{14}C$ : absorption, excretion and biotransformation by human and dog Lan,S.J.;Chando,T.J.;Weliky,I.;Schreiber,E.C.
  5. J. Neural. Transm. v.51 The endocrine profile of bromocriptione: it`s application in endocrine deseases Lancranjan,I.
  6. Farmaco. Ed. Sci. v.36 Nuevos esteres de acidos anilinonicotinicos Y N-fenilantranilicos sustituidos(New esters of substituted anilinonicotinic and phenylanthranilic acids) Los,M.;Boned,J.E.;Piccininali,C.
  7. The Extra Pharmacopoeia (29th ed.) Martindale
  8. Cephalosporin pharmacokinetics in beta-lactam antibiotics Nightingale,C.H.;French,M.A.;Quintiliani,R.;Muranishi,S.(ed.)