Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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Effect of Probenecid on the Pharmacokinetic Behavior of Pranoprofen in Rats

흰쥐에서 프로베네시드가 프라노푸로펜의 약동학적 거동에 미치는 영향

  • Li, Xiu-Guo (College of Pharmacy, Chosun University, Yanbian University Nursing College) ;
  • Piao, Yong-Ji (College of Pharmacy, Chosun University) ;
  • Choi, Jun-Shik (College of Pharmacy, Chosun University)
  • 이수국 (조선대학교 약학대학, 중국 연변대학교 간호대학) ;
  • 박영길 (조선대학교 약학대학) ;
  • 최준식 (조선대학교 약학대학)
  • Published : 2005.12.20
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Abstract

The purpose of this study was to investigate the effect of probencid on the pharmacokinetics of oral pranoprofen in rats. Pranoprofen (5 mg/kg) was coadministered with 5, 10 or 20 mg/kg of probenecid orally. Coadministration of probenecid significantly altered the pharmacokinetics of pranoprofen at 10 and 20 mg/kg. Compared with the control group, probenecid significantly (p<0.05) increased the absorption rate constant $(K_{a})$, the peak concentrations $(C_{max})$ and accordingly the area under the plasma concentration-time curve (AUC) of pranoprofen at the dose level of 10 mg/kg and 20 mg/kg of probenecid. The relative bioavailability (RB%) of pranoprofen was 1.64- to 1.82- fold increased. Furthermore, 10 and 20 mg/kg probenecid induced the decreased elimination constants $(K_{el})$ and the prolonged half-lives $(t_{1/2})$ of pranoprofen with significance (p<0.05). Coadministration of 10 and 20 mg/kg of probenecid lowered the excreted amounts of pranoprofen in the urine by 21.3-22.5% compared to the control. Overall, probenecid enhanced the bioavailability of pranoprofen and decreased its elimination rate to a greater degree at higher dose. Based on the effect of probenecid on the pharmacokinetic behavior of pranoprofen, the dosage regimen of pranoprofen should be taken into consideration when pranoprofen is administered with probenecid in the clinical setting to the patients especially with peptic ulcer or renal failure.

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References

  1. A.-B. Gutman and T.-F. Yu, Benemid (p-[di-n-propyl-sulfamyl]-benxoic acid) as uricosuric agent in chronic gouty arthritis, Trans. Assoc. Am. Physicians, 64, 279-288 (1951)
  2. A.- B. Gutman, Uricosuric drugs, with special reference to probenecid and sulfmpyrazone, Adv. Pharmacol., 4, 91-142 (1966) https://doi.org/10.1016/S1054-3589(08)60098-8
  3. K.-H. Beyer, H.-F. Russo, E.-K. Tillson, A.-K. Miller, W.-F. Verwey and S.-R. Gass, 'Benemid,' p-(di-n-propylsulfamyl)-benzoic acid; its renal affinity and its elimination, Am. J. Physiol., 166, 625-640 (1951)
  4. W.-P. Boger, F.-W. Pitts and M.-E. Gallagher, Benemid and carinamide: comparison of effect on para-aminosalicylic acid (PAS) plasma concentrations, J. Lab. Clin. Med., 36, 276-282 (1950)
  5. P.-G. Dayton, T.-F. Yu, W. Chen, L. Berger, L.-A. West and A.-B. Gutman, The physiological dispositon of probenecid, including renal clearance, in man, studied by an improved method for its estimation in biological material, J. Pharmacol. Exp. Ther., 140, 278-286 (1963)
  6. T.-B. Tjandramaga, S.-A. Cucinell, Z.-H. Israili, J.-M. Perel, P.-G. Dayton, T.-F.Yu and A.-B. Gutman, Observations on the disposition of probenecid in patients receiving allopurinol, Pharmacology, 8, 259-272 (1972)
  7. Z.-H. Israili, J.-M. Pereel, R.-F. Cunningham, P.-G. Dayton, T.-F. Yu, A.-B. Gutman, K.-R. Long, R.-C. Jr Long and J.-H. Goldstein, Metabolites of probenecid. Chemical, physical, and pharmacological studies, J. Med. Chem., 15, 709-713 (1972) https://doi.org/10.1021/jm00277a004
  8. A.- M. Guarino, W.-D. Conway and H.-M. Fales, Mass spectral identification of probenecid metabolites in rat bile, Eur. J. Pharmacol., 8, 244-252 (1969) https://doi.org/10.1016/0014-2999(69)90084-3
  9. R.-F. Cunningham, Z.-H. Israili and P.-G. Dayton, Clinical pharmacokinetics of probenecid, Clin. Pharmacokinet., 6, 135-151 (1981) https://doi.org/10.2165/00003088-198106020-00004
  10. J.-M. PereI, R.-F. Cunningham, H.-M. Fales and P.-G. Dayton, Identification and renal excretion of probenecid metabolites in man, Life Sci. I., 9, 1337-1343 (1970) https://doi.org/10.1016/0024-3205(70)90041-X
  11. W.-D. Conway and S. Melethil, Excretion of probenecid and its metabolites in bile and urine of rats, J. Pharm. Sci., 63, 1551-1554 (1974) https://doi.org/10.1002/jps.2600631013
  12. A.-M. Guarino and L.-S. Schanker, Biliary excretion of probenecid and its glucuronide, Pharmacal. Exp. Ther., 164, 387-395 (1968)
  13. S.-P. Spina and E.-C. Jr Dillon, Effect of chronic probenecid therapy on cefazolin serum concentrations, Ann. Pharmacather., 37, 621-624 (2003) https://doi.org/10.1345/aph.1C347
  14. E.-S. Ho, D.-C. Lin, D.-B. Mendel and T. Cihlar, Cytotoxicity of antiviral nucleotides adefovir and cidofovir is induced by the expression of human renal organic anion transporter 1, J. Am. Sac. Nephrol., 11, 383-393 (2000)
  15. J.-B. Prtcihard and D.-S. Miller, Mechanisms mediating renal secretion of organic anions and cations, Physial. Rev., 73, 765-796 (1993) https://doi.org/10.1152/physrev.1993.73.4.765
  16. H.-L. McLeod, Clinically relevant drug-drug interactions in oncology. Br. J. Clin. Pharmacal., 45, 539-544 (1998) https://doi.org/10.1046/j.1365-2125.1998.00719.x
  17. T. Sekine, N. Watanabe, M. Hosoyarnada, Y. Kanai and H. Endou, Expression cloning and characterization of a novel multispecific organic anion transporter J. Biol. Chem., 272, 18526-18529 (1997) https://doi.org/10.1074/jbc.272.30.18526
  18. Y. Uwai, M. Okuda, K. Takami, Y. Hashimoto and K. Inui, Functional characterization of the rat multispecific organic anion transporter OAT1 mediating basolateral uptake of anionic drugs in the kidney, FEBS. Lett., 438, 321-324 (1998) https://doi.org/10.1016/S0014-5793(98)01328-3
  19. B. Bannwarth, F. Pehourcq, T. Schaeverbeke and J. Dehais, Clinical pharmacokinetics of low-dose pulse methotrexate in rheumatoid arthritis, Clin. Pharmacakinet., 30, 194-210 (1996) https://doi.org/10.2165/00003088-199630030-00002
  20. N. Yasui-Furukori, T. Uno, K. Sugawara and T. Tateishi, Different effects of three transporting inhibitors, veraparnil, cimetidine, and probenecid, on fexofenadine pharmacokinetics, Clin. Pharmacal. Ther., 77, 17-23 (2005) https://doi.org/10.1016/j.clpt.2004.08.026
  21. A. Resetar, D. Minick and T. Spector, Glucuronidation of 3'-azido-3'-deoxythymidine catalyzed by human liver UDP-glucuronosyltransferase. Significance of nucleoside hydrophobicity and inhibition by xenobiotics, Biachem. Pharmacal., 42, 559-568 (1991) https://doi.org/10.1016/0006-2952(91)90319-Z
  22. D.-R. Abernethy, D.-J. Greenblatt, B. Ameer and R.-I. Shader, Probenecid impairment of acetaminophen and lorazepam clearance: direct inhibition of ether glucuronide formation, J. Pharmacal. Exp. Ther., 234, 345-349 (1985)
  23. R.-K. Verbeeck, Pharmacokinetic drug interactions with nonsteroidal anti-inflammatory drugs. Clin. Pharmacokinet., 19, 44-66 (1990) https://doi.org/10.2165/00003088-199019010-00004
  24. D.-H. Chatfield and J.-N. Green, Disposition and metabolism of benoxaprofen in laboratory animal and man, Xenobiotica., 8, 133-144 (1978) https://doi.org/10.3109/00498257809060392
  25. A. Rubin, P. Warric, R.-L. Wolen, S.-M. Chemish, A.-S. Ridolfo and C.-M. Gruber Physiological disposition of fenoprofen in Man. III. Metabolism and protein binding of fenoprofen, J. Pharmacol. Exp. Ther., 183, 449-457 (1972)
  26. L.-M. Fuccela, G.-C. Goldaniga, E. Moro, V. Tamassia, G.-P. Tosolini and G. Valzelli, Fate of analgesic and anti-inflammatory drug K4277 after oral administration to man, Dur. J.Clin.Pharmacol., 6, 256-260 (1973) https://doi.org/10.1007/BF00644742
  27. R.-C. Luders, M.-B. Maggio-Cavaliere, H. Egger, H.-T.-L. Chemiken, D.-B. Gum and O. Resnick, Disposition of piprofen, a new anti-inflammatory drug, Clin. Pharmacol. Ther., 21, 721-730 (1977) https://doi.org/10.1002/cpt1977216721
  28. Y.K atoh, Pranoprofen: In Drug disposition, Vol. 1, R. Katoh (Ed.), Seishi Shoin, Tokyo, pp. 223-229 (1984)
  29. Y. Kato, N. Ariamand H. Nishimine, Studies on antiinflammatory agents XXXII. Absorption, excretion, distribution and metabolism of 2-(5h-[1]benzopyrano(2,3-b] pyridin-7-yl)propionic acid. (Y-8004) in rats and mice, Yakugaku Zasshi, 96, 819-826 (1976) https://doi.org/10.1248/yakushi1947.96.7_819
  30. I. Yoshio, A. Iwata, M. Isobe, R. Takamatsu and M. Higashi, The pharmacokinetics of pranoprofen in humans, Yakugaku Zasshi, 110, 509-515 (1990) https://doi.org/10.1248/yakushi1947.110.7_509
  31. T. Imai, T. Nomura and M. Otagiri, Probenecid-induced changes in the clearance of pranoprofen enantiomers, Chirality, 15, 318-323 (2003) https://doi.org/10.1002/chir.10208
  32. K. Sagara, I. Yamada, Y. Matsuura, M. Kawata and M. Shibata, Gastrointestinal physiology-regulated dogs for bioavailability evaluation of an oral controlled-release dosage form composed of pulsatile release granules, Biol. Pharm. Bull., 19, 1184-1188 (1996) https://doi.org/10.1248/bpb.19.1184
  33. M.-L. Rocci and W.-J. Juskko, LAGRAN program for area and moments in pharmacokinetic analysis, Comput. Programs Biomed., 16, 203-216 (1983) https://doi.org/10.1016/0010-468X(83)90082-X
  34. N. Baber, L. Halliday, R. Sibeon, T. Littler and M.-L. Orme, The interaction between indomethacin and probenecid. A clinical and pharmacokinetic study, Clin. Pharmacol. Ther., 24, 298-307 (1978) https://doi.org/10.1002/cpt1978243298