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Absorption of Flurbiprofen in the Fed and Fasted States

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Abstract

The oral absorption of flurbiprofen, an antiinflammatory nonsteroidal compound, was compared in the fasted vs the fed state. When ingested as an aqueous solution of the sodium salt, absorption kinetics followed a monoexponential pattern in half of the subjects and a bimodal pattern with a lag time before the onset of the second phase of absorption in the other half of the subjects. When ingested in the free acid form as a tablet either with water (fasted state) or with water 15 min after 330 ml of apple juice (fed state), flurbiprofen absorption was always bimodal, and the lag time before the onset of the second phase was shown to be dependent on the gastric emptying time (r = 0.623, P < 0.01). The gastric emptying times were significantly longer when the drug was administered in the fed state (average GET = 57 min in the fasted state and 102 min in the fed state; P < 0.01). These results suggest that gastric emptying effects are one important way in which absorption of drugs can be affected by meal intake.

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REFERENCES

  1. P. G. Welling and F. L. S. Tse. Food interactions affecting the absorption of analgesic and antiinflammatory agents. Drug-Nutrient Interact. 2:153–168 (1983).

    Google Scholar 

  2. G. J. Szpunar, K. S. Albert, G. G. Bole, J. H. Dreyfuss, G. F. Lockwood, and J. G. Wagner. Pharmacokinetics of flurbiprofen in man. I. Area/dose relationships. Biopharm. Drug Dispos. 8:273–283 (1987).

    Google Scholar 

  3. W. Brener, T. R. Hendrix, and P. R. McHugh. Regulation of the gastric emptying of glucose. Gastroenterology 85:76–82 (1983).

    Google Scholar 

  4. W. H. Steinberg, F. A. Mina, P. G. Pick, and G. K. Frey. Heidelberg capsule. I. In vitro evaluation of a new instrument for measuring intragastric pH. J. Pharm. Sci. 54:772–776 (1965).

    Google Scholar 

  5. J. D. Maxwell, W. C. Watson, J. K. Watt, and A. Ferguson. Radiotelemetering studies of jejunal pH before and after vagotomy and pyloroplasty. Gut 9:612–616 (1968).

    Google Scholar 

  6. P. Mojaverian, R. Ferguson, P. H. Vlasses, M. L. Rocci, A. Oren, J. A. Fix, L. J. Caldwell, and C. Gardner. Estimation of gastric residence time of the Heidelberg capsule in humans: Effect of varying food composition. Gastroenterology 89:392–397 (1985).

    Google Scholar 

  7. C. A. Youngberg, R. R. Berardi, M. L. Hyneck, W. F. Howatt, G. L. Amidon, J. H. Meyer, and J. B. Dressman. Comparison of gastrointestinal pH in CF and healthy volunteers. Digest. Dis. Sci. 32:472–480 (1987).

    Google Scholar 

  8. R. F. Bergstrom, D. R. Kay, and J. G. Wagner. The pharmacokinetics of penicillamine in a female mongrel dog. J. Pharmacokin. Biopharm. 9:603–621 (1981).

    Google Scholar 

  9. Y. Plusquellec, G. Compistron, S. Stevens, J. Barre, J. Jung, J. P. Tillement, and G. Houin. A double-peak phenomenon in the pharmacokinetics of veralipride after oral administration: A double site model for drug absorption. J. Pharmacokin. Biopharm. 15:225–239 (1987).

    Google Scholar 

  10. J. G. Wagner, P. L. Stetson, J. A. Knol, J. C. Andrews, S. Walker-Andrews, C. A. Knutsen, H. Johnson, D. Priesborn, P. Terrio, Z. Yang, D. Ganos, and W. D. Ensminger. Steady-state arterial and hepatic venous plasma concentrations of 5-bromo-2′-deoxyuridine and 5-iodo-2′-deoxyuridine, drugs which are subject to both splanchnic and extra-splanchnic elimination. Select. Cancer Ther. 5:143–203 (1989).

    Google Scholar 

  11. J. B. Dressman, G. Rideout, and R. H. Guy. Delivery system technology. In C. Hansch (ed.), Advances in Medicinal Chemistry, Vol. 5. Chemistry and Pharmacy in Drug Development, Pergamon Press, Oxford, 1989, pp. 615–660.

    Google Scholar 

  12. J. E. F. Reynolds (ed.). Tetracycline monograph. In Martindale, The Extra Pharmacopeia, 28th ed., Pharmaceutical Press, London, 1982, p. 1219.

  13. J. M. Beare. Antifungal preparations in dermatology. Prescriber's J. 8:30–35 (1968).

    Google Scholar 

  14. A. Karim, T. Burns, D. Janky, and A. Hurwitz. Food induced changes in theophylline absorption from controlled release formulations. II. Importance of meal composition and dosing time relative to meal intake in assessing changes to absorption. Clin. Pharmacol. Ther. 38:642–647 (1985).

    Google Scholar 

  15. J.-R. Malagelada, G. F. Longstreth, W. H. J. Summerskill, and V. L. W. Go. Measurement of gastric functions during digestion of ordinary solid meals in man. Gastroenterology 70:203–210 (1976).

    Google Scholar 

  16. J. B. Dressman, R. R. Berardi, T. L. Russell, L. Dermentzoglou, K. Jarvenpaa, S. Schmaltz, and J. L. Barnett. Upper GI pH in healthy young men and women. Pharm. Res. 7:756–761 (1990).

    Google Scholar 

  17. J. N. Hunt and W. R. Spurrell. The pattern of emptying of the human stomach. J. Physiol. 113:157–168 (1951).

    Google Scholar 

  18. J. S. Fordtran. Ionic constituents and osmolality of gastric and small-intestinal fluids after eating. Am. J. Digest. Dis. 11:503–521 (1966).

    Google Scholar 

  19. M. Abramowitz (ed.). Drugs for treatment of systemic fungal infections. Med. Lett. 28:41 (1986).

    Google Scholar 

  20. A. J. Sedman, P. K. Wilkinson, E. Sakmar, D. J. Weidler, and J. G. Wagner. Food effects on absorption and metabolism of alcohol. J. Stud. Alcohol 37:1197–1214 (1976).

    Google Scholar 

  21. Y.-J. Lin, D. J. Weidler, D. C. Garg, and J. G. Wagner. Effects of solid food on blood levels of alcohol in man. Res. Commun. Chem. Pathol. Pharmacol. 13:713–722 (1976).

    Google Scholar 

  22. P. K. Wilkinson, A. J. Sedman, E. Sakmar, D. R. Kay, and J. G. Wagner. Pharmacokinetics of ethanol after oral administration in the fasted state. J. Pharmacokin. Biopharm. 5:207–224 (1977).

    Google Scholar 

  23. J. A. Clements, R. C. Heading, W. S. Nimmo, and C. F. Prescott. Kinetics of acetaminophen absorption and gastric emptying in man. Clin. Pharmacol. Ther. 24:420–431 (1978).

    Google Scholar 

  24. C. G. Wilson. Relationship between pharmacokinetics and gastrointestinal transit. In J. G. Hardy, S. S. Davis, and C. G. Wilson (eds.), Drug Delivery to the GI Tract, Ellis Horwood, Chichester, 1989, pp. 161–178.

    Google Scholar 

  25. S. S. Walkenstein, J. W. Dubb, W. C. Randolf, W. J. Westlake, R. M. State, and A. P. Intoccia. Bioavailability of cimetidine in man. Gastroenterology 74:360–365 (1978).

    Google Scholar 

  26. R. L. Oberle and G. L. Amidon. The influence of variable gastric emptying and intestinal transit rates on the plasma level curve of cimetidine: An explanation for the double peak phenomenon. J. Pharmacokin. Biopharm. 15:529–544 (1987).

    Google Scholar 

  27. R. F. Bergstrom, D. R. Kay, T. M. Harkcom, and J. G. Wagner. Penicillamine kinetics in normal subjects. Clin. Pharmacol. Ther. 30:404–413 (1981).

    Google Scholar 

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Dressman, J.B., Berardi, R.R., Elta, G.H. et al. Absorption of Flurbiprofen in the Fed and Fasted States. Pharm Res 9, 901–907 (1992). https://doi.org/10.1023/A:1015800932454

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