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In Vivo Evaluation of Enteric-Coated Naproxen Tablets Using Gamma Scintigraphy

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Abstract

Seven healthy, male volunteers were entered into a randomized, open crossover study of the gastrointestinal transit of two enteric-coated 500-mg naproxen tablets. Two radiolabeled tablets were given to each volunteer on two occasions separated by 7 days, once in the fasted state and once after breakfast. Radiolabeling of tablets was achieved by the incorporation of samarium-152 oxide during manufacture, followed by neutron activation of the tablet to produce the gamma-emitting isotope samarium-153. No loss of tablet integrity was seen in the stomach and all tablets disintegrated in the small intestine. Onset of tablet disintegration was controlled predominantly by gastric emptying. Time in the small intestine prior to tablet disintegration was independent of food intake. Naproxen blood levels with time were consistent with the delayed release of naproxen from the tablets. Overall, transit, disintegration, and absorption were as expected from an enteric-coated tablet.

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REFERENCES

  1. I. Haslock. Review of NSAID-induced upper gastrointestinal morbidity and mortality. In R. Cheli (ed.), Royal Society of Medicine International Congress and Symposium Series 147 Royal Society of Medicine, London, 1989, pp. 3–10.

    Google Scholar 

  2. F. L. Lanza. Endoscopic studies of gastric and duodenal injury after the use of ibuprofen, aspirin and other nonsteroidal anti-inflammatory agents. Medicine 77:19–24 (1984).

    Google Scholar 

  3. F. Halter. Mechanism of gastrointestinal toxicity of NSAIDs. Scand. Rheumatol. 73:16–21 (1988).

    Google Scholar 

  4. G. H. Griffiths, G. M. Owen, S. Kirkman, and R. Shields. Measurement of the rate of gastric emptying using chromium-51. Lancet 1:1244–1245 (1966).

    Google Scholar 

  5. M. Alpsten, G. Ekenved, and L. Solvell. A profile scanning method of studying the release properties of different types of tablets in man. Acta Pharm. Suec. 13:107–122 (1976).

    Google Scholar 

  6. D. L. Casey, R. M. Beihn, G. A. Digenis, and M. B. Shabhu. Method for monitoring hard gelatin capsule disintegration times in humans using external scintigraphy. J. Pharm. Sci. 65:1412–1413 (1976).

    Google Scholar 

  7. J. G. Hardy, J. N. C. Healey, S. W. Lee, and J. R. Reynolds. Gastrointestinal transit of an enteric-coated delayed-release 5-aminosalicylic acid tablet. Aliment. Pharmacol. Ther. 1:209–216 (1987).

    Google Scholar 

  8. S. S. Davis, N. Washington, G. D. Parr, et al. Relationship between the rate of appearance of oxprenolol in the systemic circulation and the location of an oxprenolol Oros 16/260 drug delivery system within the gastrointestinal tract as determined by scintigraphy. Br. J. Clin. Pharmacol. 26:435–443 (1988).

    Google Scholar 

  9. I. R. Wilding, S. S. Davis, C. D. Melia, et al. Gastrointestinal transit of Sinemet CR in healthy volunteers. Neurology 39 (II Suppl. 2):53–58 (1989).

    Google Scholar 

  10. C. G. Wilson, N. Washington, J. L. Greaves, et al. Bimodal release of ibuprofen in a sustained-release formulation: A scintigraphic and pharmacokinetic open study in healthy volunteers under different conditions of food intake. Int. J. Pharm. 50:155–161 (1989).

    Google Scholar 

  11. G. A. Digenis, E. P. Sandefer, A. F. Parr, et al. Gastrointestinal behaviour of orally administered radiolabeled erythromycin pellets in man as determined by gamma scintigraphy. J. Clin. Pharmacol. 30:621–631 (1990).

    Google Scholar 

  12. S. S. Davis, R. Khosla, C. G. Wilson, N. Washington, S. T. Leslie, and S. Malkowska. The gastrointestinal transit of a controlled release formulation of indomethacin. Int. J. Pharm. 60:191–196 (1990).

    Google Scholar 

  13. J. G. Hardy, G. L. Lamont, D. F. Evans, A. K. Haga, and O. N. Gamst. Evaluation of an enteric-coated naproxen pellet formulation. Aliment. Pharmacol. Ther. 5:69–75 (1991).

    Google Scholar 

  14. A. F. Parr, R. M. Beihn, R. M. Franz, G. J. Szpunar, and M. Jay. Correlation of ibuprofen bioavailability with gastrointestinal transit by scintigraphic monitoring of 171 Er-labeled sustained-release tablets. Pharm. Res. 4:486–489 (1987).

    Google Scholar 

  15. J. G. Devane, M. Kavanagh, S. S. Davis, R. A. Sparrow, and I. R. Wilding. Correlation of GI transit parameters and pharmacokinetic characteristics of a controlled release nifedipine formulation. American Society of Clinical Pharmacology and Therapeutics, San Antonio, TX, 1991.

    Google Scholar 

  16. S. F. Phillips. Small bowel. In D. Kumar and S. Gustavsson (eds.), An Illustrated Guide to Gastrointestinal Motility John Wiley and Sons, Chichester, 1988, pp. 187–206.

    Google Scholar 

  17. H. M. Park, J. M. Chernish, B. D. Rosenbek, R. L. Brunelle, B. Hargrove, and H. N. Wellman. Gastric emptying of enteric-coated tablets. Digest. Dis. Sci. 29:207–212 (1984).

    Google Scholar 

  18. A. J. Coupe, S. S. Davis, D. F. Evans, and I. R. Wilding. Correlation of the gastric emptying of non-disintegrating tablets with gastrointestinal motility. Pharm. Res. 8:1281–1285 (1991).

    Google Scholar 

  19. R. Khosla, L. C. Feely, and S. S. Davis. Gastrointestinal transit of non-disintegrating tablets in fed subjects. Int. J. Pharm. 53:107–117 (1989).

    Google Scholar 

  20. R. C. Khosla and S. S. Davis. The effect of tablet size on the gastric emptying of non-disintegrating tablets. Int. J. Pharm. 62:R9–R11 (1990).

    Google Scholar 

  21. A. J. Coupe, S. S. Davis, and I. R. Wilding. Variation in gastrointestinal transit of pharmaceutical dosage forms in healthy subjects. Pharm. Res. 8:360–364 (1991).

    Google Scholar 

  22. J. G. Hardy, D. F. Evans, I. Zaki, et al. Evaluation of an enteric-coated naproxen tablet using gamma scintigraphy. Int. J. Pharm. 37:245–250 (1987).

    Google Scholar 

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Wilding, I.R., Hardy, J.G., Sparrow, R.A. et al. In Vivo Evaluation of Enteric-Coated Naproxen Tablets Using Gamma Scintigraphy. Pharm Res 9, 1436–1441 (1992). https://doi.org/10.1023/A:1015858829187

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  • DOI: https://doi.org/10.1023/A:1015858829187

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