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. 1985;19(Suppl 2):137S–142S. doi: 10.1111/j.1365-2125.1985.tb02754.x

Oxprenolol absorption in man after single bolus dosing into two segments of the colon compared with that after oral dosing

K-H Antonin, P Bieck, M Scheurlen, M Jedrychowski, H Malchow
PMCID: PMC1463770  PMID: 4005115

Abstract

1 The systemic availability of oxprenolol after colonic and oral administration has been compared in a crossover study involving six healthy male volunteers. Drug administration into two regions of the colon (caecum and left flexure) was achieved by means of a colonoscopic technique.

2 There were no obvious differences in plasma concentrations after drug administration to the caecum and left flexure, although in one subject it was necessary to repeat colonic administration because of unexpectedly high plasma drug levels on the first occasion. The possible reasons for this abnormal response are discussed.

3 The mean systemic availability of oxprenolol was 82% after colonic compared with oral dosing, although marked differences were observed in individual plasma levels following drug administration by the two routes.

4 The results of this study support the concept of extending the duration of oxprenolol release from a rate-controlled dosage form to permit once-daily administration with this short elimination half-life drug.

Keywords: oxprenolol, drug absorption

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Alvan G., von Bahr C., Seidemann P., Sjöqvist F. High plasma concentrations of beta-receptor blocking drugs and deficient debrisoquine hydroxylation. Lancet. 1982 Feb 6;1(8267):333–333. doi: 10.1016/s0140-6736(82)91583-5. [DOI] [PubMed] [Google Scholar]
  2. Andersson K. E., Nyberg L., Dencker H., Göthlin J. Absorption of digoxin in man after oral and intrasigmoid administration studied by portal vein catheterization. Eur J Clin Pharmacol. 1975 Oct 10;9(1):39–47. doi: 10.1007/BF00613427. [DOI] [PubMed] [Google Scholar]
  3. Bond J. H., Jr, Levitt M. D., Prentiss R. Investigation of small bowel transit time in man utilizing pulmonary hydrogen (H2) measurements. J Lab Clin Med. 1975 Apr;85(4):546–555. [PubMed] [Google Scholar]
  4. Breen K. J., Bryant R. E., Levinson J. D., Schenker S. Neomycin absorption in man. Studies of oral and enema administration and effect of intestinal ulceration. Ann Intern Med. 1972 Feb;76(2):211–218. doi: 10.7326/0003-4819-76-2-211. [DOI] [PubMed] [Google Scholar]
  5. Castell D. O., Moore E. W. Ammonia absorption from the human colon. The role of nonionic diffusion. Gastroenterology. 1971 Jan;60(1):33–42. [PubMed] [Google Scholar]
  6. Colin-Jones D. G., Cockel R., Schiller K. F. Current endoscopic practice in the United Kingdom. Clin Gastroenterol. 1978 Sep;7(3):775–786. [PubMed] [Google Scholar]
  7. Cummings J. H., Wiggins H. S. Transit through the gut measured by analysis of a single stool. Gut. 1976 Mar;17(3):219–223. doi: 10.1136/gut.17.3.219. [DOI] [PMC free article] [PubMed] [Google Scholar]
  8. Degen P. H., Riess W. Simplified method for the determination of oxprenolol and other beta-receptor-blocking agents in biological fluids by gas-liquid chromatography. J Chromatogr. 1976 Jun 9;121(1):72–75. doi: 10.1016/s0021-9673(00)82299-2. [DOI] [PubMed] [Google Scholar]
  9. Griffin J. P. Drug interactions occurring during absorption from the gastrointestinal tract. Pharmacol Ther. 1981;15(1):79–88. doi: 10.1016/0163-7258(81)90017-6. [DOI] [PubMed] [Google Scholar]
  10. Kennedy M., Chinwah P., Wade D. N. A pharmacological method of measuring mouth caecal transit time in man. Br J Clin Pharmacol. 1979 Oct;8(4):372–373. doi: 10.1111/j.1365-2125.1979.tb04723.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Lennard M. S., Silas J. H., Freestone S., Trevethick J. Defective metabolism of metoprolol in poor hydroxylators of debrisoquine. Br J Clin Pharmacol. 1982 Aug;14(2):301–303. doi: 10.1111/j.1365-2125.1982.tb01982.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Mahgoub A., Idle J. R., Dring L. G., Lancaster R., Smith R. L. Polymorphic hydroxylation of Debrisoquine in man. Lancet. 1977 Sep 17;2(8038):584–586. doi: 10.1016/s0140-6736(77)91430-1. [DOI] [PubMed] [Google Scholar]
  13. Mason W. D., Winer N. Pharmacokinetics of oxprenolol in normal subjects. Clin Pharmacol Ther. 1976 Oct;20(4):401–412. doi: 10.1002/cpt1976204401. [DOI] [PubMed] [Google Scholar]
  14. Park B. K. Assessment of the drug metabolism capacity of the liver. Br J Clin Pharmacol. 1982 Nov;14(5):631–651. doi: 10.1111/j.1365-2125.1982.tb04950.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  15. Read N. W., Miles C. A., Fisher D., Holgate A. M., Kime N. D., Mitchell M. A., Reeve A. M., Roche T. B., Walker M. Transit of a meal through the stomach, small intestine, and colon in normal subjects and its role in the pathogenesis of diarrhea. Gastroenterology. 1980 Dec;79(6):1276–1282. [PubMed] [Google Scholar]
  16. de Boer A. G., Breimer D. D., Mattie H., Pronk J., Gubbens-Stibbe J. M. Rectal bioavailability of lidocaine in man: partial avoidance of "first-pass" metabolism. Clin Pharmacol Ther. 1979 Dec;26(6):701–709. doi: 10.1002/cpt1979266701. [DOI] [PubMed] [Google Scholar]
  17. de Boer A. G., Moolenaar F., de Leede L. G., Breimer D. D. Rectal drug administration: clinical pharmacokinetic considerations. Clin Pharmacokinet. 1982 Jul-Aug;7(4):285–311. doi: 10.2165/00003088-198207040-00002. [DOI] [PubMed] [Google Scholar]

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