Abstract
1 The absorption of metoprolol from the stomach, small intestine and colon of anaesthetized rats has been evaluated using an in situ technique. Absorption rates were measured in terms of the rate of disappearance of metoprolol fumarate from the lumen between 5 and 30 min after dosing. Adsorption was estimated from the initial rapid fall in luminal content within the first 5 min after drug administration.
2 The rate of drug absorption from the stomach was low or negligible. In the small intestine, the absorption rate constants, ka, at pH 6.2 and 7.5 were 0.66 and 0.81 h-1, respectively. In the colon, the rate of drug absorption at pH 7.5 was faster (ka = 1.21 h-1) than in other segments of the gut.
3 Drug adsorption in the stomach amounted to 11% of the administered dose. In the small intestine adsorption was greater (16-22%), presumably because of the larger surface area in this segment of the gut, but in the colon adsorption was negligible.
Keywords: absorption, metoprolol, rat
Full text
PDF




Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Doluisio J. T., Billups N. F., Dittert L. W., Sugita E. T., Swintosky J. V. Drug absorption. I. An in situ rat gut technique yielding realistic absorption rates. J Pharm Sci. 1969 Oct;58(10):1196–1200. doi: 10.1002/jps.2600581006. [DOI] [PubMed] [Google Scholar]
- Doluisio J. T., Crouthamel W. G., Tan G. H., Swintosky J. V., Dittert L. W. Drug absorption. 3. Effect of membrane storage on the kinetics of drug absorption. J Pharm Sci. 1970 Jan;59(1):72–76. doi: 10.1002/jps.2600590112. [DOI] [PubMed] [Google Scholar]
- Godbillon J., Evard D., Vidon N., Duval M., Schoeller J. P., Bernier J. J., Hirtz J. Investigation of drug absorption from the gastrointestinal tract of man. III. Metoprolol in the colon. Br J Clin Pharmacol. 1985;19 (Suppl 2):113S–118S. doi: 10.1111/j.1365-2125.1985.tb02751.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Jobin G., Cortot A., Godbillon J., Duval M., Schoeller J. P., Hirtz J., Bernier J. J. Investigation of drug absorption from the gastrointestinal tract of man. I. Metoprolol in the stomach, duodenum and jejunum. Br J Clin Pharmacol. 1985;19 (Suppl 2):97S–105S. doi: 10.1111/j.1365-2125.1985.tb02749.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Regårdh C. G., Johnsson G. Clinical pharmacokinetics of metoprolol. Clin Pharmacokinet. 1980 Nov-Dec;5(6):557–569. doi: 10.2165/00003088-198005060-00004. [DOI] [PubMed] [Google Scholar]
- Taylor D. C., Grundy R. Propranolol absorption in different regions of the rat gastrointestinal tract in situ: implications for sustained release formulations. J Pharm Pharmacol. 1980 Jul;32(7):499–500. doi: 10.1111/j.2042-7158.1980.tb12977.x. [DOI] [PubMed] [Google Scholar]
- Theeuwes F. Elementary osmotic pump. J Pharm Sci. 1975 Dec;64(12):1987–1991. doi: 10.1002/jps.2600641218. [DOI] [PubMed] [Google Scholar]
- Vidon N., Evard D., Godbillon J., Rongier M., Duval M., Schoeller J. P., Bernier J. J., Hirtz J. Investigation of drug absorption from the gastrointestinal tract of man. II. Metoprolol in the jejunum and ileum. Br J Clin Pharmacol. 1985;19 (Suppl 2):107S–112S. doi: 10.1111/j.1365-2125.1985.tb02750.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
