PMID: 8094244Jan 1, 1993Paper

Regional gastrointestinal absorption of the beta-blocker pafenolol in the rat and intestinal transit rate determined by movement of 14C-polyethylene glycol (PEG) 4000

Pharmaceutical Research
H Lennernäs, C G Regårdh

Abstract

The gastrointestinal absorption characteristics of pafenolol following oral administration as a solution in man and rat has previously been found to be a double-peak phenomenon and exhibited dose-dependent bioavailability, despite negligible presystemic metabolism. In both man and rat the first peak appeared approximately 0.5-1 hr postdose and the second, more pronounced peak 3-4 hr postdose. In rat more than 90% of the available dose was absorbed during the second peak. In the present study we investigated the absorption of a solution of pafenolol in rats after intrajejunal and intraileal administration. The resulting blood concentration-time profile of pafenolol exhibited one peak only; the extent of absorption was similar to that observed when the same dose was given orally. The small intestinal transit time of the 14C-PEG 4000 solution was found to be more than 3 hr. The transit rate was higher in the proximal part of the small intestine compared to the more distal part, where the transit of the solution was staggered. In conclusion, the results of the intestinal transit time investigation and the administrations of pafenolol at different levels of the alimentary tract indicate that pafenolol is a drug with a specific absor...Continue Reading

Citations

Feb 21, 2002·Biological & Pharmaceutical Bulletin·Toshikiro Kimura, Kazutaka Higaki
Feb 2, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ping QianXiu-Wei Yang
May 21, 2010·Clinical Pharmacokinetics·Neal M DaviesJaime A Yáñez
May 23, 1998·Annual Review of Pharmacology and Toxicology·L ZhangK M Giacomini
Jan 15, 2011·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Shinji YamashitaYasuyoshi Watanabe
May 16, 2021·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Jong Bong LeePavel Gershkovich

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