Evidence for Intestinal Secretion as an Additional Clearance Pathway of Talinolol Enantiomers: Concentration- and Dose-dependent Absorption in Vitro and in ... View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

1996-04

AUTHORS

Ulrike Wetterich, Hildegard Spahn-Langguth, Ernst Mutschler, Bernd Terhaag, Wolfgang Rösch, Peter Langguth

ABSTRACT

PURPOSE: To evaluate carrier-mediated intestinal secretion of talinolol enantiomers in vivo and in vitro. METHODS: In clinical studies with i.v. and p.o. dosage of rac-talinolol (30 mg and 100 mg, resp.) performed in a small number of cholecystectomized patients total and partial clearances were determined on the basis of plasma, bile and urine concentrations. The dose-dependence of AUC was investigated in 12 healthy volunteers (25, 50, 100, and 400 mg rac-talinolol as single p.o. doses). Concentration-dependence of the permeability across Caco-2 cell monolayers included concentrations from 0.1 to 2.0 mM, inhibition by verapamil was tested at 0.5 mM. RESULTS: The total clearance as well as the apparent oral clearance (CL/F) were slightly higher for S-(-)- than for R-(+)-talinolol. Calculation of the partial clearances showed that also the residual clearance was higher for the S- than for the R-enantiomer. In the healthy volunteers, CL/F increased with increasing doses, while the S/R ratio decreased approaching unity for the highest dose. Also the results from Caco-2 cell permeation studies yielded a clear concentration-dependence with decreasing stereoselectivity for the higher concentration range. Permeability of both enantiomers was considerably higher for b-->a than a-->b transport, however, this difference disappeared when verapamil was added. CONCLUSIONS: Although not very expressed, the detected stereoselectivities indicate a preferential absorption of R-(+)-talinolol in a lower concentration and dose range, which is most probably due to a moderate stereoselectivity at the carrier system involved in intestinal secretion. More... »

PAGES

514-522

Identifiers

URI

http://scigraph.springernature.com/pub.10.1023/a:1016029601311

DOI

http://dx.doi.org/10.1023/a:1016029601311

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1044138980

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/8710739


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52 schema:description PURPOSE: To evaluate carrier-mediated intestinal secretion of talinolol enantiomers in vivo and in vitro. METHODS: In clinical studies with i.v. and p.o. dosage of rac-talinolol (30 mg and 100 mg, resp.) performed in a small number of cholecystectomized patients total and partial clearances were determined on the basis of plasma, bile and urine concentrations. The dose-dependence of AUC was investigated in 12 healthy volunteers (25, 50, 100, and 400 mg rac-talinolol as single p.o. doses). Concentration-dependence of the permeability across Caco-2 cell monolayers included concentrations from 0.1 to 2.0 mM, inhibition by verapamil was tested at 0.5 mM. RESULTS: The total clearance as well as the apparent oral clearance (CL/F) were slightly higher for S-(-)- than for R-(+)-talinolol. Calculation of the partial clearances showed that also the residual clearance was higher for the S- than for the R-enantiomer. In the healthy volunteers, CL/F increased with increasing doses, while the S/R ratio decreased approaching unity for the highest dose. Also the results from Caco-2 cell permeation studies yielded a clear concentration-dependence with decreasing stereoselectivity for the higher concentration range. Permeability of both enantiomers was considerably higher for b-->a than a-->b transport, however, this difference disappeared when verapamil was added. CONCLUSIONS: Although not very expressed, the detected stereoselectivities indicate a preferential absorption of R-(+)-talinolol in a lower concentration and dose range, which is most probably due to a moderate stereoselectivity at the carrier system involved in intestinal secretion.
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