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Vol. 122, No. 2, 2000
Issue release date: June 2000
Section title: Original Paper
Int Ach Allergy Immunol 2000;122:151–154
(DOI:10.1159/000024371)

Binding of Glucocorticoids to Human Nasal Tissue in vitro

Esmailpour N. · Högger P. · Rohdewald P.
Institute of Pharmaceutical Chemistry, Westfälische Wilhelms-Universität Münster, Germany

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Article / Publication Details

First-Page Preview
Abstract of Original Paper

Published online: 6/27/2000
Issue release date: June 2000

Number of Print Pages: 4
Number of Figures: 4
Number of Tables: 0

ISSN: 1018-2438 (Print)
eISSN: 1423-0097 (Online)

For additional information: http://www.karger.com/IAA

Abstract

Background: Intranasal application of glucocorticoids is an efficacious treatment of allergic rhinitis and some cases of nonallergic rhinitis. However, no data on binding of glucocorticoids to nasal tissue are available. Pronounced binding of the compound to the target tissue is favorable as it might serve as a local deposit delivering the glucocorticoid to specific receptors and it slows down the efflux of the compound into systemic circulation. Methods: Human nasal tissue was incubated with fluticasone propionate, budesonide, flunisolide and beclomethasone-17-monopropionate. Kinetics of binding and redistribution of the tissue-bound fraction into human plasma was monitored. Results: Binding of glucocorticoids to human nasal tissue was fast and highest for the lipophilic fluticasone propionate, followed by beclomethasone-17-monopropionate. Also, highest concentrations of these lipophilic glucocorticoids remained in nasal tissue after equilibration of drug-saturated tissue with plasma. Conclusions: Lipophilic compounds exhibit a high tissue binding and retention which is an important property of topically applied glucocorticoids. It is the basis for prolonged action and low concentration of the compound in systemic circulation.

© 2000 S. Karger AG, Basel


  

Author Contacts

Correspondence to: Prof. Dr. Peter Rohdewald
Institute of Pharmaceutical Chemistry
Westfälische Wilhelms-Universität
Hittorfstrasse 58–62, D–48149 Münster (Germany)
Tel. +49 251 833 3347, Fax +49 251 833 2144

  

Article Information

Received: Received: December 16, 1999
Accepted after revision: March 17, 2000
Number of Print Pages : 4
Number of Figures : 4, Number of Tables : 0, Number of References : 6

  

Publication Details

International Archives of Allergy and Immunology
Founded 1950

Vol. 122, No. 2, Year 2000 (Cover Date: June 2000)

Journal Editor: D. Kraft, Vienna
ISSN: 1018–2438 (print), 1423–0097 (Online)

For additional information:http://www.karger.com/journals/iaa


Article / Publication Details

First-Page Preview
Abstract of Original Paper

Published online: 6/27/2000
Issue release date: June 2000

Number of Print Pages: 4
Number of Figures: 4
Number of Tables: 0

ISSN: 1018-2438 (Print)
eISSN: 1423-0097 (Online)

For additional information: http://www.karger.com/IAA


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Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in goverment regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug.
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