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Comparative assessment of effectiveness of ketoprofen and ketoprofen/beta-cyclodextrin complex in two experimental models of inflammation in rats.
MedLine Citation:
PMID:  24072487     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Oral administration of non-steroidal anti-inflammatory drugs (NSAIDs) can lead to adverse effects such as gastrointestinal distress. The complexation of different groups of active substances with β-cyclodextrin (β-CD) has drawn considerable interest over recent years. The purpose of this study was to analyze the ketoprofen/β-cyclodextrin (K/β-CD) conjugate complex as well as to assess its anti-inflammatory effect after oral administration (doses of 30 mg/m(2) and 15 mg/m(2) of body surface), compared with ketoprofen. The studies were done on two models of experimentally-induced acute inflammation in rats (n = 48, 6/group), by means of intraplantar administration of a 10% aqueous kaolin suspension and intraperitoneal administration of a 1% sodium thioglycolate solution. The dynamics of the acute inflammatory process and the anti-inflammatory effects were monitored using plethysmometric determinations after 3, 6, 9, 12, 24 and 48 h (plantar inflammation), and the absorbance of the exudates (spectrophotometrically read) and nucleated cell counts after 24 h (peritoneal inflammation). The coupling of ketoprofen with β-CD resulted in increased solubility (100% in 60 min) of the newly-formed product, which further resulted in a higher bioavailability compared with ketoprofen (<40% in 120 min). In both models of experimentally-induced inflammation, the K/β-CD complex had a higher anti-inflammatory activity than ketoprofen.
Authors:
Mariana Grecu; Valentin Nastasa; Cornelia Ilie; Liviu Miron; Mihai Mares
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-9-26
Journal Detail:
Title:  Laboratory animals     Volume:  -     ISSN:  1758-1117     ISO Abbreviation:  Lab. Anim.     Publication Date:  2013 Sep 
Date Detail:
Created Date:  2013-9-27     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0112725     Medline TA:  Lab Anim     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
Department of Pharmacology, University of Agricultural Sciences and Veterinary Medicine, Lasi, Romania.
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