Document Detail


Effect of vehicles and penetration enhancers on the in vitro percutaneous absorption of celecoxib through human skin.
MedLine Citation:
PMID:  12779049     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The aim of this study was the comparison of three different formulations (gel, o/w emulsion, oleagenous cream) and two penetration enhancers (oleic acid and menthol) as vehicle systems for celecoxib in respect of release and penetration through excised human skin in vitro. The influence of the vehicle on the release rate was studied in vitro using a cellulose acetate membrane. The release rate could be increased by up to 6.5 and 2.5 times with gel and o/w emulsion compared to oleagenous cream respectively. Further in vitro penetration measurements using human skin on Franz diffusion cells were performed with and without oleic acid and menthol as enhancers. It was shown that the penetration rate is strongly dependent upon the enhancer type and concentration but not on the vehicle itself and could be increased by 48% when 5% oleic acid was used in oleagenous cream. In all formulations tested, celecoxib was released and penetrated into human skin more quickly and to a greater extent from the gel formulations. There is no topical formulation available of celecoxib and its penetration properties through human skin have not been investigated. Since celecoxib creates some gastrointestinal disturbances, topical formulations of celecoxib preferably in gel form including 5% oleic acid could be suggested as an alternative.
Authors:
G Yener; U Gönüllü; M Uner; T Değim; A Araman
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Die Pharmazie     Volume:  58     ISSN:  0031-7144     ISO Abbreviation:  Pharmazie     Publication Date:  2003 May 
Date Detail:
Created Date:  2003-06-03     Completed Date:  2004-04-02     Revised Date:  2007-01-29    
Medline Journal Info:
Nlm Unique ID:  9800766     Medline TA:  Pharmazie     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  330-3     Citation Subset:  IM    
Affiliation:
Istanbul University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Istanbul, Turkey. gulyen@superonline.com
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MeSH Terms
Descriptor/Qualifier:
Cyclooxygenase 2
Cyclooxygenase 2 Inhibitors
Cyclooxygenase Inhibitors / administration & dosage,  pharmacokinetics*
Emulsions
Gels
Humans
Isoenzymes / metabolism
Lactose / analogs & derivatives*
Membrane Proteins
Methylcellulose / analogs & derivatives*
Ointments
Oxazines
Prostaglandin-Endoperoxide Synthases / metabolism
Pyrazoles
Skin Absorption / drug effects*
Solubility
Spectrophotometry, Ultraviolet
Sulfonamides / administration & dosage,  pharmacokinetics*
Vehicles
Chemical
Reg. No./Substance:
0/Cyclooxygenase 2 Inhibitors; 0/Cyclooxygenase Inhibitors; 0/Emulsions; 0/Gels; 0/Isoenzymes; 0/Membrane Proteins; 0/Ointments; 0/Oxazines; 0/Pyrazoles; 0/Sulfonamides; 0/Vehicles; 169590-42-5/celecoxib; 63-42-3/Lactose; 9004-67-5/Methylcellulose; 99705-65-4/MK 458; EC 1.14.99.1/Cyclooxygenase 2; EC 1.14.99.1/PTGS2 protein, human; EC 1.14.99.1/Prostaglandin-Endoperoxide Synthases

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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