Document Detail


No effect of albumin on the dermal absorption rate of hydrocortisone 21-butyrate, permethrin or diflunisal in the isolated, single-pass perfused rabbit ear.
MedLine Citation:
PMID:  8990508     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Rabbit ears were single-pass perfused with a buffer solution containing either 6% hetastarch or 5% bovine serum albumin. Hydrocortisone 21-butyrate (5 mM), diflunisal (17 mM) or permethrin (33 mM) was added to isopropyl myristate with 5% polyethylene, and applied to about 40% of the epithelial surface area of the ear. Hydrocortisone 21-butyrate or permethrin were not found in the effluent with hetastarch or albumin. Following cutaneous ester hydrolysis, the appearance rate of hydrocortisone was about 4 pmol/min per cm2 in the hetastarch- or the albumin-containing buffer solution. No hydrolysis of permethrin was detected; the appearance rate of 3-phenoxybenzyl alcohol with 3-phenoxybenzoic acid corresponded to the absorption rate of the substrate impurities. During ex vivo perfusion of intact skin, serum albumin in the perfusion fluid may not enhance the appearance rate of xenobiotics in the effluent following dermal application when the distribution coefficient n-octanol/water is > 2,000 or when the xenobiotic is ionized at physiological pH. In general, for all substances investigated with our perfusion model thus far, the appearance rates decreased with rising distribution coefficient (n-octanol/buffer pH 7.4). High lipophilicity hinders the release from isopropyl myristate and the penetration through the skin.
Authors:
G E Bast; H G Kampffmeyer
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Skin pharmacology : the official journal of the Skin Pharmacology Society     Volume:  9     ISSN:  1011-0283     ISO Abbreviation:  Skin Pharmacol.     Publication Date:  1996  
Date Detail:
Created Date:  1997-07-08     Completed Date:  1997-07-08     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  8810069     Medline TA:  Skin Pharmacol     Country:  SWITZERLAND    
Other Details:
Languages:  eng     Pagination:  327-33     Citation Subset:  IM    
Affiliation:
Walther Straub Institute for Pharmacology and Toxicology, Faculty of Medicine, Ludwig Maximilians University, Munich, Germany.
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MeSH Terms
Descriptor/Qualifier:
Administration, Cutaneous
Administration, Topical
Animals
Anti-Inflammatory Agents / chemistry,  pharmacokinetics*
Anti-Inflammatory Agents, Non-Steroidal / chemistry,  pharmacokinetics*
Cattle
Chemistry, Physical
Diflunisal / chemistry,  pharmacokinetics*
Drug Interactions
Ear, External
Hydrocortisone / analogs & derivatives*,  chemistry,  pharmacokinetics
Ointments
Perfusion
Permethrin
Physicochemical Phenomena
Pyrethrins / chemistry,  pharmacokinetics*
Rabbits
Serum Albumin, Bovine / pharmacology*
Skin Absorption / drug effects*
Solubility
Chemical
Reg. No./Substance:
0/Anti-Inflammatory Agents; 0/Anti-Inflammatory Agents, Non-Steroidal; 0/Ointments; 0/Pyrethrins; 0/Serum Albumin, Bovine; 22494-42-4/Diflunisal; 50-23-7/Hydrocortisone; 52645-53-1/Permethrin; 6677-99-2/hydrocortisone 21-butyrate

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


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