Document Detail

Pharmacokinetics of formulated tenoxicam transdermal delivery systems.
MedLine Citation:
PMID:  18088513     Owner:  NLM     Status:  MEDLINE    
To investigate the feasibility of developing a new tenoxicam transdermal delivery system (TDS), the pharmacokinetics of tenoxicam from various formulated TDS were evaluated and compared with values following oral administration of tenoxicam and with application of a piroxicam plaster (Trast) marketed in Korea. Based on previous in-vitro study results, a mixture of diethylene glycol monoethyl ether (DGME) and propylene glycol monolaurate (PGML) (40:60) was used as a vehicle, and caprylic acid, capric acid, lauric acid, oleic acid or linoleic acid (each at 3%) was added as an enhancer. Triethanolamine (5%) was used as a solubilizer, and Duro-Tak 87-2510 as a pressure-sensitive adhesive. Among these fatty acids used for the formulation of tenoxicam TDS, caprylic acid showed the greatest enhancing effect; the area under the plasma concentration-time profile (AUC) decreased in the order of caprylic acid>linoleic acid>or=oleic acid>lauric acid>capric acid. Compared with oral administration, maximum plasma concentration (Cmax) was significantly lower, and time to reach Cmax (Tmax) delayed with all formulated tenoxicam TDS. All formulated TDS resulted in a lower AUC than with the oral formulation, except for TDS containing caprylic acid, although the difference was statistically significant only with capric acid. The AUC for all the formulated tenoxicam TDS was significantly higher than that of the piroxicam plaster; TDS with caprylic acid increased AUC 8.53-fold compared with the piroxicam plaster. Even though the Tmax of tenoxicam TDS was not significantly different from that of the piroxicam plaster, Cmax was higher; formulations containing caprylic acid and linoleic acid increased Cmax by 7.39- and 8.76-fold, respectively. In conclusion, a formulation containing 1.5 mL DGME-PGML (40:60) with 3% caprylic acid and 5% triethanolamine mixed with 6 g Duro-Tak 87-2510 could be a good candidate for developing a new tenoxicam TDS to maintain a comparable extent of absorption to oral delivery while attaining a prolonged effect with fewer toxic events.
Taekyung Kim; Eunyoung Kang; Inkoo Chun; Hyesun Gwak
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  The Journal of pharmacy and pharmacology     Volume:  60     ISSN:  0022-3573     ISO Abbreviation:  J. Pharm. Pharmacol.     Publication Date:  2008 Jan 
Date Detail:
Created Date:  2007-12-19     Completed Date:  2008-05-12     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0376363     Medline TA:  J Pharm Pharmacol     Country:  England    
Other Details:
Languages:  eng     Pagination:  135-8     Citation Subset:  IM    
College of Pharmacy, Ewha Womans University, 11-1 Daehyun-Dong Seodaemun-Gu Seoul 120-750, Korea.
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MeSH Terms
Acrylates / chemistry
Administration, Cutaneous
Administration, Oral
Anti-Inflammatory Agents, Non-Steroidal / administration & dosage,  blood,  pharmacokinetics
Area Under Curve
Chemistry, Pharmaceutical / methods*
Chromatography, High Pressure Liquid
Decanoic Acids / chemistry
Drug Delivery Systems / methods
Ethanolamines / chemistry
Ethylene Glycols / chemistry
Lauric Acids / chemistry
Linoleic Acid / chemistry
Octanoic Acids / chemistry
Oleic Acid / chemistry
Piroxicam / analogs & derivatives*,  chemistry,  pharmacokinetics
Rats, Sprague-Dawley
Technology, Pharmaceutical / methods
Tissue Distribution
Vehicles / chemistry
Reg. No./Substance:
0/Acrylates; 0/Anti-Inflammatory Agents, Non-Steroidal; 0/Decanoic Acids; 0/Ethanolamines; 0/Ethylene Glycols; 0/Lauric Acids; 0/Octanoic Acids; 0/Vehicles; 102-71-6/triethanolamine; 111-90-0/carbitol; 112-80-1/Oleic Acid; 124-07-2/caprylic acid; 143-07-7/lauric acid; 2197-37-7/Linoleic Acid; 334-48-5/decanoic acid; 36322-90-4/Piroxicam; 59804-37-4/tenoxicam

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

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