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Pharmacokinetics of formulated tenoxicam transdermal delivery systems

Title
Pharmacokinetics of formulated tenoxicam transdermal delivery systems
Authors
Kim T.Kang E.Chun I.Gwak H.
Ewha Authors
곽혜선
SCOPUS Author ID
곽혜선scopus
Issue Date
2008
Journal Title
Journal of Pharmacy and Pharmacology
ISSN
0022-3573JCR Link
Citation
vol. 60, no. 1, pp. 135 - 138
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
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 ≥ oleic acid > lauric acid > capric acid. Compared with oral administration, maximum plasma concentration (C max) was significantly lower, and time to reach C max (T max) 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 T max of tenoxicam TDS was not significantly different from that of the piroxicam plaster, C max was higher; formulations containing caprylic acid and linoleic acid increased C max 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. © 2008 The Authors.
DOI
10.1211/jpp.60.1.0017
Appears in Collections:
약학대학 > 약학과 > Journal papers
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