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KMID : 0369820060360030169
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Jorunal of Korean Pharmaceutical Sciences
2006 Volume.36 No. 3 p.169 ~ p.174
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Preparation of Tenoxicam Salt with Ethanolamine to Enhance the Percutaneous Absorption
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곽병태/Gwak BT
전명관/최후균/Chun MK/Choi HK
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Abstract
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The aim of this work was to prepare tenoxicam-ethanolamine salt with improved physicochemical properties for transdermal application. Tenoxicam-ethanolamine salt was prepared in methylene chloride and its physicochemical properties were investigated by DSC and FT-lR. The broad peak of tenoxicam around 3600-3200 cm?1 was shifted to lower wavenumber and more broadened. The characteristic endothermic melting peak of tenoxicam appeared at 223?C. The melting peak of tenoxicam-ethanolamine salt was shifted to 159?C. In contrast to relatively small difference in the partition coefficients of tenoxicam and the tenoxicam-ethanolamine salt, large difference in aqueous solubility was observed. Crovol® PK4O (PEG-12 palm kernel glycerides) provided the highest skin flux for both compounds. The order of the enhancing effect of the various vehicles tested was similar for tenoxicam and tenoxicam-ethanolamine salt, which indicated that their enhancing mechanism for tenoxicam and tenoxicam-ethanolamine salt is similar. Tenoxicam-ethanolamine salt had a higher skin flux than tenoxicam by 1.2- to 31.7-fold, depending on the vehicles used. It is suggested that the vehicles with medium HLB value, 1 double bond, and lower ethylene oxide chain length have a better ability to modify the permeability of the stratum corneum and to promote the effective penetration of tenoxicam and tenoxicam-ethanolamine salt.
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KEYWORD
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Tenoxicam, Ethanolamine, Salt, Percutaneous, Enhancer, Solubility
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