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Enhanced bioavailability of piroxicam via salt formation with ethanolamines

Title
Enhanced bioavailability of piroxicam via salt formation with ethanolamines
Authors
Gwak H.-S.Choi J.-S.Choi H.-K.
Ewha Authors
곽혜선
Issue Date
2005
Journal Title
International Journal of Pharmaceutics
ISSN
0378-5173JCR Link
Citation
International Journal of Pharmaceutics vol. 297, no. 41276, pp. 156 - 161
Indexed
SCI; SCIE; SCOPUS WOS scopus
Document Type
Article
Abstract
Piroxicam can be ionized as a zwitterion that has two pKa values (pKa 1 = 1.86 and pKa2 = 5.46). Consequently, piroxicam has a low solubility in both polar and nonpolar media, and a low lipophilicity, which results in a low permeability. Three piroxicam-ethanolamine salts were prepared, which had a higher area under the curve (AUC) than piroxicam. There were minimal differences in the AUC among the salt forms. It was reported that the piroxicam triethanolamine salt had a lower permeability across the skin than piroxicam but it had a higher oral bioavailability. Piroxicam monoethanolamine showed the highest Cmax followed by piroxicam diethanolamine and piroxicam triethanolamine. The dissolution rates of piroxicam and its salts were similar at pH 1.2. Piroxicam monoethanolamine showed the highest dissolution rate at pH 6.8, which was followed by the piroxicam diethanolamine and piroxicam triethanolamine salts. The order of dissolution rate at pH 6.8 matched the order of Cmax or the AUC after oral administration. © 2005 Elsevier B.V. All rights reserved.
DOI
10.1016/j.ijpharm.2005.03.016
Appears in Collections:
약학대학 > 약학과 > Journal papers
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