Synthesis and transdermal penetration of NSAID glycoside esters

The glucoside and mannoside derivatives of the NSAIDs flurbiprofen, ibuprofen, ketoprofen and naproxen were synthesised and their penetration through human skin was determined. Experimental transdermal flux data showed that the parent NSAIDs penetrated human skin to a much higher extent than the gly...

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Veröffentlicht in:	International journal of pharmaceutics 2005-09, Vol.301 (1), p.71-79
Hauptverfasser:	Swart, Henk, Breytenbach, Jaco C., Hadgraft, Jonathan, Plessis, Jeanetta du
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Cutaneous Adult Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics Biological and medical sciences Catalysis Chromatography, High Pressure Liquid Esters - chemical synthesis Esters - pharmacokinetics Female Flurbiprofen General pharmacology Glucose - chemistry Glycoside Glycosides - chemical synthesis Glycosides - pharmacokinetics Humans Ibuprofen In Vitro Techniques Ketoprofen Mannose - chemistry Medical sciences Naproxen Octanols - chemistry Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Skin Absorption - physiology Solubility Spectrophotometry, Ultraviolet Structure-Activity Relationship Transdermal penetration Water - chemistry
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Zusammenfassung:	The glucoside and mannoside derivatives of the NSAIDs flurbiprofen, ibuprofen, ketoprofen and naproxen were synthesised and their penetration through human skin was determined. Experimental transdermal flux data showed that the parent NSAIDs penetrated human skin to a much higher extent than the glycosides.
ISSN:	0378-5173 1873-3476
DOI:	10.1016/j.ijpharm.2005.05.030