Reference : Study of the Influence of Both Cyclodextrins and L-Lysine on the Aqueous Solubility o...
Scientific journals : Article
Human health sciences : Pharmacy, pharmacology & toxicology
http://hdl.handle.net/2268/18512
Study of the Influence of Both Cyclodextrins and L-Lysine on the Aqueous Solubility of Nimesulide; Isolation and Characterization of Nimesulide-L-Lysine-Cyclodextrin Complexes
English
Piel, Géraldine mailto [Université de Liège - ULg > Département de pharmacie > Pharmacie galénique et magistrale >]
Pirotte, Bernard mailto [Université de Liège - ULg > > Chimie pharmaceutique >]
Delneuville, Isabelle [> > > >]
Neven, Philippe [> > > >]
Llabres, Gabriel mailto [Université de Liège - ULg > Département de physique > Département de physique >]
Delarge, Jacques [> > > >]
Delattre, Luc mailto [Université de Liège - ULg > Département de pharmacie > Département de pharmacie >]
Apr-1997
Journal of Pharmaceutical Sciences
Wiley Interscience
86
4
475-80
Yes (verified by ORBi)
International
0022-3549
[en] Nimesulide is a nonsteroidal antiinflammatory drug that exhibits a very poor water solubility (0.01 mg.mL-1). A nimesulide-beta-cyclodextrin complex prepared according to patent application WO 94/ 02177 has an aqueous solubility of approximately 16 mg.mL-1 of nimesulide. A nimesulide-L-lysine salt has also been prepared and increases the aqueous solubility of nimesulide to approximately 5.0-7.5 mg.mL-1. The purpose of the present study was to investigate the interaction of both cyclodextrins and L-lysine on the aqueous solubility of nimesulide. Nimesulide-L-lysine-beta- or gamma-cyclodextrin complexes were prepared by spray-drying. The inclusion of the nimesulide-L-lysine salt into the cyclodextrin cavity was confirmed by differential scanning calorimetry and proton nuclear magnetic resonance spectroscopy. These complexes offered remarkable aqueous solubility. The incorporation of nimesulide in a nimesulide-L-lysine-beta-cyclodextrin complex increased its water solubility by a factor of 10 at pH 1.5 (0.050 mg.mL-1 for the complex versus 0.005 mg.mL-1 for nimesulide), 160 at pH 6.8 (2.373 mg.mL-1 for the complex versus 0.015 mg.mL-1 for nimesulide), and 3600 in purified water (36.400 mg.mL-1 for the complex versus 0.01 mg.mL-1 for nimesulide).
Researchers ; Professionals
http://hdl.handle.net/2268/18512
also: http://hdl.handle.net/2268/31175
10.1021/js960298k

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