Article (Scientific journals)
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
Piel, Géraldine; Pirotte, Bernard; Delneuville, Isabelle et al.
1997In Journal of Pharmaceutical Sciences, 86 (4), p. 475-80
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Abstract :
[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).
Disciplines :
Pharmacy, pharmacology & toxicology
Author, co-author :
Piel, Géraldine ;  Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique et magistrale
Pirotte, Bernard ;  Université de Liège - ULiège > Chimie pharmaceutique
Delneuville, Isabelle
Neven, Philippe
Llabres, Gabriel ;  Université de Liège - ULiège > Département de physique > Département de physique
Delarge, Jacques
Delattre, Luc ;  Université de Liège - ULiège > Département de pharmacie > Département de pharmacie
Language :
English
Title :
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
Publication date :
April 1997
Journal title :
Journal of Pharmaceutical Sciences
ISSN :
0022-3549
eISSN :
1520-6017
Publisher :
Wiley Interscience
Volume :
86
Issue :
4
Pages :
475-80
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBi :
since 11 August 2009

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