Reference : Contribution of cyclodextrins in the developement of different pharmaceutical formula...
Scientific journals : Article
Physical, chemical, mathematical & earth Sciences : Chemistry
Human health sciences : Pharmacy, pharmacology & toxicology
http://hdl.handle.net/2268/18669
Contribution of cyclodextrins in the developement of different pharmaceutical formulations of a nex matrix metalloproteinase inhibitor
English
Evrard, Brigitte mailto [Université de Liège - ULg > Département de pharmacie > Pharmacie galénique >]
Bertholet, Pascal [> >]
Guéders, Maud mailto [Université de Liège - ULg > Département des sciences cliniques > Labo de biologie des tumeurs et du développement >]
Piette, Marie mailto [Université de Liège - ULg > Département de pharmacie > Pharmacie galénique >]
Piel, Géraldine mailto [Université de Liège - ULg > Département de pharmacie > Pharmacie galénique >]
Cataldo, Didier mailto [Université de Liège - ULg > Département des sciences biomédicales et précliniques > Biochimie et physiologie générales, humaines et path. >]
Delattre, Luc mailto [Université de Liège - ULg > Département de pharmacie > Département de pharmacie >]
2007
Journal of Inclusion Phenomena and Molecular Recognition in Chemistry
Springer
57
1-4
303-308
Yes (verified by ORBi)
International
0923-0750
Dordrecht
Netherlands
[en] bioavailability ; cyclodextrins ; inhibitro ; matrix metalloproteases ; pharmacokinetics ; pulmonary administration ; solubility ; Ro 28-2653
[en] Ro 28-2653 is a new synthetic inhibitor of matrix metalloproteinases. The ability of these enzymes to degrade various components of the extracellular matrix seems to play a major role in tumors progression and is potentially effective against bronchial remodeling in asthma and BPCO. Ro 28-2653 is very poorly soluble in water. This low solubility estimated at about 0.56 lg/ml in water at 25 C gives rise to difficulties in pharmaceutical formulation of oral, injectable or
<br />nebulizable solutions. The purpose of our study is to prepare and to characterize inclusion complexes between Ro 28-2653 and cyclodextrins and to investigate the biopharmaceutical repercussion of the inclusion of the active substance.The complex formation was investigated by phase solubility studies. 1H-NMR spectroscopy and molecular modeling studies were carried out to elucidate the structure of the inclusion
<br />complex between Ro 28-2653 and cyclodextrin. Oral, intravenous and nebulizable solutions of Ro 28-2653 were developed with cyclodextrin. The in vivo studies were performed on healthy sheep for the pharmacokinetic evaluation of the oral and intravenous formulations while the nebulization of the complex solution was studied by using an asthma model in mouse.
Researchers ; Professionals
http://hdl.handle.net/2268/18669
also: http://hdl.handle.net/2268/73286

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