title: Influence of cryogenic grinding on properties of a self-emulsifying formulation.
abstract: Recently, self-emulsifying drug delivery systems (SEDDS) have been developed as a method to deliver lipophilic drugs. Gelucire 44/14 is an excipient, from the lauroyl macrogolglycerides family, producing a fine oil-in-water emulsion when introduced into an aqueous phase under gentle agitation as SEDDS, improving thereby solubility of poorly water-soluble drugs and their bioavailability. The aims of this study were to process Gelucire 44/14 into a powder by cryogenic grinding to produce solid oral dosage forms and to investigate influence of this process on different properties of a formulation made of Gelucire 44/14 and ketoprofen (90/10). Cryogenic grinding produced Gelucire 44/14 in a powder form and this process did not change its physical properties, emulsification capacities and dissolution performances of the formulation tested. However, interactions took place between ketoprofen and Gelucire 44/14 with a decrease of the melting peak and a reduction of the droplet size of the formed emulsion. The influence of drug-Gelucire 44/14 interactions must be investigated case by case in any formulations.
authors.affiliation: Groupe Technologie des Poudres à Usage Pharmaceutique, Faculté de Pharmacie, Université de Bourgogne, 7 Boulevard Jeanne d'Arc, 21 079 Dijon Cedex, France.
authors.forename: O
authors.initials: O
authors.lastname: Chambin
authors.forename: V
authors.initials: V
authors.lastname: Jannin
authors.forename: D
authors.initials: D
authors.lastname: Champion
authors.forename: C
authors.initials: C
authors.lastname: Chevalier
authors.forename: M-H
authors.initials: MH
authors.lastname: Rochat-Gonthier
authors.forename: Y
authors.initials: Y
authors.lastname: Pourcelot
mesh_terms: D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems / Q000379:methods; D045703:Emulsifying Agents / Q000008:administration & dosage / Q000737:chemistry*; D005612:Freeze Drying; D008855:Microscopy, Electron, Scanning; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000737:chemistry*; D012995:Solubility / Q000187:drug effects; D013678:Technology, Pharmaceutical / Q000379:methods*
chemical_list: D045703:Emulsifying Agents; C104509:gelucire 44-14; D011092:Polyethylene Glycols