title: Polymorphism of glyceryl behenates: from the individual compounds to the pharmaceutical excipient.
abstract: The present paper deals with the crystallization behavior of glyceryl behenate mixtures that are extensively used in the field of drug delivery. The aim of the study was to understand the structural and thermal behaviors of Compritol(®) by considering first the individual polymorphism of the main components constituting this excipient and then their mixtures. This excipient mainly contains dibehenin (∼50%), tribehenin (∼30%) and monobehenin (20%). It appeared clearly that the mixture polymorphism did not result from a simple addition of the individual behavior. Indeed, the solid state organization of this excipient strongly depended on the presence of the third main component, monobehenin, into the mixture. Furthermore, a threshold ratio of monobehenin, at least 10%, must be reach in order to obtain the typical structural organization (co-existence of α/sub-α subcells) and thermal behavior (solid-solid transition and melting) of Compritol(®). This underlines that special attention is required when mixing Compritol(®) with other pharmaceutical ingredients that could trap monoglycerides and modify the equilibrium present in the pure excipient.
authors: Université Paris-Sud, Institut Galien - UMR CNRS 8612, 5 Rue J.B. Clément, Châtenay-Malabry 92290, France.
authors: Perrine
authors: P
authors: Pivette
authors: Université Paris-Sud, Institut Galien - UMR CNRS 8612, 5 Rue J.B. Clément, Châtenay-Malabry 92290, France. Electronic address: vincent.faivre@u-psud.fr.
authors: Vincent
authors: V
authors: Faivre
authors: Synchrotron Soleil, L'Orme des Merisiers, Saint-Aubin 91190, France.
authors: Jean-Blaise
authors: JB
authors: Brubach
authors: Sanofi, 1 Rue de la Vierge, Carbon Blanc Cedex 33 565, France.
authors: Georges
authors: G
authors: Daste
authors: Université Paris-Sud, Institut Galien - UMR CNRS 8612, 5 Rue J.B. Clément, Châtenay-Malabry 92290, France.
authors: Michel
authors: M
authors: Ollivon
authors: Université Paris-Sud, Institut Galien - UMR CNRS 8612, 5 Rue J.B. Clément, Châtenay-Malabry 92290, France.
authors: Sylviane
authors: S
authors: Lesieur
mesh_terms: D003460:Crystallization / Q000379:methods*; D005079:Excipients / Q000737:chemistry*; D005227:Fatty Acids / Q000737:chemistry*; D050178:Monoglycerides / Q000737:chemistry*; D044367:Phase Transition; D013814:Thermal Conductivity
chemical_list: D005079:Excipients; D005227:Fatty Acids; D050178:Monoglycerides; C086409:glyceryl behenate
keywords: Calorimetry; Compritol(®); Dibehenin; Glyceryl behenates; Polymorphism; X-ray diffraction