Polymorphism of glyceryl behenates: From the individual compounds to the pharmaceutical excipient

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(R) by considering first the individual polymorphism of the main components constituting this excipient and then their mixtures. This excipient mainly contains dibehenin (similar to 50%), tribehenin (similar to 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 alpha/sub-alpha subcells) and thermal behavior (solid-solid transition and Melting) of Compritol(R). This underlines that special attention is required when mixing Compritol(R) with other pharmaceutical ingredients that could trap monoglycerides and modify the equilibrium present in the pure excipient. (C) 2014 Elsevier Ireland Ltd. All rights reserved.