Determining Drug Release From Compritol® 888 Atomatrix Formulations

Lars Kühnemund1, Delphine Marchaud2, Elise Dauphin2, Jean-Michel Girard2, Cédric Miolane2, Yvonne Cuppok2, Grzegorz Garbacz1-3, Sandra Klein1, 1 Center of Drug Absorption and Transport, Ernst Moritz Arndt University Greifswald, Felix Hausdorff St. 3, 17489 Greifswald, Germany, email: [email protected], 2Gattefosse SAS, Chemin de Genas, BP603-F69804 Saint-Priest, France, email: [email protected], 3Physiolution GmbH, Walther-Rathenau-St. 49a, 17489 Greifswald, Germany


The development and use of in vitro biorelevant dissolution tests is becoming more and more relevant since in depth understanding of the in vivo dissolution behaviour of solid dosage forms - being subject to high mechanical stress and food effects throughout gastrointestinal passage - is highly desirable. Biorelevant dissolution tests will eventually be integrated into quality control procedures in formulation development and drug production since it will be essential to assure robust and reproducible oral drug delivery systems in conditions that more closely match the physiological environment.

Such tests may identify unmet needs – and therefore offer opportunities - in terms of excipients, drug delivery and dosage form development.

The objective of this study is to evaluate the robustness of lipid matrix tablets in biorelevant dissolution test systems which simulate passage through the human gastrointestinal (GI) tract. Compritol® 888 ATO (glyceryl dibehenate), the matrix former, is a fine white powder composed of spherical particles with a mean particle diameter of 50μm.

It has excellent tabletting properties and is chemically inert and neutral in flavour. With a low HLB of 1 and a high melting point (70°C) it has proven utility in the production of an insoluble and non-swellable matrix which sustains drug release principally by a mechanism of diffusion [1].