Vacuum Compression Molding as a Screening Tool to Investigate Carrier Suitability for Hot-Melt Extrusion Formulations

Abstract

Hot-melt extrusion (HME) is the most preferred and effective method for manufacturing amorphous solid dispersions at production scale, but it consumes large amounts of samples when used for formulation development. Herein, we show a novel approach to screen the polymers by overcoming the disadvantage of conventional HME screening by using a minimum quantity of active pharmaceutical ingredient (API). Vacuum Compression Molding (VCM) is a fusion-based method to form solid specimens starting from powders. This study aimed to investigate the processability of VCM for the creation of amorphous formulations and to compare its results with HME-processed formulations. Mixtures of indomethacin (IND) with drug carriers (Parteck® MXP, Soluplus®, Kollidon® VA 64, Eudragit® EPO) were processed using VCM and extrusion technology. Thermal characterization was performed using differential scanning calorimetry, and the solid-state was analyzed via X-ray powder diffraction. Dissolution studies in the simulated gastric fluid were performed to evaluate the drug release. Both technologies showed similar results proving the effectiveness of VCM as a screening tool for HME-based formulations.

Eudragit®: A Versatile Family of Polymers for Hot Melt Extrusion and 3D Printing Processes in Pharmaceutics

“…Eudragit polymers presenting pH-dependent solubility have also been used to formulate ASDs, depending on the site of action, or in other words, where the drug should be released from the polymeric material. EE is soluble at pH < 5 and has been used to promote gastric release [ 52 , 68 ], whereas E 4155F, which is soluble at pH > 7, has been used for colonic delivery, as the ionization of the free carboxylic acid groups occurs mainly at pH > 7 [ 77 ].…”

Linear and branched polymer prodrugs of the water-soluble nucleoside reverse-transcriptase inhibitor emtricitabine as structural materials for long-acting implants

“…Vacuum compression moulding (VCM) has recently been reported as a screening tool for excipients in hot-melt extrusion processes. 30 The VCM process applies relatively low temperatures to fuse powders together into homogeneous solid structures whilst applying a vacuum to apply a 150 N force and remove gases to avoid bubble entrapment, Fig. 6 .…”

3D Printed Mini-Floating-Polypill for Parkinson’s Disease: Combination of Levodopa, Benserazide, and Pramipexole in Various Dosing for Personalized Therapy

“…To compare the release profiles of different sustained release (SR) polymers under the same conditions, molten platelets were prepared with vacuum compression molding (VCM, MeltPrep GmbH, Graz, Austria) technology [ 75 ]. The resulting platelets had the same surface area (SA) and volume (V), so that the SA/V ratio did not influence the release profile.…”