02. October 2018
The formulation of amorphous solid dispersions (ASDs) is an effective way to improve the bioavailability of poorly water-soluble active pharmaceutical ingredients (APIs). The combination of an amorphous state of the drug and the presence of crystallization-inhibiting polymers retains a high amount of dissolved API over time. ASDs with ketoconazole and different polymers were manufactured by spray drying and their characteristics as well as performance were analyzed. Dissolution tests with a...
13. September 2018
Herein we introduce an innovative process for preparation of directly compressible API and excipient agglomerates for extended release formulation of a highly water soluble drug, demonstrated with metformin HCl. Metformin is poorly compressible and currently employs wet granulation for tablet manufacturing, resulting in long cycle times. We have co-processed metformin HCl with hydroxypropyl methylcellulose (HPMC) and sodium carboxymethlycellulose (NaCMC) in solvent medium to generate...
04. August 2018
In this paper, we explain the crystallization process of mannitol during convective droplet drying based on the crystallization kinetics calculated from two mathematical models coupled with experimental investigations. A novel differential-reaction engineering approach was developed, correlating the mannitol crystallization behavior to the deviation of droplet drying kinetics at different drying temperatures. The model was compared with a conventional glass transition-based model and the...
13. March 2018
Mannitol/sucrose formulations are employed to generate lyophilizates for biopharmaceuticals with an elegant cake appearance. The aim of this study was to dry protein/mannitol/sucrose formulations as fast as possible without loss of cake appearance and protein stability. Glycerol was included as potential additional protein stabilizer. Three proteins (lysozyme and two monoclonal antibodies) at low and high concentration were analyzed comparing fast with conservative freeze-drying.
11. January 2018
Inhibit the fast surface crystallization of amorphous drugs with gelatin nano-coatings.
05. January 2018
Supercritical fluid (SCF) technology has been applied to drug product development over the last thirty years and drug particle generation using SCFs appears to be an efficient way to carry out drug formulation which will form end-products meeting targeted specifications.
25. May 2017
The alarming numbers of poorly soluble discovery compounds have centered the efforts towards finding strategies to improve the solubility. One of the attractive approaches to enhance solubility is via amorphization despite the stability issue associated with it
19. April 2017
Abstract We developed a step-by-step experimental protocol using differential scanning calorimetry (DSC), dynamic vapour sorption (DVS), polarized light microscopy (PLM) and a small-scale dissolution apparatus (μDISS Profiler) to investigate the mechanism (solid-to-solid or solution-mediated) by which crystallization of amorphous drugs occurs upon dissolution. This protocol then guided how to stabilize the amorphous formulation. Indapamide, metolazone, glibenclamide and glipizide were selected...
22. November 2016
Abstract The aim of this study was to prepare spherical agglomerates of lactose and to evaluate their physicochemical properties, flow properties, particle friability and compaction properties, and to compare them to commercially available types of lactose for direct compression (spray-dried, granulated and anhydrous β-lactose). Porous spherical agglomerates of α-lactose monohydrate with radially arranged prism-like primary particles were prepared exhibiting a high specific surface area. All...