Hot-melt co-extrusion for the production of fixed-dose combination products with a controlled release ethylcellulose matrix core.

In this study, hot-melt co-extrusion was evaluated as a technique for the production of fixed-dose combination products, using ethylcellulose as a core matrix former to control the release of metoprolol tartrate and a polyethylene oxide-based coat formulation to obtain immediate release of hydrochlorothiazide. By lowering the concentration of the hydrophilic additive polyethylene oxide in the plasticized ethylcellulose matrix or by lowering the drug load, the in vitro metoprolol tartrate release from the core was substantially sustained. The in vitro release of hydrochlorothiazide from the polyethylene oxide/polyethylene glycol coat was completed within 45 min for all formulations.

Hot-melt co-extrusion: requirements, challenges and opportunities for pharmaceutical applications.

Objectives: Co-extrusion implies the simultaneous hot-melt extrusion of two or more materials through the same die, creating a multi-layered extrudate. It is an innovative continuous production technology that offers numerous advantages over traditional pharmaceutical processing techniques. This review provides an overview of the co-extrusion equipment, material requirements and medical and pharmaceutical applications.

Development of injection moulded matrix tablets based on mixtures of ethylcellulose and low-substituted hydroxypropylcellulose.

The objective of this study was to produce sustained-release matrix tablets by means of injection moulding and to evaluate the influence of matrix composition, process temperature and viscosity grade of ethylcellulose on processability and drug release by means of a statistical design. The matrix tablets were physico-chemically characterized and the drug release mechanism and kinetics were studied. Formulations containing metoprolol tartrate (30%, model drug), ethylcellulose with dibutylsebacate (matrix former and plasticizer) and L-HPC were extruded and subsequently injection moulded into tablets (375mg, 10mm diameter, convex-shaped) at different temperatures (110, 120 and 130 degrees C).

Mixture design applied to optimize a directly compressible powder produced via cospray drying.

Coprocessing via spray drying was applied to improve the compactability of acetaminophen and to select an optimal formulation. Four-component mixtures containing acetaminophen, mannitol, erythritol, and maltodextrin were produced by cospray drying. A D-optimal mixture design was constructed to evaluate the spray dried powder and tablet properties.

Coprocessing via spray drying as a formulation platform to improve the compactability of various drugs.

It was evaluated if coprocessing via spray drying can be used as a formulation platform to improve the compactability of formulations containing drug substance (acetaminophen, ibuprofen, cimetidine) and excipients (carbohydrates, disintegrant, glidant, surfactant). Experimental design was applied to optimise the drug concentration and solid content of the feed suspension. In addition, scaling-up of acetaminophen- and ibuprofen-containing formulations was performed on a production-scale spray dryer.