Effect of Liquid Load Level and Binder Type on the Tabletability of Mesoporous Silica Based Liquisolids.

Mesoporous silica offers an easy way to transform liquids into solids, due to their high loading capacity for liquid or dissolved active ingredients and the resulting enhanced dissolution properties. However, the compression of both unloaded and loaded mesoporous silica bulk material into tablets is challenging, due to poor/non-existing binding capacity. This becomes critical when high drug loads are to be achieved and the fraction of additional excipients in the final tablet formulation needs to be kept at a minimum.

Immediate-Release Formulations Produced via Twin-Screw Melt Granulation: Systematic Evaluation of the Addition of Disintegrants.

The current study evaluated the effect of location and amount of various superdisintegrants on the properties of tablets made by twin-screw melt granulation (TSMG). Sodium-croscarmellose (CCS), crospovidone (CPV), and sodium starch glycolate (SSG) were used in various proportions intra- and extra-granular. Tabletability, compactibility, compressibility as well as friability, disintegration, and dissolution performance were assessed.

Melt granulation: A comparison of granules produced via high-shear mixing and twin-screw granulation.

Melt granules of DI-CAFOS® A12 and 15% (w/w) Kolliphor® P407 were manufactured in a twin-screw granulator (TSG) at five different conditions (screw speed and throughput varied) and compared to granules manufactured in a high-shear granulator (HSG) (rotation speed of chopper/impeller and granulation time varied). Evaluated granules characteristics were process yield, particle-size distribution (PSD), particle morphology, flowability, porosity, specific surface area (SSA), tabletability, compressibility and binder distribution. Compared to TSG, granules produced from HSG were more spherical in shape with lower porosity, smaller mean particle size and a superior flowability.

Dissolution enhancement of carbamazepine using twin-screw melt granulation.

The current study explored the twin-screw melt granulation (TSMG) as a potential technology for the water solubility enhancement of biopharmaceutical classification system (BCS) class II drugs. As a model drug, carbamazepine (CBZ) was formulated with three different polymers as melt granules produced in a co-rotating twin-screw granulator. Polyethylene glycol 6000 (PEG 6000) and Kolliphor® (poloxamer) P407 were used as binding materials at two different granulation temperatures (T: 70 °C; 100 °C).

Improvement of tabletability via twin-screw melt granulation: Focus on binder distribution.

In this study, the impact of binder distribution on the tabletability and compactibility of granules produced by twin-screw melt granulation was investigated. To this end, two grades of dicalcium phosphate anhydrous (fine and coarse) were used as model substances (filler) in combination with two grades of poloxamer (fine and coarse) as melt binder at three concentrations. For the fine filler, granule forming followed the immersion mechanism, whereas a distribution mechanism was observed in case of the coarse filler.