The Value of Bead Coating in the Manufacturing of Amorphous Solid Dispersions: A Comparative Evaluation with Spray Drying

Despite the fact that an amorphous solid dispersion (ASD)-coated pellet formulation offers potential advantages regarding the minimization of physical stability issues, there is still a lack of in-depth understanding of the bead coating process and its value in relation to spray drying. Therefore, bead coating and spray drying were both evaluated for their ability to manufacture high drug-loaded ASDs and for their ability to generate physically stable formulations. For this purpose, naproxen (NAP)–poly(vinyl-pyrrolidone-co-vinyl acetate) (PVP-VA) was selected as an interacting drug–polymer model system, whilst naproxen methyl ester (NAPME)–PVP-VA served as a non-interacting model system. The solvent employed in this study was methanol (MeOH). First, a crystallization tendency study revealed the rapid crystallization behavior of both model drugs. In the next step, ASDs were manufactured with bead coating as well as with spray drying and for each technique the highest possible drug load that still results in an amorphous system was defined via a drug loading screening approach. Bead coating showed greater ability to manufacture high drug-loaded ASDs as compared to spray drying, with a rather small difference for the interacting drug–polymer model system studied but with a remarkable difference for the non-interacting system. In addition, the importance of drug–polymer interactions in achieving high drug loadings is demonstrated. Finally, ASDs coated onto pellets were found to be more physically stable in comparison to the spray dried formulations, strengthening the value of bead coating for ASD manufacturing purposes.

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About this article: Boel, E.; Reniers, F.; Dehaen, W.; Van den Mooter, G. The Value of Bead Coating in the Manufacturing of Amorphous Solid Dispersions: A Comparative Evaluation with Spray Drying. Pharmaceutics 2022, 14, 613. https://doi.org/10.3390/pharmaceutics14030613

Materials
NAP (i.e., 2-(6-Methoxynaphthalen-2-yl)propanoic acid) was obtained from SA Fagron NV (Waregem, Belgium). NAP was also used as substrate in the synthesis of NAPME (i.e., methyl 2-(6-Methoxynaphtalen-2-yl)propanoate (see Section 2.2). BASF ChemTrade GmbH (Ludwigshafen, Germany) supplied Kollidon-VA 64 (PVP-VA). Phosphorus pentoxide and MeOH (purity ≥ 99.8%) were purchased from Acros Organics (Geel, Belgium). Microcrystalline cellulose (MCC) pellets (Vivapur® 700: 18–25 mesh, 710–1000 µm) were acquired from JRS Pharma GmbH (Rosenberg, Germany). ChemLab NV (Zedelgem, Belgium) provided sodium chloride.

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