Physicochemical properties of the amorphous drug, cast films, and spray dried powders to predict formulation probability of success for solid dispersions: Etravirine

Weuts, Ilse, Van Dycke, Frederic, Voorspoels, Jody, De Cort, Steve, Stokbroekx, Sigrid, Leemans, Ruud, Brewster, Marcus E., Xu, Dawei, Segmuller, Brigitte, Turner, Ya Tsz A., Roberts, Clive J., Davies, Martyn C., Qi, Sheng, Craig, Duncan Q. M. and Reading, Mike (2011) Physicochemical properties of the amorphous drug, cast films, and spray dried powders to predict formulation probability of success for solid dispersions: Etravirine. Journal of Pharmaceutical Sciences, 100 (1). pp. 260-274. ISSN 0022-3549

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Abstract

Solid dispersion technology represents an enabling approach to formulate poorly water-soluble drugs. While providing for a potentially increased oral bioavailability secondary to an increased drug dissolution rate, amorphous dispersions can be limited by their physical stability. The ability to assess formulation risk in this regard early in development programs can not only help in guiding development strategies but can also point to critical design elements in the configuration of the dosage form. Based on experience with a recently approved solid dispersion-based product, Intelence (R) (etravirine), a three part strategy is suggested to predict early formulate-ability of these systems. The components include an assessment of the amorphous form, a study of binary drug/carrier cast films and the evaluation of a powder of the drug and polymer processed in a manner relevant to the intended final dosage form. A variety of thermoanalytical, spectroscopic, and spectrophotometric approaches were applied to study the prepared materials. The data suggest a correlation between the glass forming ability and stability of the amorphous drug and the nature of the final formulation. Cast films can provide early information on miscibility and stabilization and assessment of processed powders can help define requirements and identify issues with potential final formulations. (C) 2010 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100: 260-274, 2011

Item Type: Article
Uncontrolled Keywords: molecular mobility,state,atomic-force microscopy,characterization,polymers pvp-k30,t-g,etravirine,hpmc,pharmaceutical systems,dosage forms,melt extrusion,solid dispersion,glassy itraconazole,amorphous,crystalline
Faculty \ School: Faculty of Science > School of Pharmacy
Depositing User: Rachel Smith
Date Deposited: 12 May 2011 15:44
Last Modified: 21 Apr 2020 16:55
URI: https://ueaeprints.uea.ac.uk/id/eprint/30524
DOI: 10.1002/jps.22242

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