Process characteristics and compaction of spray-dried emulsions containing a drug dissolved in lipid

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Process characteristics and compaction of spray-dried emulsions containing a drug dissolved in lipid
December 2004
Tue Hansen, a, b, Per Holm, c and Kirsten Schultz, a
aPharmaceutical Development, H. Lundbeck A/S, Ottiliavej 9, DK-2500 Valby, Denmark
bDepartment of Pharmaceutics, The Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK-2100 Copenhagen, Denmark
cLifeCycle Pharma A/S, Kogle All? 4, DK-2970 H?rsholm, Denmark
International Journal of Pharmaceutics Volume 287, Issues 1-2 , 9 December 2004, Pages 55-66
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Abstract
The objective of the present study is to prepare directly compressible powders, containing a poorly water-soluble drug dissolved in medium-chain triglycerides (MCT), by spray drying o/w-emulsions in a pilot plant spray dryer. In addition to the lipid phase, the emulsions contained a water-soluble carrier (a sugar), a water-insoluble carrier (magnesium alumino metasilicate) and a combined emulsifier and film-forming agent (gelatine). A factorial design was used to investigate the effect of formulation variables on the spray drying process and powder properties. The factors varied were soluble carrier type (trehalose or mannitol), insoluble carrier particle size distribution (granular or fine powder) and amount of lipid phase in the emulsion (low or high). Compressibility and compactibility of the spray-dried emulsions were mainly affected by the content of lipid in the powders and decreased on increasing the amount of lipid. Increasing the particle size of the insoluble carrier decreased spray drying process yield and lipid encapsulation efficiency whereas compactibility and handling properties were improved. Incorporation of a soluble carrier becoming amorphous on spray drying resulted in tablets with an increased mechanical strength compared to powders containing a crystalline soluble carrier.