Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 532, Issue 1, Pages 289-298Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2017.09.015
Keywords
Co-amorphous; Amino acid; Spray drying; Stability; Dissolution
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Funding
- Doctoral Programme in Drug Research in the Doctoral School of University of Eastern Finland
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Co-amorphous drug-amino acid mixtures have shown potential for improving the solid-state stability and dissolution behavior of amorphous drugs. In previous studies, however these mixtures have been produced mainly with small-scale preparation methods, or with methods that have required the use of organic solvents or other dissolution enhancers. In the present study, co-amorphous ibuprofen-arginine and indomethacin-arginine mixtures were spray dried from water. The mixtures were prepared at two drug-arginine molar ratios (1: 1 and 1:2). The properties of the prepared mixtures were investigated with differential scanning calorimetry, X-ray powder diffractometry, Fourier-transform infrared spectroscopy and a 24 h, non-sink, dissolution study. All mixtures exhibited a single glass transition temperature (T-g), evidence of the formation of homogenous single-phase systems. Fourier transform infrared spectroscopy revealed strong interactions (mainly salt formation) that account for the positive deviation between measured and estimated T-g values. No crystallization was observed during a 1-year stability study in either 1:1 or 1:2 mixtures, but in the presence of moisture, handling difficulties were encountered. The formation of co-amorphous salts led to improved dissolution characteristics when compared to the corresponding physical mixtures or to pure crystalline drugs.
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