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Spray drying of poorly soluble drugs from aqueous arginine solution

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Article (963.4Kb)
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final draft
Date
2017
Author(s)
Ojarinta R
Lerminiaux L
Laitinen R
Unique identifier
10.1016/j.ijpharm.2017.09.015
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Self-archived article

Citation
Ojarinta R. Lerminiaux L. Laitinen R. (2017). Spray drying of poorly soluble drugs from aqueous arginine solution.  INTERNATIONAL JOURNAL OF PHARMACEUTICS, 532 (1) , 289-298. 10.1016/j.ijpharm.2017.09.015.
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© Elsevier B.V
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CC BY-NC-ND https://creativecommons.org/licenses/by-nc-nd/4.0/
Abstract

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 (Tg), 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 Tg 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.

Subjects
Co-amorphous   Amino acid   Spray drying   Stability   Dissolution   
URI
https://erepo.uef.fi/handle/123456789/4317
Link to the original item
http://dx.doi.org/10.1016/j.ijpharm.2017.09.015
Publisher
Elsevier BV
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  • Terveystieteiden tiedekunta [1331]
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