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Spray drying of poorly soluble drugs from aqueous arginine solution.
Int J Pharm. 2017 Oct 30; 532(1):289-298.IJ

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 24h, 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.

Authors+Show Affiliations

School of Pharmacy, University of Eastern Finland, P.O. Box 1627, 70211 Kuopio, Finland. Electronic address: rami.ojarinta@uef.fi.School of Pharmacy, University of Eastern Finland, P.O. Box 1627, 70211 Kuopio, Finland; Laboratory for Pharmaceutical Process Analytical Technology, Department of Pharmaceutical Analysis, Faculty of Pharmaceutical Sciences, Ghent University, Ottergemsesteenweg 460, 9000 Ghent, Belgium.School of Pharmacy, University of Eastern Finland, P.O. Box 1627, 70211 Kuopio, Finland.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

28890173

Citation

Ojarinta, Rami, et al. "Spray Drying of Poorly Soluble Drugs From Aqueous Arginine Solution." International Journal of Pharmaceutics, vol. 532, no. 1, 2017, pp. 289-298.
Ojarinta R, Lerminiaux L, Laitinen R. Spray drying of poorly soluble drugs from aqueous arginine solution. Int J Pharm. 2017;532(1):289-298.
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. https://doi.org/10.1016/j.ijpharm.2017.09.015
Ojarinta R, Lerminiaux L, Laitinen R. Spray Drying of Poorly Soluble Drugs From Aqueous Arginine Solution. Int J Pharm. 2017 Oct 30;532(1):289-298. PubMed PMID: 28890173.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Spray drying of poorly soluble drugs from aqueous arginine solution. AU - Ojarinta,Rami, AU - Lerminiaux,Louise, AU - Laitinen,Riikka, Y1 - 2017/09/08/ PY - 2017/07/19/received PY - 2017/09/05/revised PY - 2017/09/07/accepted PY - 2017/9/12/pubmed PY - 2018/6/5/medline PY - 2017/9/12/entrez KW - Amino acid KW - Co-amorphous KW - Dissolution KW - Spray drying KW - Stability SP - 289 EP - 298 JF - International journal of pharmaceutics JO - Int J Pharm VL - 532 IS - 1 N2 - 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 24h, 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. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/28890173/Spray_drying_of_poorly_soluble_drugs_from_aqueous_arginine_solution_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(17)30870-0 DB - PRIME DP - Unbound Medicine ER -