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Molecules 2015, 20(12), 21532-21548; doi:10.3390/molecules201219784

Characterization of Amorphous and Co-Amorphous Simvastatin Formulations Prepared by Spray Drying

1
School of Pharmacy, University of Eastern Finland, Yliopistonranta 1C, Kuopio FI-70210, Finland
2
Department of Pharmaceutical Analysis, University of Ghent, Harelbekestraat 72, Ghent B-9000, Belgium
3
Department of Pharmacy, University of Copenhagen, Universitetsparken 2, Copenhagen DK-2100, Denmark
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 25 August 2015 / Revised: 24 November 2015 / Accepted: 25 November 2015 / Published: 3 December 2015
(This article belongs to the Collection Poorly Soluble Drugs)
View Full-Text   |   Download PDF [5780 KB, uploaded 3 December 2015]   |  

Abstract

In this study, spray drying from aqueous solutions, using the surface-active agent sodium lauryl sulfate (SLS) as a solubilizer, was explored as a production method for co-amorphous simvastatin–lysine (SVS-LYS) at 1:1 molar mixtures, which previously have been observed to form a co-amorphous mixture upon ball milling. In addition, a spray-dried formulation of SVS without LYS was prepared. Energy-dispersive X-ray spectroscopy (EDS) revealed that SLS coated the SVS and SVS-LYS particles upon spray drying. X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) showed that in the spray-dried formulations the remaining crystallinity originated from SLS only. The best dissolution properties and a “spring and parachute” effect were found for SVS spray-dried from a 5% SLS solution without LYS. Despite the presence of at least partially crystalline SLS in the mixtures, all the studied formulations were able to significantly extend the stability of amorphous SVS compared to previous co-amorphous formulations of SVS. The best stability (at least 12 months in dry conditions) was observed when SLS was spray-dried with SVS (and LYS). In conclusion, spray drying of SVS and LYS from aqueous surfactant solutions was able to produce formulations with improved physical stability for amorphous SVS. View Full-Text
Keywords: co-amorphous; spray drying; dissolution; solubility; stability; energy-dispersive X-ray spectroscopy co-amorphous; spray drying; dissolution; solubility; stability; energy-dispersive X-ray spectroscopy
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Craye, G.; Löbmann, K.; Grohganz, H.; Rades, T.; Laitinen, R. Characterization of Amorphous and Co-Amorphous Simvastatin Formulations Prepared by Spray Drying. Molecules 2015, 20, 21532-21548.

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