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

Molecules

Holger Grohganz¹  Korbinian Löbmann¹  Thomas Rades¹  Riikka Laitinen²  Goedele Craye² 

[1]Department of Pharmacy, University of Copenhagen, Universitetsparken 2, Copenhagen DK-2100, Denmark

[2]School of Pharmacy, University of Eastern Finland, Yliopistonranta 1C, Kuopio FI-70210, Finland

关键词: co-amorphous;    spray drying;    dissolution;    solubility;    stability;    energy-dispersive X-ray spectroscopy;   

DOI  :  10.3390/molecules201219784

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown