Abstract
In this paper, the role of mesoporous silica (MS) particle size in the stabilization of amorphous simvastatin (SVT) is revealed. For inhibiting recrystallization of the supercooled drug, the two MS materials (Syloid® XDP 3050 and Syloid® 244 FP) were employed. The crystallization tendency of SVT alone and in mixture with the MS materials was investigated by Differential Scanning Calorimetry (DSC) and Broadband Dielectric Spectroscopy (BDS). Neither confinement of the SVT molecules inside the MS pores nor molecular interactions between functional groups of the SVT molecules and the surface of the stabilizing excipient could explain the observed stabilization effect. The stabilization effect might be correlated with diffusion length of the SVT molecules in the MS materials that depended on the particle size. Moreover, MS materials possessing different particle sizes could offer free spaces with different sizes, which might influence crystal growth of SVT. All of these factors must be considered when mesoporous materials are used for stabilizing pharmaceutical glasses.
Highlights
The poor aqueous solubility of active pharmaceutical ingredients (APIs) is one of the most challenging issues of modern pharmacy [1,2,3]
We investigated the effect of two mesoporous silica (MS) materials (SYL244 and Syloid® 3050 XDP (SYL3050)) on the physical stability of supercooled SVT
Despite the differences in the obtained crystallization kinetics resulting from the use of different research techniques, one could have observed the same stabilization trends
Summary
The poor aqueous solubility of active pharmaceutical ingredients (APIs) is one of the most challenging issues of modern pharmacy [1,2,3]. Over 40% of marketed immediate-release oral dosage forms contain poorly soluble drugs [4,5]. It has been many times reported that the transformation into amorphous form significantly increased the solubility of drug molecules in comparison with their crystalline counterparts [8,9]. Much effort is being made to (i) investigate physical stability of amorphous form of pharmaceuticals [15,16,17], (ii) find effective methods leading to their stabilization [18,19,20], and (iii) discover the molecular mechanisms responsible for the observed recrystallization inhibition [16,21,22,23,24,25]
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