M. Wulff et al., AN INVESTIGATION INTO THE CRITICAL SURFACTANT CONCENTRATION FOR SOLIDSOLUBILITY OF HYDROPHOBIC DRUG IN DIFFERENT POLYETHYLENE GLYCOLS, International journal of pharmaceutics, 142(2), 1996, pp. 189-198
Solid dispersions of 10% w/w griseofulvin in different polyethylene gl
ycols (PEGs) with or without incorporation of alkali dodecyl sulphates
(MDS) were prepared by the melting method. The investigations concern
ed the solid state (X-ray powder diffraction), the transition from sol
id to liquid stale (Oscillating DSC) and the liquid state (low frequen
cy dielectric spectroscopy). The critical concentrations of SDS for th
e formation of solid solutions in varying PEGs were evaluated. In PEG
3000 this formation occurs at 1.4% w/w SDS, whereas PEG 6000 and PEG 2
0000 require solely 1.0% ww SDS to transfer a dispersion into a solid
solution. PEG 3000 was also investigated with the addition of MDS. The
critical surfactant concentrations for the formation of solid solutio
ns with the counterions Li+, Na+ and K+ were 1.0%, 1.4% and 2.1% w/w,
respectively. The investigated systems had varying degrees of crystall
inity. With the addition of SDS to PEGs with a range of molecular weig
hts, the highest crystallinity was seen in the PEG 3000 sample. The di
fferent polymers contained different amounts of folded and extended ch
ains which influences the amount of amorphous material within the poly
mer structure. When surfactants with different counterions were added
to PEG 3000, the lithium sample showed the highest crystallinity. In t
he melt the Li+ sample showed the lowest dielectric mobility. The resu
lts show that concentration and structure of surfactant together with
the presence of folded and extended chains form the conditions for the
formation of solid solutions.