(176an) Ternary Amorphous Solid Dispersions – an Investigation Onto the Effects of the Addition of Mesoporous Silica on the Physicochemical Properties and Release Profile

Low
solubility of active pharmaceutical ingredients (API) poses a significant
problem in the pharmaceutical industry and novel methods and materials are
constantly sought in improving the solubility of these APIs in aqueous media [1]. One
such method is the conversion of these APIs from their crystalline form into
their amorphous form by using hot melt extrusion (HME). In order to increase
the stability of the amorphous form, these APIs are often co-extruded with
polymers [2]. Hot
melt extrusion has been commonly used as a technique to disperse drug molecules
into polymer matrices and more recently also in dispersions comprised of silica
and a polymer [3]. Our
initial investigations (Figure 1) indicated that the type of MPSI employed in
ternary dispersions strongly influences the observed API release profile of
prepared formulations. Thus, in the current work, physico-chemical properties
along with the stability of prepared ternary amorphous dispersions are
investigated. Formulations investigated, comprise of mesoporous silica (MPSi), a
polymer and a model BCS II drug.

Figure 1: Dissolution profile of prepared HME
formulations

References

1. Ridhurkar,
D., A. Vajdai, and Z. Zsigmond, Hot-melt extrusion (HME)and its application
for pharmacoki-netic improvement of poorly water soluble drugs. Vol. 2.
2016. 47-51.

2. Mahmah,
O., et al., A comparative study of the effect of spray drying and hot-melt
extrusion on the properties of amorphous solid dispersions containing
felodipine. Vol. 66. 2014. 275-84.

3. Genina,
N., B. Hadi, and K. Löbmann, Hot Melt Extrusion as Solvent-Free Technique
for a Continuous Manufacturing of Drug-Loaded Mesoporous Silica. Journal of
Pharmaceutical Sciences, 2018. 107(1): p. 149-155.