Evaluation of the formulation of solid dispersions by co-spray drying itraconazole with Inutec SP1, a polymeric surfactant, in combination with PVPVA 64

Abstract

In order to improve the in vitro performance and stability of co-spray-dried itraconazole/Inutec SP1 systems, the influence of adding PVPVA 64, a polymer that is compatible with itraconazole, was evaluated. Dissolution tests were carried out on several itraconazole/PVPVA 64/Inutec SP1 compositions and spray-dried itraconazole/PVPVA 64 powders were used as references. The physicochemical properties of the samples were assessed with modulated temperature differential scanning calorimetry (MDSC), X-ray powder diffraction (XRD) and environmental scanning electron microscopy (ESEM). Physicochemical analysis revealed that there is no interaction between itraconazole and Inutec SP1 and that sufficient amount of PVPVA 64 is required to keep the drug molecularly dispersed. The improvement of the ternary solid dispersions over the binary solid dispersions was composition dependent. On one hand the increased drug/PVPVA 64 ratio in the ternary systems slowed dissolution down, on the other hand this was compensated by the solubilizing power of Inutec SP1.