Rheological Properties and Process Temperature Prediction for the Hot Melt Extrusion of Artesunate with...

Area of Science:

• Pharmaceutical Science
• Materials Science
• Chemical Engineering

Background:

• Active Pharmaceutical Ingredients (APIs) often exhibit poor water solubility, necessitating advanced formulation strategies.
• Hot-Melt Extrusion (HME) is a key technique for creating Amorphous Solid Dispersions (ASDs) to enhance API bioavailability.
• Processability and temperature control are critical for successful HME of API-polymer blends.

Purpose of the Study:

• To establish optimal Hot-Melt Extrusion (HME) conditions for Artesunate (AS) based Amorphous Solid Dispersions (ASDs).
• To investigate the utility of dynamic rheological studies in predicting HME processability.
• To correlate rheological properties with thermal and structural characteristics of the ASDs.

Main Methods:

• Dynamic rheological studies to determine the Soft Point of Mixture (SPM) and Initial Fusion Plateau Temperature (IFPT).
• Hot-Melt Extrusion (HME) of Artesunate (AS), Soluplus®, and Span®20 blends.
• Characterization using Thermogravimetric Analysis (TGA), Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD), and Scanning Electron Microscopy (SEM).

Main Results:

• Rheological parameters, specifically the SPM, effectively predicted suitable HME temperature profiles.
• Successful preparation of ASDs with enhanced properties was achieved by optimizing extrusion conditions based on rheology.
• Correlation established between rheological behavior and thermal/structural properties analyzed by TGA, DSC, XRD, and SEM.

Conclusions:

• Dynamic rheology is a powerful and efficient tool for determining optimal HME parameters for ASD formulation.
• Utilizing rheological data simplifies the process of setting appropriate temperature profiles for HME.
• This approach facilitates faster and more effective development of high-performance ASDs for poorly soluble APIs.