Application of hot melt extrusion for improving bioavailability of artemisinin a thermolabile drug

Abstract

Hot melt extrusion has been used to produce a solid dispersion of the thermolabile drug artemisinin. Formulation and process conditions were optimized prior to evaluation of dissolution and biopharmaceutical performance. Soluplus^®, a low T_g amphiphilic polymer especially designed for solid dispersions enabled melt extrusion at 110 °C although some drug-polymer incompatibility was observed. Addition of 5% citric acid as a pH modifier was found to suppress the degradation. The area under plasma concentration time curve (AUC_0–24h) and peak plasma concentration (C_max) were four times higher for the modified solid dispersion compared to that of pure artemisinin.

Keywords:

• Extrusion
• thermolabile drug
• artemisinin
• Soluplus^®
• compatibility
• bioavailability

Acknowledgements

The authors are thankful to BASF for the gift sample of Soluplus^®.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was supported by the Engineering and Physical Sciences Research Council grant no [EP/J003360/1] and UKIERI: UK-India Education and Research Initiative (TPR 26).