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

Kulkarni, C., Kelly, A. L., Gough, T., Jadhav, V., Singh, Kamalinder orcid iconORCID: 0000-0001-7325-0711 and Paradkar, A. (2017) Application of hot melt extrusion for improving bioavailability of artemisinin a thermolabile drug. Drug Development and Industrial Pharmacy . pp. 1-9. ISSN 0363-9045

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Official URL: https://doi.org/10.1080/03639045.2017.1386200

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 Tg 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 (AUC0–24h) and peak plasma concentration (Cmax) were four times higher for the modified solid dispersion compared to that of pure artemisinin.


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