Application of hot melt extrusion for improving bioavailability of artemisinin a thermolabile drug. (1st February 2018)

• Record Type: Journal Article
• Authors: Kulkarni, C.; Kelly, A. L.; Gough, T.; Jadhav, V.; Singh, K. K.; Paradkar, A.
• Is Part Of: Drug development and industrial pharmacy. Volume 44:Number 2(2018)
• Page Start: 206
• Page End: 214
• Publication Date: 2018-02-01
• Subjects: Extrusion -- thermolabile drug -- artemisinin -- Soluplus® -- compatibility -- bioavailability; Pharmaceutical chemistry -- Periodicals; Pharmaceutical industry -- Periodicals; Drug Industry -- Periodicals; Technology, Pharmaceutical -- Periodicals; 615.05
• DOI: 10.1080/03639045.2017.1386200
• Languages: English
• ISSNs: 0363-9045

Abstract

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