期刊
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
卷 44, 期 2, 页码 206-214出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/03639045.2017.1386200
关键词
Extrusion; thermolabile drug; artemisinin; Soluplus (R); compatibility; bioavailability
资金
- Engineering and Physical Sciences Research Council [EP/J003360/1]
- UKIERI: UK-India Education and Research Initiative [TPR 26]
- EPSRC [EP/J003360/1] Funding Source: UKRI
- Engineering and Physical Sciences Research Council [EP/J003360/1] Funding Source: researchfish
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 (R), a low T-g amphiphilic polymer especially designed for solid dispersions enabled melt extrusion at 110 degrees 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.
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