Different Solid Dispersion Techniques For Dissolution Enhancement Using Paracetamol As A Model Drug
INTERNATIONAL JOURNAL OF PHARMACEUTICAL AND PHYTOPHARMACOLOGICAL RESEARCH(2015)
摘要
The objective of this study was to investigate the effect of different preparation techniques such as fusion, solvent evaporation or hot melt extrusion (HME) on the characteristics of solid dispersions (SDs) using paracetamol (PCT) as a model drug. SDs of PCT, with different carriers viz., Eudragit E100, mannitol, HPMC, PVP and PEG 6000, were prepared at 1: 1 ratio. Initially, solvent evaporation and fusion were used for the preparation of PCT SDs. The prepared SDs were characterized using DSC, FT-IR and in vitro dissolution. Eudragit E100 and mannitol exhibited the best dissolution performance. Based on both dissolution data and crystallinity reduction, Eudragit E100 was selected for preparation of solid dispersions using HME, as a third preparation technique, at the ratios of 1: 1 and 1: 2. The powdered extrudates were characterized for their thermal characteristics, powder X-ray diffraction (PXRD), and dissolution behaviour. Extrusion completely transformed the drug into an amorphous form with a complete loss of crystallinity, as evidenced by DSC and PXRD. The dissolution patterns were close to those prepared by either solvent evaporation or simple fusion. It could be concluded that the different preparation techniques resulted in SDs with almost similar characteristics, however, HME would offer several advantages over the traditional techniques.
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关键词
solid dispersion, hot melt extrusion, fusion, solvent evaporation, MDT
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