| Hot melt extrusion (HME) is a new pharmaceutical technology, which can realize the mixing, melting, shaping process carried out on a single machine. HME offers many advantages on sustained and fast release system, for example, neither water nor solvents were used in this process, producing no pollution, with the drugs well dispersed.Three drugs of ibuprofen, indomethacin and yixintong were chosen to make extrudates:PEO, EC and HPMC were choosed as carriers to make ibuprofen sustained-release systems by HME. The results of drug release indicated all of the three carriers sustained the IBP release from extrudates. The order of drug release rate was:HPMC>PEO>EC. The release rate in12hr was improved nearly17%when half amount of HPMC was replaced by MCC. The accumulate releasing amounts of IBP were23%、60%and90%in2hr,6hr and12hr, respectively. IBP release was increased with adding the excipients of agar, L-HPC, MCC to the PEO based system, while Xanthan gum showed the opposite effect. Adding of Xanthan gum into EC system enhanced drug release rate.From the results of DSC analysis and SEM of the Ibuprofen extrudates, the relative area of drug peak were reduced in DSC, the extrudates had more compact and smooth cross section compared to directly compressed tablets in SEM, all which above approved the drug’s high disperse. The HPLC results confirmed the drug was stable for no new peak appearing and little content changed.The HME technology enhanced the dissolution rate of indomethacin from the extrusion capsule compared to the physical mixture and the pure drug capsule. The system of PEG-10000/PVP-k30/F-68/indomethacin (1:1:1:1) showed the fastest dissolution rate. In the different time of10and45min, the dissolution rates of extrusion capsule were10%higher than that of physical mixture capsule.The yixintong extrudates were prepared and afterwards foamed with supercritical CO2. The result of SEM confirmed the formation of large numbers of microcells, which improved releasing of the drug. |
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