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目的制备莪术醇固体分散体(Cur-SDs),优选最优处方及工艺,以期提高其体外溶出度。方法以体外溶出度为评价指标,分别考察以聚乙烯吡咯烷酮K30(PVP K30)、泊洛沙姆188(F68)、聚乙二醇4000(PEG4000)、聚乙二醇6000(PEG6000)为载体以及采用溶剂法、熔融法或溶剂-熔融法制备所得SDs对莪术醇的增溶能力。并利用红外光谱(IR)、差示扫描量热(DSC)、X-射线衍射(XRD)对SDs中药物的存在形态进行研究,并初步考察了其在长期储存过程中的稳定性。结果以F68为载体,采用溶剂-熔融法制备的Cur-SDs体外溶出行为优于其他处方、工艺制备的SDs,最优药物-载体比为1∶5。DSC、IR及XRD结果表明药物主要以分子或无定形状态存在于SDs中,且药物分子未发生变化。稳定性研究表明,室温放置6个月其溶出度未见下降、物相状态未见明显改变。结论将难溶性药物莪术醇制备成SDs,能显著提高其体外溶出度及溶出速率,且稳定性良好,工艺简单可行。
Objective To prepare curcumol solid dispersions (Cur-SDs), optimize the optimal prescription and process, in order to improve its in vitro dissolution. Methods The dissolution rate in vitro was taken as the evaluation index. The effects of PVP K30, poloxamer 188, PEG 4000, PEG 6000 and Solubility, melting or solvent-melting method was used to prepare the solubilized SDs of curcumol. The existing forms of SDs in SDs were studied by IR, DSC and XRD, and their stability in long-term storage was also investigated. Results In vitro dissolution behavior of Cur-SDs prepared by solvent-melt method was better than that of other prescriptions. The best drug-carrier ratio was 1: 5. The results of DSC, IR and XRD showed that the drug existed mainly in the molecular or amorphous state in SDs, and the drug molecule did not change. Stability studies show that at room temperature for 6 months, dissolution did not decline, no significant changes in the phase state. Conclusion The curcumol, a poorly soluble drug, can be prepared into SDs, which can significantly improve the dissolution rate and dissolution rate in vitro. The stability is good and the process is simple and feasible.