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目的探讨微型化介质研磨法制备难溶性黄酮类化合物纳米混悬剂(NS)的可行性。方法以磁力搅拌器为动力装置,西林瓶为研磨室,采用氧化锆珠子为研磨介质构建微型化介质研磨法制备槲皮素(QCT)、黄芩苷(BCN)、葛根素(PRN)及水飞蓟素(SLR)4种黄酮类化合物NS,以平均粒径、多分散度指数(PDI)和稳定性指数(SI)为指标,对工艺参数转速、研磨介质用量和研磨时间进行优化。结果 QCT-NS、BCN-NS、PRN-NS和SLR-NS制备的最佳工艺参数转速、研磨时间、氧化锆用量与药物混悬液比例分别为QCT-NS 800 r/min、8 h、1∶1,BCN-NS 800 r/min、24 h、1∶1,PRN-NS800 r/min、24 h、2∶1,SLR-NS 800 r/min、12 h、1∶1;以最佳工艺参数制备所得QCT-NS、BCN-NS、PRN-NS和SLR-NS的平均粒径均在400 nm以下,QCT-NS、BCN-NS和SLR-NS的PDI在0.3以下,SI高于0.75;PRN-NS的PDI和SI分别为0.41和0。结论微型化介质研磨法制备难溶性黄酮类化合物NS工艺简单、稳定可行,值得进一步深入研究。
Objective To investigate the feasibility of preparing nanosuspensions (NS) of insoluble flavonoids by miniaturized medium grinding method. Methods Using magnetic stirrer as power unit and vials as grinding chamber, zirconia beads were used as the grinding medium to prepare quaternary ammonium chloride (QCT), baicalin (BCN), puerarin (PRN) and silymarin SLR), four flavonoids, NS, were optimized by using the average particle size, polydispersity index (PDI) and stability index (SI) as parameters. Results The optimum process parameters of QCT-NS, BCN-NS, PRN-NS and SLR-NS were set at 800 r / min QCT-NS, : 1, BCN-NS 800 r / min, 24 h, 1: 1, PRN-NS800 r / min, 24 h, 2: 1, SLR-NS 800 r / min, The average particle size of QCT-NS, BCN-NS, PRN-NS and SLR-NS prepared in the process parameters were both below 400 nm. The PDIs of QCT-NS, BCN-NS and SLR- The PDI and SI of PRN-NS were 0.41 and 0 respectively. Conclusion The preparation of insoluble flavonoids by miniaturized medium grinding method is simple, stable and feasible and worth further study.