流化床法制备水飞蓟素纳米结晶微丸

Preparing silymarin nanocrystal pellets by fluid-bed method

目的研究水飞蓟素纳米结晶微丸的最优工艺参数及体外释放度。方法流化床法制得水飞蓟素纳米结晶微丸。以黏合剂用量、恒流泵转速和雾化压力为考察因素,以微丸的得丸率、上药率和平均再分散粒径为指标,采用星点设计-效应面法优化工艺参数,并进行体外释放度测定。结果最优工艺参数为羟丙甲基纤维素用量0.16%,恒流泵转速9.5 r/min,雾化压力0.12 MPa。微丸的得丸率(85.74±1.29)%,上药率(86.43±1.52)%,平均再分散粒径(251.6±3.8)nm,30 min内药物累积释放度达90%以上。结论该方法制成的水飞蓟素纳米结晶微丸兼顾了纳米混悬剂和固体制剂的优点,工艺简单、可行,可为液体制剂固体化提供新的制备方法。

AIM To study the best technology parameters for silymarin nanocrystal pellets and their in vitro release rate. METHODS Silymarin nanocrystal pellets were made by fluid-bed method. Considering the yield of pellets,layering efficiency and average particle size of redispersion as the indices,central composite design-response surface method was applied to investigating the adhesive consumption,speed of constant flow pump and atomizing pressure for optimizing technology parameters and determining release rate in vitro. RESULTS The technology parameters were thus optimized,viz.,the HPMC consumption was 0. 16%,the speed of constant flow pump was9. 5 r / min,and atomization pressure was 0. 12 MPa. The yield of pellets was（ 85. 74 ± 1. 29） %,layering efficiency was（ 86. 43 ± 1. 52） %,average particle size of redispersion was（ 251. 6 ± 3. 8） nm,and the accumulative release rate of drug reached more than 90% within 30 min. CONCLUSION The silymarin nanocrystal pellets made by this method reveal the superiorities of both nanosuspension and solid preparation. This simple and feasible technology can be applied to solidifying the liquid preparation.