制备波棱瓜子总木脂素纳米混悬剂

Nanosuspension preparation for total lignans from Herpetospermum caudigerum

目的制备波棱瓜子(Herpetospermum caudigerum)总木脂素纳米混悬剂,优化其处方并考察其体外溶出行为。方法采用p H依赖的溶解-沉淀法联合高压均质技术制备纳米混悬剂,Box-Behnken设计-响应面法优化处方,同时对其形态、粒径及晶型结构进行表征。然后,采用桨法测定总木脂素纳米混悬剂的体外溶出度。结果以总木脂素10 mg/m L,PVP K30 3.3 mg/m L,SDS 2.1 mg/m L制得的波棱瓜子总木脂素纳米混悬剂的平均粒径为(306.15±7.06)nm,扫描电镜显示,其呈不规则球形,大小较均匀;X射线衍射图表明,总木脂素在纳米混悬前后,晶型无显著变化,以无定型状态存在;体外溶出实验表明,该纳米混悬剂的溶出量明显高于其物理混合物。结论该制备工艺简单、稳定,适用于弱酸弱碱类难溶性药物纳米混悬剂的制备。

AIM To prepare nanosuspension for total lignans from Herpetospermum caudigerum,study its dissolution in vitro,and optimize the formulation. METHODS The nanosuspension was prepared by p H-dependent dissolving-precipitating and homogenization optimized by Box-Behnken design-response surface method and characterized in terms of morphology,particle size,and X-ray diffraction,with its dissolution in vitro measured by paddle method. RESULTS The optimal formulation（ drug concentration 10 mg / m L,PVP K30 3. 3 mg / m L,SDS 2. 1mg / m L） for nanosuspension of total H. caudigerum lignan was found to bring particles with an average size of（ 306. 15 ± 7. 06） nm,in an irregular spherical and in amorphous state in both coarse powder（ before the nanosuspensions） and nanosuspensions shown by electron microscopy and X-ray diffraction. The in vitro accumulated dissolution rate of nanosuspension was higher than that of physical mixture under the same conditions. CONCLUSION The optimally formulated preparation sets a both simple and stable model for preparing nanosuspension of insoluble drugs of either weak acid or weak base.