目的提高灯盏花素口服生物利用度,考察流化床包衣法制备灯盏花素前体脂质体的可行性。方法采用流化床包衣法制备灯盏花素前体脂质体;超滤-HPLC法测定灯盏花素前体脂质体的包封率,考察了载体、药脂比、进口温度、喷雾速率和喷雾风量对前体脂质体包封率的影响。结果以山梨醇为载体,药脂比小于1:3的前体脂质体包封率较高,进口温度、喷雾速率和喷雾风量对包封率均有一定影响;在较优条件下制备的前体脂质体颗粒流动性较好,粒径分布较均匀;重建的灯盏花素脂质体平均粒径为98nm,包封率为(63.1±2.8)%(n=3)。结论流化床包衣法制备灯盏花素前体脂质体是可行的。

Objective To enhance the oral bioavailability of breviscapine and investigate the feasibility of preparing the proliposome of breviscapine by fluidized bed coating method. Methods The fluidized bed coating method was used to prepare breviscapine proliposome and ultrafiltration-HPLC was applied to determination of the encapsulation efficiency. The influence factors on encapsulation efficiency including carriers, drug-lipid weight ratio, inlet air temperature, spray rate, and spray air volume were investigated. Results When the carrier was sorbitol and the drug-lipid weight ratio was under 1:3, the encapsulation efficiency could be higher. Inlet air temperature, spray rate, and spray air volume had some effects on the encapsulation efficiency. By the method, the fluidity of the proliposome granules was well and the particle size distribution ratio of them was uniform; the mean particle size of liposomal formulation of breviscapine after rehydration was 98 nm, and the encapsulation efficiency was (63.1±2.8)% (n=3). Conclusion It is feasible to prepare the breviscapine proliposome with fluidized bed coating method.