灯盏花素乳剂的优化制备、表征及心脏中的分布

灯盏花素(breviscapine)是菊科植物短葶飞蓬（Erigeron breviscapus (vant.)Hand-Mazz）中提取的黄酮类有效成分。为了克服现有剂型生物利用度低、稳定性差、半衰期短等问题，本课题研制了灯盏花素静脉输液乳剂，提高了制剂的稳定性，有效延长了药物的作用时间。本文选择高速分散－高压均质法制备灯盏花素乳剂，以粒径、多分散系数、Zeta电位及稳定常数等指标进行综合评分，在单因素考察的基础上，通过正交实验设计优化处方工艺。所得乳剂粒径为(225.3 ± 8.8) nm，多分散系数为0.221 ± 0.020，Zeta电位为(-29.6 ± 1.5) mV，Ke值为(24.3±2.9)%，含量为(94.5±0.6)% (n = 3)。该载体可以提高药物在缓冲液和胎牛血清中的稳定性，延缓药物在缓冲液和大鼠血浆中的释放，提高药物在小鼠心脏中的分布，大大延长平均驻留时间。表明该处方工艺下制备的乳剂可做为心脏疾病的优良载体。

Xiong F., Wang H., Geng K. K., Gu N., Zhu J. B. Optimized Preparation,Characterization and Biodistribution in heart of Breviscapine Lipid Emulsion. Chem. Pharm. Bull. 2010, 2(11): 1455-1460.

Fig. 1 Structure of scutellarin

Fig. 2. Particle size, polydispersity index (a) and content of scutellarin, Ks value (b) of preemulsion as a function of temperature of mixing (8000rpm, 60s, mean ± S.D., n=3).

Fig. 9. In vitro release of scutellarin from Bre-LE (○) when incubated with PBS (a) and rat plasma (b) at 37˚C (mean ± S.D., n = 3). Release of Injectio Breviscapine (Δ) was also presented as a control.