摘要
目的:分析槲皮素液体型前体脂质体的处方影响因素并考察该制剂的质量。方法:采用液体型前体脂质体的制备方法制备槲皮素前体脂质体。以槲皮素脂质体的粒径和包封率为指标,通过单因素试验和正交试验筛选槲皮素脂质体的处方。利用Zetasizer 3000HS型粒径仪测定脂质体的粒径和Zeta电位。采用透析法分离槲皮素脂质体和游离槲皮素,通过HPLC测定槲皮素的含量,检测波长360 nm,流动相甲醇-0.1%甲酸水溶液(55∶45),考察该制剂在人工胃液和人工肠液中的稳定性。结果:选择卵磷脂为脂质膜材,聚氧乙烯氢化蓖麻油(cremophor RH40)为表面活性剂,药脂比1∶20,cremophor RH40按磷脂和主药总量的20%加入,制剂中槲皮素质量浓度10.0 g·L-1。该处方下前体脂质体水合后的粒径(228.7±2.61)nm,Zeta电位(-21.2±1.47)m V,包封率(93.12±1.18)%,有较好的重复性,且水合后脂质体在12 h内具有良好的稳定性,适合口服给药。结论:制备的槲皮素液体型前体脂质体具有良好体外性质。该制剂在人工胃液和人工肠液中的粒径略大于在水中的粒径,但无论是在哪种水性介质中,12 h内其粒径变化不显著。
Objective： To analyze factors affecting formulation of quercetin liquid proliposomes and evaluate its quality. Method： Quercetin liquid proliposomes was prepared. Taking particle size and encapsulation efficiency as indexes,formulation of quercetin liquid proliposomes was optimized by single factor experiment and orthogonal test. Free quercetin and quercetin proliposomes was separated by dialysis method, the content of quercetin was determined by HPLC, stability of quercetin proliposomes in artificial gastric juice and artificial intestinal juice was investigated. Result： Optimum formulation of quercetin liquid proliposomes was as follows：lecithin as lipid membrane material, cremorphor RH40 as surfactant, drug phospholipids ratio of 1 ∶ 20,cremorphor RH40 amount of 20% to total content of phospholipid and main drug,the concentration of quercetin of10 g·L^- 1. The particle size,Zeta potential and encapsulation efficiency of the proliposomes after hydration were（ 228. 7 ± 2. 61） nm,（- 21. 2 ± 1. 47） m V and（ 93. 12 ± 1. 18） % with good stability within 12 h and good repeatability. It was suitable for oral administration. Conclusion： Quercetin liquid proliposomes has good in vitro properties. Within 12 h,its particle size do not change significantly in each aqueous medium.
出处
《中国实验方剂学杂志》
CAS
CSCD
北大核心
2015年第23期17-20,共4页
Chinese Journal of Experimental Traditional Medical Formulae
基金
徐州市科学技术局项目(XZZD1327)
徐州市科学技术局项目(KC14SH077)
徐州医学院院课题(2012KJ20)
关键词
槲皮素
前体脂质体
表面活性剂
包封率
质量评价
quercetin
proliposomes
surfactant
encapsulation efficiency
quality evaluation
