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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 the factors influencing the prescription of quercetin liquid precursor liposomes and investigate the quality of the preparation. Methods: The liposomes of quercetin were prepared by liquid preparation of liposomes. Quercetin liposome particle size and encapsulation efficiency as an indicator, single factor test and orthogonal test screening quercetin liposomes prescription. The particle size and zeta potential of the liposomes were determined using a Zetasizer 3000HS particle size analyzer. Quercetin liposomes and free quercetin were separated by dialysis, and the content of quercetin was determined by HPLC. The detection wavelength was 360 nm and the mobile phase methanol-0.1% aqueous solution of formic acid (55:45) And artificial intestinal fluid stability. Results: Lecithin was selected as the lipid membrane, cremophor RH40 was used as surfactant, the ratio of lipid to lipid was 1:20, cremophor RH40 was added by 20% of the total amount of phospholipid and main drug, Genistin concentration 10.0 g · L-1. The particle size (228.7 ± 2.61) nm, Zeta potential (-21.2 ± 1.47) mV and entrapment efficiency (93.12 ± 1.18)% of the liposome hydration after the liposome hydration were good, After liposomes with good stability within 12 h, suitable for oral administration. Conclusion: The prepared quercetin liquid precursor liposomes have good in vitro properties. The particle size of the preparation in artificial gastric juice and artificial intestinal juice is slightly larger than that in water, but the particle size does not change significantly within 12 h in any aqueous medium.