College of Pharmacy, Yanbian University, Yanji City, Jilin Province 133000, China.
Arch Pharm Res. 2012 Jun;35(6):1037-43. doi: 10.1007/s12272-012-0611-z. Epub 2012 Jun 30.
In this study, we developed an optimized formulation of a breviscapine lipid emulsion (BLE) and evaluated the physicochemical properties and in vivo pharmacokinetics of BLE in rats. For the preparation of the lipid emulsion, soybean oil and oleic acid were used as the oil phase, lecithin and poloxamer 188 as surfactants and glycerol as co-surfactant. An optimized formulation consisting of soybean oil (10.0%), oleic acid (0.9%), lecithin (1.5%), poloxamer 188 (0.4%), and glycerol (2.25%) was selected. The results showed that the average particle size, polydispersity index, and zeta potential of the optimized formulation were 183.5 ± 5.5 nm, 0.098 ± 0.046, and -35.0 ± 2.5 mV, respectively. The BLE was stable for at least three month at room temperature. After a single intravenous dose of 4 mg/kg to rats, the AUC of scutellarin from the lipid emulsion was about 1.5-fold higher than that of the commercial product (breviscapine injection). In conclusion, the optimized formulation of BLE showed positive results over the commercial product in terms of the physicochemical properties and pharmacokinetics of BLE in rats.
在这项研究中，我们开发了灯盏花素脂质体乳液（BLE）的优化配方，并评估了 BLE 在大鼠体内的理化性质和药代动力学。为了制备脂质体乳液，我们使用大豆油和油酸作为油相，卵磷脂和泊洛沙姆 188 作为表面活性剂，甘油作为助表面活性剂。选择了由大豆油（10.0%）、油酸（0.9%）、卵磷脂（1.5%）、泊洛沙姆 188（0.4%）和甘油（2.25%）组成的优化配方。结果表明，优化配方的平均粒径、多分散指数和 Zeta 电位分别为 183.5±5.5nm、0.098±0.046 和-35.0±2.5mV。BLE 在室温下至少稳定三个月。大鼠单次静脉注射 4mg/kg 后，脂质体乳液中灯盏花素的 AUC 约为商业产品（灯盏花素注射液）的 1.5 倍。总之，与商业产品相比，BLE 的优化配方在 BLE 在大鼠体内的理化性质和药代动力学方面表现出了积极的结果。
