Department of Pharmaceutical Sciences, Laboratory of nanotechnology, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, Telangana, 506009, India.
AAPS PharmSciTech. 2019 Jan 2;20(1):26. doi: 10.1208/s12249-018-1225-7.
Rebamipide has low oral bioavailability (10%) due to its low solubility and permeability. Lipid nanoemulsions (LNEs) were prepared in order to improve its oral bioavailability. Rebamipide-loaded lipid nanoemulsions were formulated by hot homogenization and ultrasonication method. Olive oil and egg lecithin in various concentrations as emulsifier were used in the preparation of LNEs. The lipid nanoemulsions were evaluated for various parameters. The globule size, polydispersity index (PDI), and zeta potential (ZP) of the formulations ranged from 230.3 ± 3.88 to 279.8 ± 5.76 nm, 0.204 ± 0.008 to 0.246 ± 0.029, and - 27.7 ± 2.05 to - 31.0 ± 1.87 mV, respectively. Entrapment efficiency and assay values ranged from 99.90 ± 0.006 to 99.92 ± 0.002% and 99.3 ± 0.808 to 99.6 ± 0.360, respectively. Physical stability test results revealed that the optimized LNEs were stable for 2 months at both room (25°C) and refrigerated temperature (4°C). The optimized LNE showed 4.32-fold improvement in the oral bioavailability in comparison to a marketed tablet suspension. In vivo anti ulcer activity of rebamipide LNE was studied by testing the prophylactic effect in preventing the mucosal damage in stomach region. The mucosa of stomach in animals was damaged by per oral administration of 80% alcohol. Maximum prophylactic antiulcer activity was observed by per oral delivery of rebamipide as LNE. Our results indicated that LNEs were a promising approach for the oral delivery of rebamipide for systemic effects along with local effects in protecting gastric region, which gets damaged during peptic ulcers.
雷贝拉唑的口服生物利用度较低（10%），这是由于其低溶解度和低通透性所致。为了提高其口服生物利用度，制备了脂质纳米乳液（LNEs）。采用热匀化和超声法制备雷贝拉唑载药脂质纳米乳液。采用不同浓度的橄榄油和蛋黄卵磷脂作为乳化剂制备 LNEs。对制剂的各种参数进行了评价。制剂的粒径、多分散指数（PDI）和 Zeta 电位（ZP）范围分别为 230.3±3.88nm 至 279.8±5.76nm、0.204±0.008 至 0.246±0.029 和-27.7±2.05mV 至-31.0±1.87mV。包封效率和含量测定值分别为 99.90±0.006%至 99.92±0.002%和 99.3±0.808%至 99.6±0.360%。物理稳定性试验结果表明，在室温（25°C）和冷藏温度（4°C）下，优化的 LNEs 稳定 2 个月。与市售片剂混悬剂相比，优化的 LNEs 可使口服生物利用度提高 4.32 倍。通过检测对胃区黏膜损伤的预防作用，研究了雷贝拉唑 LNE 的体内抗溃疡活性。通过口服给予 80%酒精来损伤动物胃区的黏膜。通过口服给予雷贝拉唑 LNE 可观察到最大的预防抗溃疡活性。我们的结果表明，LNEs 是一种有前途的方法，可用于雷贝拉唑的口服给药，以实现全身作用，并在保护胃区方面发挥局部作用，胃区在消化性溃疡时会受到损伤。
