Kim Ju-Young, Bae Hyun-Ju, Choi Jungsub, Lim Jong-Rae, Kim Sang-Wook, Lee Sung-Hoon, Park Eun-Seok
School of Pharmacy, Sungkyunkwan University, Jangan-gu, Suwon, Gyeonggi-do, 440-746, Republic of Korea.
Arch Pharm Res. 2014 Aug;37(8):1053-62. doi: 10.1007/s12272-013-0278-0. Epub 2013 Nov 20.
The purpose of the present study is to investigate the influence of gastric retention of ecabet sodium (ECS) on its mucoprotective effect in rat ulcer models. Mini-tablets containing 9 mg ECS were prepared using the direct compression method. The release rates of ECS mini-tablets were controlled by the amount and viscosity grade of hydroxypropylmethyl cellulose incorporated. Gastric retention of ECS mini-tablets after oral administration to rats was visually confirmed using a fluorescence imaging system. Because ECS mini-tablets exhibited size-dependent gastric retention, their gastric retention time was prolonged as the release rate decreased. In the in vivo efficacy study, gastro-retentive dosage forms of ECS did not influence the mucoprotective effect in the immediate irritation model but enhanced the effect in the delayed irritation model compared with ECS suspension. This finding indicates that the duration of the mucoprotective effect of ECS can be extended by the employment of gastro-retentive dosage formulations and provides a rationale for development of ECS gastro-retentive dosage forms.
本研究的目的是在大鼠溃疡模型中研究埃索美拉唑钠（ECS）的胃内滞留对其黏膜保护作用的影响。采用直接压片法制备了含9 mg ECS的微型片。ECS微型片的释放速率通过加入的羟丙基甲基纤维素的量和粘度等级来控制。使用荧光成像系统直观确认大鼠口服ECS微型片后的胃内滞留情况。由于ECS微型片表现出尺寸依赖性胃内滞留，其胃内滞留时间随着释放速率的降低而延长。在体内药效学研究中，与ECS混悬液相比，ECS的胃滞留剂型在即时刺激模型中不影响黏膜保护作用，但在延迟刺激模型中增强了该作用。这一发现表明，采用胃滞留剂型可延长ECS的黏膜保护作用持续时间，并为开发ECS胃滞留剂型提供了理论依据。
