Naito Y, Yoshikawa T, Iinuma S, Miyazaki R, Yagi N, Yoshida N, Osumi T, Hirao Y, Kondo M
First Department of Medicine, Kyoto Prefectural University of Medicine, Japan.
Arzneimittelforschung. 1996 Jul;46(7):698-700.
The potential anti-ulcer action of rebamipide (CAS 11911-87-6, OPC-12759) on experimental and clinical injury to the gastric mucosa depends on its presence in sufficient concentration in the gastric mucosa. To investigate its local penetration, rebamipide levels in the gastric mucosa and serum were measured. A dose of 100 mg of rebamipide was given orally (tablet) to patients with chronic gastritis (n = 32). Gastroscopy was performed between 22 and 353 min after drug ingestion. Venous blood was sampled for determination of serum concentrations. Samples were analyzed by high-performance liquid chromatography (HPLC). The maximal concentration in the gastric mucosa was reached after 30-60 min, and the concentration remained elevated for about 120 min thereafter. The mean mucosal concentration of rebamipide between 30 and 120 min after ingestion was 60.0 +/- 109.8 micrograms/g of tissue, which was higher than 0.1 mmol/l (37 micrograms/g of tissue). The serum concentration of rebamipide peaked about 30-60 min after drug ingestion and remained elevated for about 5 h thereafter. The mean serum concentration of rebamipide between 30 and 120 min after ingestion was 0.25 +/- 0.23 microgram/ml, being below the level of 1.0 mumol/l (0.37 microgram/ml). Data indicate that the concentration of rebamipide in the gastric mucosa resulted from local penetration, and suggest that the blood level and systemic distribution of rebamipide have little effect on its antioxidative and anti-neutrophilic activities.
瑞巴派特（CAS 11911-87-6，OPC-12759）对实验性和临床胃黏膜损伤的潜在抗溃疡作用取决于其在胃黏膜中达到足够的浓度。为研究其局部渗透情况，对胃黏膜和血清中的瑞巴派特水平进行了测定。给予32例慢性胃炎患者口服100 mg瑞巴派特（片剂）。在服药后22至353分钟之间进行胃镜检查。采集静脉血样以测定血清浓度。样品通过高效液相色谱法（HPLC）进行分析。胃黏膜中的最大浓度在30 - 60分钟后达到，此后该浓度持续升高约120分钟。服药后30至120分钟之间瑞巴派特的平均黏膜浓度为60.0±109.8微克/克组织，高于0.1 mmol/l（37微克/克组织）。瑞巴派特的血清浓度在服药后约30 - 60分钟达到峰值，此后持续升高约5小时。服药后30至120分钟之间瑞巴派特的平均血清浓度为0.25±0.23微克/毫升，低于1.0μmol/l（0.37微克/毫升）的水平。数据表明，胃黏膜中瑞巴派特的浓度是由局部渗透所致，并提示瑞巴派特的血药浓度和全身分布对其抗氧化及抗中性粒细胞活性影响较小。
