Bioequivalence Evaluation of Two Rebamipide Preparations After a Single Oral Dose to Healthy Korean Volunteers
试验速览
- 阶段
- 不适用
- 状态
- 已完成
- 入组人数
- 30
- 试验地点
- 1
- 主要终点
- Serum concentration of rebamipide
研究概览
简要总结
The aims of this study were to evaluate the pharmacokinetic properties and bioequivalence of two rebamipide preparations in healthy Korean male volunteers for generic substitution and to evaluate the association between the genetic polymorphisms in ABCB1 gene (exon 21 and 26) and rebamipide disposition.
详细描述
A randomized, single-dose, 2-period crossover design with a 7-day washout period was conducted in 30 healthy Korean male volunteers. Subjects were randomly assigned to receive a single 100-mg dose of the test or reference preparation of rebamipide, administered with 240 mL of water after a 12-hour overnight fast. All subjects were selected after passing a clinical screening procedure that included a physical examination and laboratory tests. Serum concentrations of rebamipide up to 12 hours after administration were determined using a validated HPLC method with fluorescence detection. Adverse events (AEs) were continuously monitored by clinical staff via observation, personal interview, and vital signs (temperature, blood pressure, heart rate) during the study period. All adverse events were recorded on the clinical record form per subject up to 1 week after the study. Pharmacokinetic parameters were determined using a noncompartmental method. The preparations were considered bioequivalent if the log-transformed ratios of AUC0-t, AUC0-∞, and Cmax were within the predetermined bioequivalence range (ie, 80-125%), as set by the US Food and Drug Administration (FDA) and Korean legislation. In vitro dissolution profiles of both preparations were examined and the influence of genetic polymorphisms in ABCB1 gene (P-glycoprotein) on the pharmacokinetics of rebamipide was also investigated.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 主要目的
- Treatment
- 盲法
- None
入排标准
- 年龄范围
- 19 Years 至 50 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Subjects were selected after passing a clinical screening procedure that included a physical examination and laboratory tests (blood analysis; hemoglobin, hematocrit, RBC, WBC, platelet, differential counting of WBC, total proteins, albumin, ALT, AST, alkaline phosphatase, total bilirubin, cholesterol, creatinine, blood urea nitrogen, and fasting glucose and urine analysis; specific gravity, color, pH, sugar, albumin, bilirubin, RBC, WBC and cast).
排除标准
- •Subjects possibly sensitive to this type of preparation,
- •Subjects who had a history of any hepatic illness,
- •Subjects who had a history of any renal illness,
- •Subjects who had a history of any respiratory illness,
- •Subjects who had a history of any endocrine illness,
- •Subjects who had a history of any cardiovascular system illness,
- •Subjects who had taken alcohol within 4 weeks prior to the study,
- •Subjects who had taken other preparations within 4 weeks prior to the study.
研究组 & 干预措施
Rebamipide, Serum concentration, Tablet
The test preparation, Rebamide® (containing 100 mg of rebamipide; lot No. KP005; expiration date, April 2010; Kyungdong Pharmaceutical Company, Seoul, Korea) and the reference preparation, Mucosta® (containing 100 mg of rebamipide; lot No. MC704067; expiration date, May 2010; Korea Otsuka Pharmaceuticals Co., Ltd., Seoul, Korea)
干预措施: Rebamide (Drug)
结局指标
主要结局
Serum concentration of rebamipide
时间窗: Pre-dose (to serve as a control) and at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, and 12 hours after oral administration of rebamipide tablet (100 mg)
次要结局
- Genetic polymorphisms in ABCB1 gene (exon 21 and 26)(A 3-mL blood sample was taken from each subject who participated in our bioequivalence studies before administration of rebamipide.)