雷贝拉唑胶囊和片剂的药动学和生物利用度

目的:研究雷贝拉唑胶囊和片剂的药动学与相对生物利用度,评价其生物等效性。方法:18名男性健康志愿者随机分2组,按双周期交叉口服雷贝拉唑的2种制剂,剂量40mg,用高效液相色谱法测定给药后不同时间点血浆中雷贝拉唑的浓度,计算2种制剂药动学参数和相对生物利用度,并评价其生物等效性。结果:口服雷贝拉唑片和雷贝拉唑胶囊的药动学参数:cmax分别为(1050±s470)和(1149±750)μg·L-1;tmax分别为(3.3±1.1)和(3.2±0.8)h;t12ke分别为(1.7±0.9)和(1.6±0.7)h;AUC0～t分别为(4211±3225)和(4373±3578)μg·h·L-1;AUC0～∞分别为(4340±3568)和(4478±3732)μg·h·L-1。2制剂间无显著差异(P>0.05)。雷贝拉唑胶囊相对生物利用度F0～t为(103±29)%。结论:方差分析及双单侧t检验表明,雷贝拉唑胶囊和片剂具有生物等效性。     

3种疗程三联疗法根除十二指肠溃疡病人幽门螺杆菌感染的比较(英文)

目的 :通过与 7d三联疗法比较 ,观察 3d和 5d三联疗法根除幽门螺杆菌 (Hp)和治疗十二指肠溃疡的疗效。方法 :116例经胃镜检查确诊为十二指肠溃疡活动期并经快速尿素酶试验和血清抗Hp抗体 (ELASE)或病理学检查确定为Hp阳性的病人分为 3组 :3d(3d组 ,39例 )和 5d试验组 (5d组 ,37例 )和 7d对照组 (7d组 ,4 0例 )。 3组均给予三联治疗 :雷贝拉唑 10mg +呋喃唑酮 10 0mg +克拉霉素 2 5 0mg ,每日 2次 ,疗程分别为 3,5和 7d ,后再给予雷贝拉唑 10mg ,每日 1次 ,3d组为 2 5d ,5d组为 2 3d ,7d组为 2 1d。并于抗Hp方案结束后d 2 8～ 5 6内作13C 尿素呼气试验判断Hp根除率的效果。同时在用药后d 1,3,5 ,7,2 1和 35对病人的上腹痛、反酸以及上腹烧灼感等症状进行评估。结果 :10 7例病人完成全部治疗方案 ,9例失访 ,3,5 ,7d组人数分别为 37,35 ,35例。Hp根除率 3d组为 76 % (2 8/ 37) ,5d组为 89% (31/ 35 ) ,7d组为91% (32 / 35 ) ,5d组和 7d组之间差异无显著意义(P >0 .0 5 ) ,且均高于 3d组 (P <0 .0 5 )。3组从用药d 1起均能有效改善病人的上腹痛、反酸、上腹烧灼感等症状 ,各组症状缓解率无显著差异 (P >0 .0 5 )。结论 :3组治疗方案均能有效缓解十二指肠溃疡病人的症状 ,而根除Hp ,5d和 7d疗程较 3d疗程为优     

反相高效液相色谱法测定雷贝拉唑的血药浓度

目的　建立测定雷贝拉唑血药浓度的高效液相色谱(HPLC)方法。方法　色谱条件 :luna C8色谱柱 ,流动相为 2 0mmol·L-1 磷酸盐缓冲液 (pH7 0 ) /乙腈 (70 / 30 ,V/V) ,流速1 2ml·min-1 ,测定波长 2 88nm ,以雷贝拉唑峰面积定量。结果　雷贝拉唑的标准曲线为 ^Y =1 2 4 95 0X - 80 6 0 5 (r =0 999) ,线性范围为 0 0 1～ 0 75mg·L-1 ,具有良好的线性关系 ;其 0 0 5、0 1、0 5mg·L-1 3个浓度的血清样本回收率分别为 75 2 3%± 3 0 2 %、84 2 3%± 3 33%、91 0 5 %± 7 5 1 % ;日内变异分别为 5 0 9%、9 2 0 %、6 75 % ;日间变异分别为8 2 5 %、3 5 1 %、4 1 9%。结论　该方法简便、快速且无干扰 ,满足测定要求 ,可用于雷贝拉唑的药代动力学研究     

Rabeprazole improves health-related quality of life in patients with erosive gastroesophageal reflux disease

The purpose of this study was to assess the effect of rabeprazole 20 mg once a day on patient-reported health-related quality of life in routine clinical practice. Patients with erosive gastroesophageal reflux disease participating in an open-label, 8-week study completed the SF-36 Health Survey before and after treatment with rabeprazole. For all SF-36 scales, there was a statistically significant (p 0.007) improvement in mean scores from baseline to week 8. Improvements in each of the subscales, except for physical functioning, general health, and mental health, were at least 5% in magnitude, a level considered clinically meaningful. Furthermore, while baseline scores were significantly poorer than general United States population scores, follow-up scores for four of the subscales (role limitations due to physical problems, social functioning, role limitations due to emotional problems, and mental health) were comparable to general population scores. In conclusion, rabeprazole significantly improved health-related quality of life in erosive gastroesophageal reflux disease patients and restored social functioning and emotional well-being to levels comparable to those observed in the United States general population.     

CYP2C19 genotype and the PPIs – focus on rabeprazole

Abstract:   Amongst all the proton pump inhibitors (PPI), the hepatic metabolism of rabeprazole is least dependent on the CYP4502C19 system. Rabeprazole is therefore the PPI least affected by CYP4502C19 genetic polymorphism. This unique feature of rabeprazole complements rabeprazole's fast onset of action, and may lead to profound and consistent inhibition of gastric acid secretion in the treatment of acid-related disorders.     

Long-term efficacy and safety of rabeprazole in patients taking low-dose aspirin with a history of peptic ulcers: a phase 2/3, randomized,parallel-group, multicenter,extension clinical trial

A 24-week, double-blind, clinical trial of rabeprazole for the prevention of recurrent peptic ulcers caused by low-dose aspirin (LDA) has been reported, but trials for longer than 24 weeks have not been reported. The aim of this study is to assess the long-term efficacy and safety of rabeprazole for preventing peptic ulcer recurrence on LDA therapy. Eligible patients had a history of peptic ulcers on long-term LDA (81 or 100 mg/day) therapy. Patients with no recurrence of peptic ulcers at the end of the 24-week double-blind phase with rabeprazole (10- or 5-mg once daily) or teprenone (50 mg three times daily) entered the extension phase. Rabeprazole doses were maintained for a maximum of 76 weeks, including the double-blind 24-week period and the extension phase period (long-term rabeprazole 10- and 5-mg groups). Teprenone was randomly switched to rabeprazole 10 or 5 mg for a maximum of 52 weeks in the extension phase (newly-initiated rabeprazole 10- and 5-mg groups). The full analysis set consisted of 151 and 150 subjects in the long-term rabeprazole 10- and 5-mg groups, respectively, and the cumulative recurrence rates of peptic ulcers were 2.2 and 3.7%, respectively. Recurrent peptic ulcers were not observed in the newly-initiated rabeprazole 10- and 5-mg groups. No bleeding ulcers were reported. No clinically significant safety findings, including cardiovascular events, emerged. The use of long-term rabeprazole 10- and 5-mg once daily prevents the recurrence of peptic ulcers in subjects on low-dose aspirin therapy, and both were well-tolerated.     

Early effects of lafutidine or rabeprazole on intragastric acidity: which drug is more suitable for on-demand use?

Background Medication for the relief of heartburn should have the rapid onset of action required for on-demand use. We studied the inhibition of gastric acid secretion by lafutidine and rabeprazole, given in single doses to fasting and postprandial subjects.Methods A total of 22 healthy male, Helicobacter pylori-negative volunteers participated in this randomized, two-way crossover study. They were randomly assigned to receive a single oral dose of 10mg lafutidine or 20mg rabeprazole after fasting overnight (12 subjects, fasting study) or after eating a test meal (noodles, 364kcal; protein, 10.1g; fat, 16g; carbohydrates, 44.9g; NaCl, 1.1g; 10 subjects, postprandial study). Intragastric pH was monitored continuously for 6h after treatment. The other drug was given after a washout period of at least 7 days, and intragastric pH was similarly monitored.Results In the fasting study, lafutidine sustained pH at >3 and >4 during the second, third, fourth, fifth, and sixth hours of the study for significantly longer than rabeprazole. During the first 6h after treatment, lafutidine sustained pH at more than 2, 3, 3.5, 4, 5, 6, and 7 longer than rabeprazole. In the postprandial study, lafutidine sustained pH >3 and >4 for longer periods than rabeprazole during the third, fourth, fifth, and sixth hours of the study. During the first 6h after treatment, lafutidine sustained pH at more than 2, 3, 3.5, 4, 5, 6, and 7 longer than rabeprazole.Conclusions Lafutidine 10mg produces a prompter rise in intragastric pH than rabeprazole 20mg in fasting and postprandial Helicobacter pylori-negative male subjects.     

雷贝拉唑、阿莫西林联合甲硝唑对幽门螺旋杆菌的临床效果观察

目的 探讨雷贝拉唑、阿莫西林联合甲硝唑对幽门螺旋杆菌的临床效果。方法 选取2016年1月—2017年12月于中国人民解放军第464医院诊治的幽门螺旋杆菌患者90例进行前瞻性研究,采用随机数字法分为观察组（45例）和对照组（45例）,对照组患者给予奥美拉唑、阿莫西林联合甲硝唑,观察组患者给予雷贝拉唑、阿莫西林联合甲硝唑,两组患者均接受治疗4周。比较两组患者临床治疗有效率,腹胀、腹痛、反酸及嗳气的缓解时间及不良反应发生率。结果 观察组患者的有效率为91.11%,对照组患者的治疗有效率为73.33%,差异具有统计学意义（P<0.05）。与对照组相比,观察组患者的腹胀、腹痛、反酸及嗳气缓解时间均显著缩短,差异具有统计学意义（P<0.05）。观察组患者的不良反应发生率为13.33%,对照组患者的不良反应发生率为17.78%,差异无统计学意义。结论 雷贝拉唑、阿莫西林联合甲硝唑对幽门螺旋杆菌的临床治疗效果较好,能够有效改善患者的临床症状,具有积极的临床意义。     

Therapeutic efficacy and safety of Kangfuxin in combination with rabeprazole in the treatment of peptic ulcer: A systematic review and meta-analysis

Background:Kangfuxin (KFX), a well-known Chinese patent medicine which extracted from Periplaneta americana, is widely used as an adjuvant in the treatment of peptic ulcers (PUs) with proton pump inhibitors (PPIs) such as rabeprazole, in China. However, no clear consensus has been reached on the efficacy for PU treatment.Methods:We searched in 7 electronic databases to find randomized controlled trials (RCTs) completed before May 31, 2020 to explore the clinical efficiency of KFX plus rabeprazole in the treatment of PU. Risk ratio (RR) corresponding to 95% confidence interval (CI) was calculated to estimate the outcomes. Publication bias was assessed by both Egger''s and Begg''s tests. Statistical analyses were performed using RevMan 5.4 and Stata version 10.0.Results:Twenty-five RCTs, comprising 2555 PU patients, were included in this study. Meta-analysis showed that, when compared with rabeprazole-based treatment alone, KFX plus rabeprazole significantly improved the healing rate (RR = 1.34, 95% CI 1.25–1.44) and overall response rate of ulcers (RR = 1.16, 95% CI 1.13–1.20), alleviated the clinical symptoms of PU (RR = 1.14, 95% CI 1.08–1.21), and reduced the recurrence of PU (RR = 0.38, 95% CI 0.24–0.61) without an increase in the occurrence of adverse events (RR = 0.92, 95% CI 0.66–1.28).Conclusion:Our study suggests that KFX combined with rabeprazole showed positive therapeutic effects and is safe for treating PU, which may provide more reliable evidence for the clinical use of KFX in the treatment of PU.