埃索美拉唑三联与奥美拉唑三联疗法治疗Hp阳性十二指肠溃疡对比研究

目的比较埃索美拉唑三联与奥美拉唑三联疗法治疗幽门螺杆菌（Hp）阳性十二指肠球部溃疡的临床疗效。方法将104例经内镜诊断并检测证实Hp阳性的十二指肠球部溃疡患者随机分为两组。埃索美拉唑组（52例）：埃索美托唑20mg＋阿莫西林1g＋克托霉素500mg，每日2次，共7d；奥美拉唑组（52例）：奥美拉唑20mg＋阿莫西林1g＋克拉霉素500mg，每日2次，共7d。疗程结束4周后复查胃镜并检测Hp，观察腹痛缓解率、溃疡愈合率、Hp根除率及用药后的不良反应等。结果埃索美拉唑组第1天和第2天腹痛缓解率分别为34．6％和59、6％，高于奥美托唑组的17.3％和38．5％（P〈0．05）。埃索美托唑组和奥美拉唑组溃疡愈合率分别为92.3％和88．5％，Hp根除率分别为88．5％和82．7％，差异无显著性（P〉0．05）。两组用药后不良反应少，有较好的安全性。结论埃索美拉唑三联疗法治疗Hp阳性的十二指肠溃疡安全有效．腹痛缓解速度优于奥美拉唑三联疗法。     

艾司奥美拉唑、克拉霉素、阿莫西林短程三联疗法根除幽门螺杆菌

目的:观察艾司奥美拉唑、克拉霉素、阿莫西林短程三联疗法根除幽门螺杆菌(Hp)的疗效。方法:Hp阳性的活动性十二指肠溃疡病人44例,以艾司奥美拉唑20mg、克拉霉素500mg及阿莫西林1000mg,po,bid治疗,疗程7d,7d之后继服法莫替丁20mg,po,bid×3wk。观察Hp根除率、症状缓解和消失率、溃疡愈合率及不良反应。结果:Hp根除率为88%(按完成试验方案分析)和86%(按意图分析),d7症状缓解率为100%、消失率为72%,wk5溃疡愈合率为100%。不良反应发生率为14%,其中1例因皮疹退出。结论:艾司奥美拉唑、克拉霉素,阿莫西林三联短程疗法并后续法莫替丁治疗3wk,是当前治疗Hp阳性的活动性十二指肠溃疡的满意选择之一。     

埃索美拉唑治疗小儿胃食管反流临床观察

胃食管反流(gastro蛳oesophagealreflux disease,GERD)是指胃内容物,包括从十二指肠流入胃的胆盐和胰酶等反流入食管,分生理性和病理性2种。病理性反流是由于食管下括约肌功能障碍和(或)与其功能有关的组织结构异常,以至食管下括约肌压力低下而出现的反流,引起一系列如上腹痛、烧心、泛酸等临床症状。GERD是一种潜在的、较严重的长期疾病,不论有无食管炎的发生,它对人的生活质量有不同程度的不良影响。本研究目的是确认埃索美拉唑改善小儿GERD症状的疗效,同时评价药物在GERD小儿中应用的安全性和耐受性。1对象与方法1.1临床资料收集2…     

Site selective syntheses of [3H]omeprazole using hydrogen isotope exchange chemistry

Omeprazole (Prilosec®) is a selective and irreversible proton pump inhibitor used to treat various medical conditions related to the production of excess stomach acids. It functions by suppressing secretion of those acids. Radiolabeled compounds are commonly employed in the drug discovery and development process to support efforts including library screening, target identification, receptor binding, assay development and validation and safety assessment. Herein, we describe synthetic approaches to the controlled and selective labeling of omeprazole with tritium via hydrogen isotope exchange chemistry. The chemistry may also be used to prepare tritium labeled esomeprazole (Nexium®), the active pure (S)‐enantiomer of omeprazole.     

Improving opportunities for effective management of gastro-oesophageal reflux disease

The recent introduction of proton pump inhibitors has extraordinarily improved the therapeutic approach to gastro-oesophageal reflux disease. The concept of decreasing gastric acid secretion and increasing the pH in the lower oesophagus has been demonstrated to be therapeutically effective and the higher the level of pH achieved, the better the results. In spite of the evident efficacy of these molecules, there are still many patients who will continue to have symptoms despite medical treatment. Proton pump inhibitors suppress gastric acidity, but this effect shows a remarkable interindividual variation depending on different reasons. Thus, it is still possible to optimise medical therapy for gastro-oesophageal reflux disease. Esomeprazole, the S-isomer of omeprazole, has an advantageous metabolism and this particular feature translates into superior clinical efficacy. Clinical trials for initial and long-term treatment across the gastro-oesophageal reflux disease spectrum, have clearly demonstrated the superiority of esomeprazole over omeprazole, even if tolerability and safety are very similar.     

Esomeprazole: potent acid suppression in the treatment of acid-related disorders

Esomeprazole (S-omeprazole), an enantiomer of the racemate omeprazole, is the first proton pump inhibitor to be developed as an isomer. This confers improved pharmacokinetics and pharmacodynamics compared with the racemate R/S-omeprazole. The difference in the pharmacokinetics of esomeprazole compared with omeprazole and the R-isomer is due to reductions in total body clearance and first-pass metabolism in the liver. Pharmacodynamic studies showed that esomeprazole 40 mg provides greater intragastric acid control than respective doses of all the other proton pump inhibitors on the market. Several well-designed clinical trials, employing both endoscopic and symptomatic response criteria, have compared the efficacy of esomeprazole with that of other proton pump inhibitors in the management of gastroesophageal reflux disease patients, and in the eradication of Helicobacter pylori. In addition, the efficacy of esomeprazole for the healing and prevention of nonsteroidal anti-inflammatory drug-associated dyspeptic symptoms and ulcers has been established. The aim of this review is to provide an overview of the pharmacokinetics, pharmacodynamics and consequent clinical importance of esomeprazole in the treatment of acid-related disorders.     

埃索美拉唑镁三水合物生产新工艺

目的 探讨合成埃索美拉唑镁三水合物的新工艺.方法 以2-巯基-5-甲氧基苯并咪唑与2-氯甲基-3,5-二甲基-4-甲氧基吡啶盐酸盐为起始物料,经缩合、sharpless不对称氧化、成盐、离子交换及转晶制得埃索美拉唑镁三水合物.结果 采用该工艺得到46.2 kg符合药用晶型的埃索美拉唑镁三水合物白色固体,摩尔总收率64.7％,色谱纯度为99.9％,ee值为100％.结论 本工艺操作简便,收率较高,产品质量符合药用要求,能满足原料药工业化大生产需要.     

伊托必利和埃索美拉唑联合氟哌噻吨美利曲辛治疗功能性消化不良的临床疗效观察

目的：观察伊托必利和埃索美拉唑联合氟哌噻吨美利曲辛（黛力新）治疗功能性消化不良的临床疗效。方法将62例功能性胃肠病患者随机分为两组,对照组仅给予消化科常规治疗,使用伊托必利和埃索美拉唑,研究组在常规治疗的基础上给予黛力新,比较各组治疗前后患者消化道症状积分以及临床疗效。结果与对照组比较,两组治疗后消化道症状积分评分明显降低,症状缓解总有效率均显著高于对照组（P＜0．05）。结论伊托必利和埃索美拉唑联合黛力新治疗功能性消化不良,疗效确切,比伊托必利和埃索美拉唑有更好的临床疗效。