埃索美拉唑联合抗生素治疗幽门螺杆菌阳性萎缩性胃炎的临床研究

目的观察埃索美拉唑联合阿莫西林克拉维酸钾及左氧氟沙星对幽门螺杆菌(Hp)阳性慢性萎缩性胃炎(CAG)的临床疗效。方法 Hp阳性慢性萎缩性胃炎伴异型增生患者400例随机分为治疗组300例和对照组100例,治疗组给予埃索美拉唑40 mg,每天1次;阿莫西林克拉维酸钾片375 mg,每天2次;左氧氟沙星片100 mg,每天2次,均口服;对照组给予奥美拉唑肠溶胶囊20 mg,每天2次;阿莫西林胶囊1.0 g,每天2次;克拉霉素片0.25 g,每天2次,均口服。2组均治疗2周。60 d后行胃镜及组织学复查。结果消化道症状改善:治疗组总有效率为95.0%,高于对照组的72.0%(P<0.05);组织学观察:治疗组总有效率为94.0%,高于对照组的25.0%(P<0.01)。治疗组治疗后除纳差、嗳气、恶心外,其余各项评分均较对照组相应指标变化显著(P<0.05或P<0.01)。治疗组Hp转阴率为94.7%,高于对照组的71.0%(P<0.05)。2组不良反应比较差异无统计学意义(P>0.05)。结论埃索美拉唑联合阿莫西林克拉维酸钾及左氧氟沙星可以提高Hp根除率,且对CAG伴异型增生的逆转疗效显著。     

埃索美拉唑联合康复新液治疗食管癌、贲门癌术后胃食管反流病的疗效观察

目的：探讨食管、贲门癌术后胃食管反流病的治疗方法。方法：将本院收治的96例食管癌、贲门癌术后胃食管反流病患者随机分成两组,治疗组给予埃索美拉唑＋康复新液进行治疗,对照组给予埃索美拉唑治疗,观察两组的疗效和复发情况。结果：应用埃索美拉唑＋康复新液的患者总有效率高于应用埃索美拉唑的患者,差异有统计学意义（P〈0．05）。应用埃索美拉唑＋康复新液的患者1年后的复发率低于应用埃索美拉唑的患者,但差异无统计学意义（P〉0．05）。结论：埃索美拉唑＋康复新液在治疗食管、贲门癌术后胃食管反流病方面的临床有效率高于单用埃索美拉唑,两种治疗方法的复发情况没有差别。     

埃索美拉唑联合莫沙必利治疗反流性食管炎的临床疗效观察

目的观察埃索美拉唑联合莫沙必利治疗反流性食管炎的临床疗效和安全性。方法将100例反流性食管炎患者随机分为治疗组和对照组各50例,治疗组给予莫沙必利加埃索美拉唑治疗;对照组给予莫沙必利加奥美拉唑治疗。8周后将两组患者的临床综合疗效、内镜复查食管黏膜愈合情况及不良反应进行比较。结果治疗组的临床综合疗效、内镜下食管黏膜愈合情况优于对照组(均P<0.05),不良反应少。结论治疗组在反流性食管炎中的优势明显,安全性高,有较高的临床价值。     

埃索美拉唑肠溶胶囊人体生物等效性试验

目的采用高效液相色谱法测定受试者口服埃索美拉唑肠溶胶囊与埃索美拉唑镁肠溶片后血药浓度,评价埃索美拉唑肠溶胶囊的生物等效性。方法 2009年9月-10月,36例健康男性受试者单次交叉口服埃索美拉唑肠溶胶囊(试验制剂)和埃索美拉唑镁肠溶片(参比制剂),测定给药后不同时间点血浆中埃索美拉唑经时血药浓度,采用DAS 2.0软件进行药物代谢动力学参数计算和生物等效性评价。结果受试者单次口服试验制剂与参比制剂后,达峰时间分别为(2.19±0.96)、(2.43±0.92)h,峰浓度分别为(1 748.86±615.81)、(1 442.92±476.41)μg/L,药时曲线下面积(AUC)0-t分别为(3 927.14±1 839.10)、(3 878.79±1 734.84)μg/L.h,AUC0-∞分别为(3 998.36±1 866.22)、(3 918.31±1 773.44)μg/L.h。试验制剂与参比制剂的生物等效性为94.0%,其90%CI为(82.3%,107.2%)。结论埃索美拉唑肠溶胶囊与埃索美拉唑镁肠溶片生物等效。     

埃索美拉唑治疗反流性食管炎临床分析

目的探讨埃索美拉唑治疗反流性食管炎的临床疗效。方法将确诊的80例反流性食管炎患者分为治疗组和对照组,各40例。治疗组服用埃索美拉唑40mg,每日1次,对照组服用奥关拉唑40mg,每日1次,治疗4周后比较两组症状改善及治愈情况。结果经临床症状疗效观察,治疗组和对照组的愈显效率分别为72．5％和47．5％;内镜复查结果显示,治疗组愈显效率达92．5％,对照组愈显效率为80．0％。两组愈显效率比较差异有统计学意义（P〈0．05）。结论埃索美拉唑治疗反流性食管炎疗效显著,安全性较好。     

Preparation of esomeprazole zinc solid dispersion and study on its pharmacokinetics

Esomeprazole zinc (EZ) is a poorly water-soluble substance. In order to increase its dissolution rate and bioavailability, solid dispersions of esomeprazole zinc (SDEZ) in polyethylene glycol 4000 (PEG4000) with different EZ to PEG4000 ratios were prepared by solvent method. Our studies showed that dissolution rate of EZ were distinctively increased in the solid dispersion system compared to that in pure EZ or physical mixtures. The increase of dissolution rate was obviously related to the ratio of EZ to PEG4000. The solid dispersion system (EZ/PEG4000=1/8, w/w) gave the highest dissolution rate: about 14.7-fold higher than that of the pure EZ. EZ was proved to be in amorphous state in this solid dispersion by using differential scanning calorimetry (DSC) and scanning electron microscopy (SEM) techniques. In vivo administration studies, SDEZ in enteric capsule (SDEZ-EC) has a lower Cmax and a longer Tmax than that of esomeprazole magnesium enteric-coated tablet (Nexium), and the differences of Cmax and Tmax between SDEZ-EC and Nexium are significant. This result suggests SDEZ-EC has a lower absorption rate than Nexium and corresponds with the in vitro dissolution.     

Effects of esomeprazole on glutathione levels and mitochondrial oxidative phosphorylation in the gastric mucosa of rats treated with indomethacin

Proton pump inhibitors exert their preventive and healing effects on gastropathy induced by nonsteroidal anti-inflammatory drug (NSAIDs) by a dual action: the antisecretory and the antioxidant effect. The latter was investigated by using esomeprazole against indomethacin-induced gastric mucosa lesions in rats and assessed by a histomorphometric analysis. Treatment by intragastric gavage were 1% methocel as vehicle; esomeprazole 10, 30, or 60 μmol/kg; indomethacin 100 μmol/kg; and esomeprazole 10, 30, or 60 μmol/kg plus indomethacin 100 μmol/kg. The evaluation of glutathione (GSH) levels and respiratory chain complex activities [nicotinamide adenine dinucleotide, reduced (NADH)-ubiquinone oxidoreductase, succinate dehydrogenase, cytochrome C reductase, cytochrome oxidase] was performed in the isolated gastric mucosa. Esomeprazole (10–60 μmol/kg) dose dependently reversed, up to complete recovery, the inhibitory effect of indomethacin on GSH levels (approximately 60% inhibition) and mitochondrial enzyme activities (inhibition ranging from 60% to 75%). Indomethacin-induced mucosal injuries were reduced by esomeprazole. Thus, in addition to inhibiting acid secretion, the gastroprotective effect of esomeprazole can be ascribed to a reduction in gastric oxidative injury.     

埃索美拉唑与奥美拉唑治疗十二指肠溃疡疗效比较

目的：评估埃索美拉唑治疗十二指肠溃疡（duodenal ulcer,DU）的临床疗效和安全性。方法70例DU患者,分别用埃索美拉唑片剂40 mg,qd和奥美拉唑胶囊40 mg,qd进行治疗,胃镜观察溃疡愈合程度。结果4周后埃索美拉唑组和奥美拉唑组溃疡愈合率分别为91.4%和88.6%,总有效率分别为97.1%和94.2%。但埃索美拉唑比奥美拉唑缓解DU疼痛更为快速,埃索美拉唑组1 d内的疼痛消失率为42.9%,而奥美拉唑组为14.3%。结论埃索美拉唑治疗DU具有较好的疗效,且无明显不良反应,值得临床推广。     

耐信与奥美拉唑联合莫沙必利治疗反流性食管炎的临床疗效对比

目的：对比耐信联合莫沙必利与奥美拉唑联合莫沙必利治疗反流性食管炎的临床疗效。方法将78例反流性食管炎患者随机分为对照组与治疗组,对照组行奥美拉唑联合莫沙必利治疗,治疗组行耐信联合莫沙必利治疗。对比2组患者的临床疗效。结果治疗8周后治疗组临床症状评分显著低于对照组（P<0.05）。2组患者胃镜判定治疗有效率无统计学差异（P<0.05）。结论耐信联合莫沙必利是治疗反流性食管炎的有效方案,在改善患者临床症状方面较奥美拉唑有更好的效果。     

埃索美拉唑联合莫沙比利治疗反流性食管炎的临床研究

目的：评价埃索美拉唑联合莫沙比利治疗反流性食管炎安全性、有效性。方法2013年5月~2015年5月,观察组与对照组各入选40例GERD,分别采用埃索美拉唑联合莫沙必利、单独应用莫沙必利治疗,对比疗效、不良反应发生例。结果观察组痊愈率42.5%、愈显率92.5%高于对照组22.5%、60.0%,差异具有统计学意义（P<0.05）;对照组未见不良反应,观察组出现1例骨质疏松症、1例胸痛,差异无统计学意义（P>0.05）。结论埃索美拉唑联合莫沙必利治疗GERD疗效较好,安全可靠。