正交试验法优选左旋泮托拉唑的合成工艺条件

为了优化左旋泮托拉唑的合成工艺条件,以麦芽酚、扑热息痛为原料合成左旋泮托拉唑,通过正交试验法考察氧化剂与硫醚的摩尔比、催化剂与硫醚的摩尔比、反应温度、反应时间对左旋泮托拉唑合成产率的影响。优化工艺条件为:氧化剂与硫醚的比为1.2∶1,催化剂与硫醚的摩尔比为0.9∶1,反应温度为10~15℃,反应时间为10 h。以此优化条件下,产率达到72.7%。工艺条件温和、操作简便、适合工业化大生产。     

泮托拉唑钠与奥美拉唑治疗脑出血并发应激性溃疡出血疗效比较

目的对应用泮托拉唑钠和奥美拉唑治疗脑出血并发应激性溃疡出血的疗效进行对比观察。方法随机将96例患者分为泮托拉唑组和奥美拉唑组,在分别治疗5d后,评价疗效并进行对比观察。结果两组患者均有明显止血效果,泮托拉唑组用药48h显效率67.39%,总成功率95.65%,奥美拉唑组分别为40.00%和76.00%,泮托拉唑组疗效显著高于奥美拉唑组(P<0.05)。结论泮托拉唑治疗脑出血并发应激性溃疡疗效确切,无明显不良反应,且疗效明显优于法莫替丁,值得临床推广应用。     

泮托拉唑、克拉霉素、阿莫西林三联治疗十二指肠溃疡30例疗效

目的观察泮托拉唑、克拉霉素、阿莫西林三联疗法对十二指肠溃疡(DU)的疗效。方法将60例经电子胃镜检查确诊为DU活动期,并经活检取材行快速尿素酶试验确定幽门螺旋杆菌(HP)阳性的患者随机分为两组:泮托拉唑三联治疗组和奥美拉唑三联对照组各30例。两组均先予三联治疗:泮托拉唑胶囊40mg或奥美拉唑胶囊20mg 克拉霉素片500mg 阿莫西林胶囊1000mg,每天2次,连续7d,然后单独给予泮托拉唑40mg,每日1次,或奥美拉唑20mg每日1次,连续3周。治疗共4周后复查胃镜并检测HP,观察溃疡治愈率、HP根治率及不良反应率。结果泮托拉唑和奥美拉唑组治愈率分别为93.3%、90%;HP根除率90%、86.7%,两组差异均无显著性(P>0.05)。不良反应率泮托拉唑组低于奥美拉唑组(P<0.05),有显著差异性。结论泮托拉唑、克拉霉素、阿莫西林三联治疗DU效果好、不良反应少。     

思密达辅助治疗消化性溃疡疗效观察

目的为了观察思密达与泮托拉唑联合用药对消化性溃疡的疗效和安全性。方法56例消化性溃疡患者随机分为2组,抗Hp治疗l周后,治疗组予泮托拉唑+思密达治疗4周,对照组仅予泮托拉唑治疗4周后复查胃镜,并进行疗效判断。结果治疗组疗效优于对照组2组疗效有显著性差异。治疗组在缩短病程,提高疗效方面优于对照组。结论思密达辅助治疗消化性溃疡是有效和安全的方法。     

泮托拉唑联合施林治疗反流性食管炎的疗效观察

目的了解泮托拉唑联合施林治疗反流性食管炎的疗效情况。方法采用随机平行对照、单盲的临床试验。随机分为两组,治疗组(60例)和对照组(40例)。两组疗程均为4周。观察方法:治疗前后对反流、烧灼痛等症状各记录1次。结果两组治疗前后的临床症状变化及胃镜下反流性食管炎程度变化情况见表1、2。结论泮托拉唑与施林联合应用效果显著,明显优于单独应用泮托拉唑,值得临床推广应用。     

高血压脑出血并上消化道出血30例治疗体会

目的探讨高血压脑出血并发上消化道出血的治疗方法与效果。方法对30例高血压脑出血并发上消化道出血患者不同治疗方案的临床效果进行分析,其中对照组予常规脱水、降颅压及对症支持治疗,治疗组加用泮托拉唑治疗。结果治疗组的疗效明显好于对照组,治疗组死亡率较对照组低。结论泮托拉唑是治疗高血压脑出血并发上消化道出血的一种有效药物,其止血效果与预后好,值得临床推广。     

泮托拉唑钠肠溶胶囊治疗十二指肠溃疡的临床分析

目的观察泮托拉唑治疗幽门螺杆菌(Hp)相关性十二指肠溃疡的临床疗效。方法将入选病例随机分为治疗组50例、对照组50例。2组病例在性别、年龄、临床表现及内镜检查等方面无显著差异性。治疗组予以泮托拉唑钠肠溶胶囊+阿莫西林胶囊+甲硝唑片+痢特灵片治疗;对照组予以雷尼替丁胶囊+阿莫西林胶囊+甲硝唑片+痢特灵片治疗。结果经4周治疗发现,泮托拉唑治疗组患者明显改善临床症状(如反酸、烧心、上腹部疼痛等)并使溃疡愈合。雷尼替丁胶囊治疗组患者临床症状(如反酸、烧心、上腹部疼痛等)改善差并且溃疡愈合也相对差。结论泮托拉唑+阿莫西林胶囊+甲硝唑片+痢特灵片治疗可有效地控制十二指肠溃疡的临床症状,加速溃疡愈合,清除Hp的感染,是治疗十二指肠溃疡的一种有效、价廉的方法。     

左旋泮托拉唑钠、镁的合成

探讨了左旋泮托拉唑钠、镁的合成。以麦芽酚(2-甲基-3-羟基-4-吡喃酮)为起始原料,经过甲基化、氨化、氯化、氧化、甲氧基化、重排、水解、氯化反应合成得到2-氯甲基-3,4-二甲氧基吡啶盐酸盐;以扑热息痛(对乙酰氨基酚)为原料经过醚化、硝化、还原、环合反应合成5-二氟甲氧基-2-巯基-1H-苯并咪唑;二者缩合制得5-二氟甲氧基-2-{[(3,4-二甲氧基-2-吡啶基)甲基]硫}-1H-苯并咪唑;以D-(-)-酒石酸二乙酯为手性试剂,过氧化异丙苯为氧化剂,不对称氧化制得S-(-)-5-二氟甲氧基-2-[(3,4-二甲氧基-2-吡啶基)甲基]亚硫酰基-1H-苯并咪唑;然后与氢氧化钠、氯化镁成盐制得左旋泮托拉唑钠和左旋泮托拉唑镁。通过该法得到了目标产物左旋泮托拉唑钠和左旋泮托拉唑镁,且该合成方法操作简便。     

泮托拉唑注射液治疗上消化道出血的疗效观察

引起上消化道出血的病因主要有许多种,例如:食管胃底静脉曲张破裂、肿瘤等,它是消化系统疾病中最常见的急症。泮托拉唑的作用机理在于它是不可逆质子泵抑制剂,能够减少胃酸分泌。是治疗上消化道出血的常用药物,但其在临床使用过程中的有效性和安全性还有待进一步确定。     

血凝酶注射与内科治疗消化道出血的临床观察

目的对比血凝酶注射和内科治疗消化道出血时的医疗效果。方法将117例诊断为消化道出血的患者随机分为治疗组和观察组,治疗组采取白眉蛇毒血凝酶以及泮托拉唑注射的方式,观察组采取奥美拉唑40mg+5%葡萄糖液静脉注射及内服方式。结果治疗组的有效率为63.3%,高于观察组的49.1%。同时在其他病症上,治疗组的疗效也明显高于观察组,其中出血症状显效率为56.7%对42.1%,有效率为36.7%对28.1%,大便病症显效率为48.3%对31.6%,有效率为46.7%对33.3%。结论白眉蛇毒血凝酶以及泮托拉唑针注射是消化道出血治疗更有效的方法。     

难治性胃溃疡组织中VEGF表达的检测及意义

目的研究血管内皮生长因子(VEGF)在消化性溃疡发病中的作用,探讨难治性胃溃疡的血管分子学机制。方法收集30例因难治性溃疡和并发穿孔等并发症而行胃大部切除的患者作为难治性溃疡组,取其溃疡周边和远处组织,同时收集30例首诊为胃溃疡且经胃镜证实的患者,取溃疡周边和远处组织与难治性胃溃疡组作对照进行研究。采用免疫组化法检测VEGF蛋白表达。结果难治性溃疡组周边区的VEGF阳性细胞数为36,远处区为55,对照组溃疡周边区和远处区的阳性细胞数分别为57和70,两组患者溃疡周边区和远处区VEGF阳性细胞数组间和组内比较差别均有显著性意义(P<0.01)。结论VEGF表达水平显著降低。     

IL-1β-31、IL-10-819和TNF-α-1031基因多态性与幽门螺杆菌感染相关性胃溃疡及胃癌易感性的关系

目的分析人群中IL-1β-31、IL-10-819和TNF-α-1031基因多态性与幽门螺杆菌(H.pylori)感染相关性胃溃疡及胃癌易感性之间的关系,为临床诊断及预防该病提供新的思路和方法。方法选取H.pylori阳性的51例胃溃疡患者、43例胃癌患者和100例健康对照者,采用PCR-限制性长度片段多态法和多重引物特异PCR法,检测其IL-1β-31、IL-10-819和TNF-α-1031位点,分析其多态性。结果在胃溃疡组中TNF-α-1031各基因型的频率分布与健康对照组比较,差异有统计学意义。在胃癌组中TNF-α-1031各基因型的频率分布与健康对照组比较,差异有统计学意义;Logistic回归分析表明,与携带TNF-α-1031T/T者相比,携带TNF-α-1031C/C者发生胃溃疡的危险性为OR=5.84(95%CI:1.00～33.84),发生胃癌的危险性为OR=6.95(95%CI:1.19～40.63)。在疾病组和健康对照组中,IL-10-819和IL-1β-31各基因型频率的分布差异无统计学意义。结论 TNF-α-1031基因多态性与胃溃疡、胃癌的易感性相关。     

白细胞介素-1B和肿瘤坏死因子-α基因多态性与胃溃疡、胃癌易感性的相关性

目的探讨人群中白细胞介素-1B(IL-1B)和肿瘤坏死因子-α(TNF-α)基因多态性与胃溃疡、胃癌易感性的相关性。方法选取幽门螺杆菌阳性的39例胃溃疡患者、35例胃癌患者和70名健康对照者,采用聚合酶链式反应-限制性片段长度多态性(PCR-RFLP)分析法检测该人群中IL-1B-511、TNF-A-308和TNF-A-857基因多态性。结果疾病组与对照组中IL-1B-511各基因型频率的分布差异无统计学意义。与对照组比较,胃溃疡组TNF-A-308各基因型的频率分布、TNF-A-857各基因型的频率分布以及胃癌组TNF-A-308各基因型的频率分布差异均有统计学意义。经Logistic回归分析,与携带TNF-A-308G/G者比较,携带TNF-A-308A/A者发生胃溃疡的危险性为OR=21.62(95%CI:2.07～226.13);与携带TNF-A-857C/C者比较,携带TNF-A-857T/T者发生胃溃疡的危险性为OR=5.37(95%CI:1.28～22.50);与携带TNF-A-308G/G者比较,携带TNF-A-308A/A者发生胃癌的危险性为OR=16.41(95%CI:1.62～116.55)。结论TNF-α基因多态性与胃溃疡、胃癌的易感性相关。     

Significance of Lipoperoxides in Gastric Cancer

The “lipoperoxide hypothesis” proposed by the author, according to which cancer is generated by oxidized lipids accumulated in a living body, is valuable in understanding following phenomena in gastric cancer: decrease in the secretion of hydrochloric acid to gastric juice; relatively frequent occurrence of gastric cancer amongst people who take smoked, baked or dried fish and who live in a low and moist land or in an acidic soil region; gastric cancer often originates from gastric ulcer; males suffer more from this disease than females.     

依卡倍特钠的核磁共振数据解析

依卡倍特钠是日本田边公司生产的一种具有覆盖作用的抗胃炎、胃溃疡的新型药物。笔者对依卡倍特钠进行了1H NMR、13C NMR检测,并通过DEPT、gCOSY、gHMQC、gHMBC等2DNMR技术对其NMR数据进行较为详细的解析和NMR信号全归属,为今后的分析鉴定工作提供完善的NMR数据。     

Effect of a Cytoprotective Dose of Dehydroleucodine,Xanthatin, and 3-Benzyloxymethyl-5H-furan-2-one on Gastric Mucosal Lesions Induced by Mast Cell Activation

The aim of this study was to determine whether the lactones dehydroleucodine, xanthatin and 3-benzyloxymethyl-5H-furan-2-one, would be effective in an animal model of gastric ulcer induced by mast cell activation. Rats were divided into ten groups. Treatments were repeated for four days. The degree of gastric erosion was assessed with a scoring system and histological preparations. Gastric mast cell morphology was analyzed by histological procedures. Serum serotonin levels were determined as markers of mast cell activation. Statistical analyses were done using ANOVA and Tukey–Kramer test. We demonstrated that the repeated administration of compound 48/80 results in extensive mucosal lesions in the gastric mucosa and that such lesions occurred in association with mast cell degranulation and a significant increase of serum serotonin. We showed that these lesions were prevented by dehydroleucodine, xanthatin, and 3-benzyloxymethyl-5H-furan-2-one and that this effect was similar to that obtained with sodium cromoglycate. In conclusion, the results of the present study indicate that the optimal gastric cytoprotective dose of dehydroleucodine, xanthatin, and 3-benzyloxymethyl-5H-furan-2-one is efficacious in an animal model of gastric ulcer induced by mast cell activation. Our findings suggest that these lactones could be valuable tools for designing novel therapeutic agents for digestive disorders associated with inappropriate mast cell activation.     

瑞巴派特治疗胃溃疡的临床疗效观察

目的观察瑞巴派特治疗胃溃疡的疗效。方法将69例胃溃疡患者随机分成2组:试验组35例,在雷贝拉唑和阿莫西林治疗基础上加用瑞巴派特口服,0.1g/次,3次/d;对照组34例,在雷贝拉唑和阿莫西林治疗基础上加用铝碳酸镁口服,1.0g/次,3次/d。均治疗8周。治疗前及治疗2、4、6、8周对患者上腹痛、上腹胀、反酸和嗳气症状进行症状评分,治疗前、后分别行胃镜检查及胃黏膜组织病理学检查,并进行胃镜下疗效评分和胃黏膜慢性炎症程度、炎症活动程度评分。结果治疗后2组患者上腹痛、上腹胀、反酸和嗳气总积分间差别有统计学意义(P<0.05);胃镜评分间比较,差别无显著性意义(P>0.05);胃黏膜糜烂区慢性炎症程度及炎症活动程度评分间差别有统计学意义(P<0.05)。结论瑞巴派特治疗胃溃疡有良好的疗效。     

Healing,Antioxidant and Cytoprotective Properties of Indigofera truxillensis in Different Models of Gastric Ulcer in Rats

The present study evaluated the antiulcerogenic activity and mechanisms of the aqueous (AqF 100 mg/kg) and ethyl acetate (AcF 50 mg/kg) fractions from Indigofera truxillensis leaves. This dose was selected to assess its activity on ulcer healing and its action on gastric acid and mucus secretion, prostaglandin production and antioxidant enzyme activity (superoxide dismutase (SOD), glutathione peroxidase (GSH-Px) and glutathione reductase (GSH-Rd)). Gastric ulcer was induced by absolute ethanol. Antisecretory action, mucus and prostaglandin production, healing and antioxidant enzyme activities were evaluated for both fractions. AqF and AcF significantly inhibited the gastric mucosal damage caused by ethanol. This effect was statistically significant at 100 and 50 mg/kg compared with the vehicle. Neither fraction interfered with gastric secretion. AcF increased the PGE₂ production, and both fractions increased mucus production. l-NAME did not alter the gastroprotection exerted by the fractions, but N-ethylmaleimide attenuated only AcF. In the ischemia/reperfusion model both fractions inhibited the mucosal damage. AcF increased SOD, GSH-Px and GSH-Rd activity, but AqF increased only SOD and GSH-Px. In the acetic acid-induced ulcer model AcF only accelerated ulcer healing. These results showed that Indigofera truxillensis acted as a gastroprotective agent, stimulating protective factors and antioxidants enzymes.     

梅花鹿免疫细胞活性因子对乙醇型胃粘膜损伤模型鼠的保护作用

目的　观察梅花鹿免疫细胞活性因子 (SIAF)对小鼠乙醇型胃粘膜损伤的保护作用。方法　制备小鼠乙醇型胃粘膜损伤模型 ,测定溃疡指数 ,观察胃的出血情况 ,免疫组化染色检测胃粘膜EGFR的表达 ,用酶法测定血清中NO的含量。结果　SIAF组的溃疡指数、胃出血情况与模型组相比 ,差异均有显著意义。SIAF组小鼠损伤周围胃粘膜EGFR表达与模型组相比明显增强。该组小鼠血清NO含量与模型组相比也明显增高。结论　SIAF具有显著的保护此种胃粘膜损伤的作用