奥美拉唑胶囊的含量及体外溶出度比较

国产奥美拉唑胶囊（商品名为奥克）是中国医学科学院药物研究所和常州四药制药有限公司共同研制的。瑞典Astra公司生产的奥美拉唑胶囊（商品名为洛赛克）。奥美拉唑作为第一个质子泵抑制剂出现，使消化性溃疡的治疗进入了新纪元。它具有疗效高疗程短耐受性好和复发率低的优点。为了比较国产及进口奥美拉唑胶囊的我们用HPLC测定了两种奥美拉唑胶囊的含量及体外溶出度。并进行比较。     

奥美拉唑治疗反流性食管炎疗效观察

观察奥美拉唑（奥克）治疗反流性食管炎的疗效。40例反流性食管炎随机分为两组,治疗组20例,服奥克20mgBid,一周后改为20mgqd;对照组20例,服雷尼替丁150mgBid,共6周,治疗组的临床症状缓解,有效率与对照组比较有显性差异。结论：奥克治疗反流性食管炎有较满意的临床疗效。     

奥克——国产奥美拉唑治疗十二指肠球部溃疡疗效观察

奥美拉唑(Omeprazole)是目前国际公认的、最新的消化性溃疡强效胃酸泵抑制剂。该药由瑞典Astra医药公司生产,商品名洛赛克(Losec)。1991年国产奥美拉唑问世,商品名为奥克,由常州第四制药厂生产。我院近两年对奥克进行了临床对比研究及疗效评     

2007～2009年我院质子泵抑制剂利用调查

目的：了解我院近年来质予泵抑制剂（PPIs）的应用情况及趋势。方法：对PPIs的品种、销售金额、用药频度（DDDs）、日均费用（DDC）进行综合分析。结果：2007～2009年我院PPIs的销售金额占消化系统销售金额的40％以上,每年以20％～30％的速度增长,高于整个消化系统用药的增长速度;口服PPIsDDDs比例为85％,DDC7．28～7．91元,注射PPIsDDDs比例为15％,DDC61．14—71．70元;销售金额前3位是：奥美拉唑钠（IV）两个国产品种和雷贝拉唑;DDDs前3位：奥美拉唑（奥克）、雷贝拉唑和兰索拉唑。结论：PPIs是一类发展潜力巨大的药物,兰索拉唑增长速度最快,我院PPIs的使用基本合理。     

国产奥美拉唑制剂治疗消化性溃疡的临床研究

目的:探讨国产奥美拉唑(奥克)联合抗生素治疗消化性溃疡的疗效。方法:将符合条件的病人随机分为奥克三联组(A组)和雷尼替丁三联组(B组),治疗4周后复查胃镜并检测Hp,观察两组溃疡愈合率及Hp根除情况。结果:A组和B组溃疡愈合率分别为92.2%(59/64)和53.4%(30/56),两组比较有高度显著性差异(P<0.01)。A组和B组Hp根除率分别为89.06%(57/64)和64.24%(36/56),两组有显著性差异(P<0.05)。两种治疗方法副作用均较少,患者能耐受治疗。结论:奥克三联疗法对消化性溃疡的疗效和对Hp的根除率明显优于雷尼替丁三联组,国产奥美拉唑制剂奥克是一种高效、价廉、副作用少的治疗消化性溃疡的新型国产PPI制剂。     

奥美拉唑治疗反流性食管炎疗效观察

观察奥美拉唑(奥克)治疗反流性食管炎的疗效.40例反流性食管炎随机分为两组,治疗组20例,服奥克20 mgBid,一周后改为20 mg qd;对照组20例,服雷尼替丁150 mg Bid,共6周.治疗组的临床症状缓解,有效率与对照组比较有显著性差异.结论奥克治疗反流性食管炎有较满意的临床疗效.     

奥美拉唑在儿科门诊超说明书用药分析

目的　对广东省妇幼保健院儿科门诊奥美拉唑的超说明书应用状况进行分析,为儿童合理使用奥美拉唑提供临床参考。方法　采用回顾性调查方法,对2020年3月至10月广东省妇幼保健院儿科门诊使用奥美拉唑的相关用药数据进行收集、统计分析。结果　收集和审查儿科门诊使用奥美拉唑制剂的处方共930张,以口服剂型为主（921张,99.03%）;在使用奥美拉唑制剂处方中,治疗疾病分类排名前3位分别为奥美拉唑制剂主要用于治疗急、慢性胃炎［51.40%（478/930）］、幽门螺旋杆菌感染［22.26%（207/930）］和消化不良［11.29%（105/930）］。联合用药处方746张,奥美拉唑与抗菌药物（279张,37.40%）、胃黏膜保护剂（151张,20.24%）和微生态制剂（143张,19.17%）联合使用。结论　奥美拉唑在广东省妇幼保健院儿科门诊的超说明书用药主要为超适应人群和超适应证用药的类型,用法符合循证医学要求,处方的治疗范围和给药方案均合理。医生与药师应共同推进奥美拉唑制剂的合理使用,使儿童用药安全、有效。     

2018年某院住院患者口服质子泵抑制剂的临床用药分析

目的:分析我院住院患者使用口服质子泵抑制剂(PPIs)的情况及其合理性。方法:回顾性分析我院口服PPIs的应用情况。结果:2018年我院住院患者口服PPIs的销售金额从高到低排序为济诺(雷贝拉唑肠溶胶囊)、波利特(雷贝拉唑钠肠溶片)、奥克(奥美拉唑肠溶胶囊)、耐信(艾司奥美拉唑镁肠溶片)、洛赛克(奥美拉唑镁肠溶片);用药频度(DDDs)排序从高到低为济诺、奥克、波利特、耐信、洛赛克。结论:2018年我院住院患者使用口服PPIs是合理的,济诺作为第二代PPIs,在我院具有更多临床应用。     

生长抑素与奥美拉唑治疗上消化道出血的成本-效果分析

目的 比较生长抑素和奥美拉唑治疗上消化道出血的经济效果.方法 采用药物经济学原理对不同治疗方案进行成本-效果分析.结果 生长抑素（A组）与奥美拉唑（B组）治疗上消化道出血有效率分别为96.29%和89.06%,无显著差异（P＞0.05）,成本-效果比分别为2 873.61和1 770.13.结论 奥美拉唑治疗上消化道出血为一种经济、有效的方案.     

奥美拉唑对利培酮和9-羟利培酮血药浓度影响的研究

目的：观察奥美拉唑对利培酮和9-羟利培酮血药浓度的影响。方法20例精神分裂症合并胃溃疡患者,给予利培酮联合奥美拉唑治疗1周。检测奥美拉唑治疗后利培酮以及9-羟利培酮血药浓度。结果未使用奥美拉唑前,利培酮与9-羟利培酮血药浓度为（29.25±7.82）μg/L;使用奥美拉唑后,利培酮与9-羟利培酮血药浓度为（37.15±11.68）μg/L,差异有统计学意义（P〈0.05）。结论奥美拉唑能够提高利培酮与9-羟利培酮血药浓度,因此,临床上治疗精神分裂症合并胃溃疡患者,给予奥美拉唑联合利培酮治疗时,应该监测患者利培酮与9-羟利培酮血药浓度,及时对药物剂量进行调整。     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.