HPLC法测定盐酸依托必利分散片的含量

盐酸依托必利为新型取代苯甲酰胺类胃肠动力促进剂 ,根据其结构特点 ,本文选用HPLC法测盐酸依托必利分散片的含量 ,该方法灵敏度高 ,重现性好。1 仪器与色谱条件TSP高效液相色谱仪 ,UV - 6 0 0 0紫外检测器。色谱柱 :phenomenex -C184 6 0× 2 5 0mm ;流动相 :0 0 5mol/L醋酸钠溶液 (用冰醋酸调节 pH值至 5 0 )-甲醇 (6 0∶4 0 ) ;流速 :1 0ml/min ;检测波长 :2 5 8nm。2 样品与试剂　盐酸依托必利对照品 (药厂提供 ,含量 99 6 % ) ;盐酸依托必利分散片 (威海迪沙药业有限公司 ) ;甲醇为色谱纯 ;醋酸钠为分析纯。　　 3 线性关系考…     

艾普拉唑治疗难治性胃食管反流病62例

目的 探讨艾普拉唑、氯波必利及硫糖铝联合应用治疗难治性胃食管反流病(refractory gastroesophageal reflux disease,rGERD)的临床效果.方法 将我院收治的62例rGERD随机分为艾普拉唑组32例,治疗方案为艾普拉唑+氯波必利+硫糖铝;泮托拉唑组30例,治疗方案为泮托拉唑+氯波必利+硫糖铝.8周后通过临床症状评分和胃镜复查结果进行效果评价.结果 治疗8周后,艾普拉唑组和泮托拉唑组临床症状评分改善率分别为93.8%和83.3%,两组比较差异有统计学意义(X2=0.799,P<0.05);两组胃镜检查结果显示有效率分别为90.6%和76.7%,两组比较差异亦有统计学意义(X2=1.318,P<0.05).结论 艾普拉唑、泮托拉唑联合氯波必利和硫糖铝治疗rGERD效果均显著,但艾普拉唑组效果更优于泮托拉唑组.     

某综合医院胃动力药1998～2002年药物利用分析

目的 :了解医院胃动力药的用药情况及趋势 ,为临床合理用药提供参考。方法 :对某院 5年来 7种胃动力药的年消耗量、限定日剂量、用药频度 ,不同的品种的胃动力药的价格比进行统计分析。结果 :DDDs·d-1排序从高到低依次为多潘立酮、莫沙必利、甲氧氯普胺、曲美布汀、胃肠舒、西沙必利、氯波必利。结论 :该院的胃动力药随着年度的增长 ,用药品种有所改变 ,但以多潘立酮 (吗丁林 )的使用频度为最高。     

帕可(氨磺必利片)——齐鲁制药在精神科治疗领域又一力作

<正>帕可(氨磺必利片)是齐鲁制药有限公司历经7年研制开发的产品,属于国内氨磺必利片的首仿制剂。氨磺必利为苯甲酰胺精神类抑制药,选择性作用于人体多巴胺D2和D3受体亚型,而对其D1、D4和D5受体亚型无任何亲和力,对5-羟色胺和肾上腺素能等其他神经受体亲和力较低。基于上述特征,该药物在发挥治疗作用的同时,即可避免如患者嗜睡、体重增加等副反应的发生。除此之外,因氨磺必利具有优先选择作用于边缘系统的特点而使其引起的锥体外系副反应有降低的趋势。     

苹果酸克立波必利

异名化学名 4-氨基-N-(1-苄基-4-哌啶基)-5-氯-2-甲氧基苯甲酰胺苹果酸氢盐药效分类抗溃疡药开发单位 (西班牙)Almirall 上市厂商 (日)万有,明治 1984年4月上市药理本品为苯甲酰胺类具抗多巴胺作用的化合物,其化学结构与舒必利类似。主要作用于胃、小肠,使其运动亢进,同时使胃     

伊托必利与莫沙必利治疗糖尿病性胃轻瘫的疗效比较

目的 比较促胃肠动力药伊托必利和莫沙必利治疗糖尿病性胃轻瘫的疗效,以确定伊托必利是否值得在临床上推广使用.方法 将100例确诊为糖尿病性胃轻瘫的患者随机分为两组,每组50例,分别给予伊托必利和莫沙必利治疗,4周后观察两种药物的临床疗效以及胃排空时间的变化.结果 伊托必利和莫沙必利两种药物对糖尿病性胃轻瘫症状缓解的总有效...     

胃肠运动促进剂 西沙必利(Cisapride)

异名 Prepulsid 化学名顺式-4-氨基-5-氯-N-〔1-(3-(4-氟苯氧基)丙基)-3-甲氧基-4-哌啶基〕-2-甲氧基苯甲酰胺药效分类消化器官运动赋活调整药开发单位 Jessen Pharm NV 上市厂商 (瑞典)Jessen Pharm Ltd1988年药理本品主要作用于胃肠道器官壁内肌神经丛神经节后末梢。促使壁肌释放出乙酰胆碱,刺激整个消化系统器官,从而增进食管、胃、肠运动机能,使运动亢进。据认为本品刺激消化道运动方式类似于消化道生理性的前进复合移行运动。用本品灌注豚鼠离体胃肠标本,显示胃收缩活动增强,并能抑制由新福林、多巴胺、5-羟色胺等引起的胃松弛作     

氯波必利引起痉挛性斜颈3例

例 1,男 ,3 4岁。因腹胀、反酸 1个月 ,门诊胃镜检查示返流性食管炎 ,给予氯波必利 (湖南省株洲制药厂 ,批号 :2 0 0 2 0 60 5 ,每片 0 .68mg) 1次 1片 ,tid ,当日口服 3片 ,晚上突发头向右侧扭转 ,不能转正而入院。体检 :体温 3 7℃ ,心率 80次·min 1 ,血压12 0 80mmHg(1mmHg =0 .13 3kPa) ,呼吸率 2 0次·min 1 ,神清 ,心肺 (-) ,腹无压痛 ,脑神经 (-) ,头向右侧扭转 ,不能转正 ,四肢肌力正常 ,未引出病理征。因既往无特殊病史 ,当日情绪未受刺激 ,仅口服氯波必利 ,故考虑为其所致痉挛性斜颈。以地西泮 10mg缓慢静脉注射 ,患者渐安静 …     

泰必乐的合成、药理和临床应用

<正> 泰必乐(tiapride)系含烷砜基邻茴香酰胺的衍生物,其WHO的非专利商品名为Tiapridal;化学名为N-(2-二乙胺基乙基)-2-甲氧基-5甲砜基苯甲酰胺。结构式如下: 胺类抗精神病药舒必利(sulpiride)、索托必利(sultopride)之后,于最近发现的新型神经精神安定药,自1974年上市以来,国外已经广泛应用。鉴于国内尚无泰必乐产品,作者于1980年开始研制。综合文献报道,泰必乐是以2-甲氧基-5-甲砜基苯甲酸为主要中间体,其合成路线有几种图1。     

西沙必利的临床应用

西沙必利 (ｃｉｓａｐｒｉｄｅ)为第三代全胃肠动力药 ,是氟哌啶醇衍生的新型苯酰基类药物。它通过 5 羟色胺不同受体的多种作用来促进胃肠道肌间神经丛释放乙酰胆碱于一个适度水平 ,从而发挥促胃肠动力功能。与第一代胃肠动力药甲氧氯普胺相比 ,作用强 10 0倍。随着对它的认识加深 ,其临床应用也逐渐拓宽。1　胃节律障碍60例以胃排空延缓为特征 ,体表胃电图 (ＥＧＧ)示胃节律紊乱的患者 ,分为给药组 3 0例 ,男 11例 ,女 19例 ,年龄 ( 4 4± 11)岁 ,病程 ( 4 .8± 1.5 )个月 ,给予西沙必利 10ｍｇ ,餐前 15ｍｉｎ口服 ,ｔｉｄ ,3周为 1个疗…     

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.     

Pharmacological treatment of COVID-19: an opinion paper

The precocity and efficacy of the vaccines developed so far against COVID-19 has been the most significant and saving advance against the pandemic. The development of vaccines has not prevented, during the whole period of the pandemic, the constant search for therapeutic medicines, both among existing drugs with different indications and in the development of new drugs. The Scientific Committee of the COVID-19 of the Illustrious College of Physicians of Madrid wanted to offer an early, simplified and critical approach to these new drugs, to new developments in immunotherapy and to what has been learned from the immune response modulators already known and which have proven effective against the virus, in order to help understand the current situation.     

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.     

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.