HPLC法测定腹膜透析液中头孢呋辛钠的含量及其配伍稳定性考察

目的:建立腹膜透析液中头孢呋辛钠的含量测定方法并考察二者配伍稳定性。方法:采用高效液相色谱法测定头孢呋辛钠含量,色谱柱为Phenomenex Luna C18,流动相为乙腈-0.05mol·L-1醋酸钠缓冲液(pH3.9)=10∶90,流速为1.0mL·min-1,检测波长为273nm;考察头孢呋辛钠水溶液、头孢呋辛钠腹膜透析液放置6h后的不溶性微粒、澄清度、外观性状、pH值及含量。结果:头孢呋辛钠检测浓度线性范围为1.25～125μg·mL-1(r=0.9998),平均回收率为99.6%,RSD为0.6%(n=6);2种溶液6h内各检查指标均无明显变化。结论:所建立的含量测定方法简单、准确、灵敏,可用于腹膜透析液中头孢呋辛钠的含量测定;头孢呋辛钠与腹膜透析液配伍6h内稳定性良好。     

240例患者注射用头孢呋辛钠致不良反应发生的原因分析及其对策

目的:分析头孢呋辛钠临床合理用药现状及不良反应发生的原因,为临床合理用药提供参考。方法:抽取2018年1月-12月使用头孢呋辛钠治疗的4 600例患者资料,分析其患者使用头孢呋辛钠期间出现的不良反应以及不良反应发生特点及其对策,评估头孢呋辛钠临床用药的合理性。结果:4 600例患者中,发生头孢呋辛钠致不良反应240例,其发生率为5.22%;其中20岁以下年龄段与60岁以上年龄段患者头孢呋辛钠致不良反应发生率分别占27.50%和25.83%;不良反应可累及多个组织器官,其中涉及较多的为皮肤及附件(占56.67%)、胃肠道(占16.25%)和中枢神经系统(占10.00%);经对症治疗后其治愈率为77.08%(185/240),240例患者中有186例存在不合理用药问题。结论:头孢呋辛钠临床使用期间存在诸多不合理用药问题,应采取干预措施以提高临床用药的合理性,确保患者用药的安全性。     

头孢呋辛钠序贯治疗急性下呼吸道感染2种方案的成本-效果分析

目的:对头孢呋辛钠2种不同给药方案治疗急性下呼吸道细菌性感染的药物经济学评价.方法:将90例急性下呼吸道细菌性感染患者随机分为A、B组.每组各45例.A组采用注射用头孢呋辛钠连续静脉滴注;B组采用注射用头孢呋辛钠及头孢呋辛钠片序贯治疗,两组总疗程均为7 d,并进行成本-效果分析.结果:A、B组有效率分别为84.44%、82.22%(P>0.05),细菌清除率分别为95.6%、91.7%(P>0.05),不良反应发生率分别为4.44%、2.22%(P>0.05);A组的治疗费用明显高于B组,A、B组治疗成本分别为823.2、626.1元,成本-效果比分别为1001.22、782.63.结论:头孢呋辛钠序贯疗法治疗下呼吸道细菌性感染较经济.     

三拗片联合头孢呋辛钠治疗肺气肿的疗效观察

目的:观察三拗片联合头孢呋辛钠治疗肺气肿的疗效。方法:选取我院肺气肿患者150例,根据随机数字表法均分为三拗片组、头孢呋辛钠组和联合组。三拗片组患者给予口服三拗片,2粒/次,3次/d;头孢呋辛钠组患者给予静脉滴注含头孢呋辛钠2 g的生理盐水100 ml,2次/d;联合组同时给予三拗片口服和头孢呋辛钠静脉滴注,用法与用量与其他两组一致。3组患者均以1周为1个疗程,治疗2个疗程后,对3组患者的治疗效果及肺功能改善情况进行比较。结果:联合组的总有效率为92.0%,显著高于三拗片组(82.0%)和头孢呋辛钠组(80.0%),差异具有统计学意义(P<0.05);联合组动脉血氧分压(PaO2)、二氮化碳分压(PaCO2)、第1秒用力呼气容积(FEV1.0)和第1秒用力呼气容积占预计值百分比(FEV1%)均优于三拗片组和头孢呋辛钠组,差异具有统计学意义(P<0.05)。结论:三拗片联合头孢呋辛钠治疗肺气肿,疗效较好,患者呼吸功能得到了很大程度的改善。     

痰热清联合头孢呋辛钠治疗65例老年人肺气肿的疗效分析

目的观察痰热清联合头孢呋辛钠治疗老年人肺气肿的疗效分析。方法选取我院自2008年1月至2010年12月收治的老年人肺气肿患者130例随机分为观察组(痰热清联合头孢呋辛钠组)和对照组(头孢呋辛钠组)各65例,治疗周期均为2周,观察两组的治疗效果。结果观察组完全缓解率47例(89.75%),部分缓解16例(28.21%);对照组完全缓解30例(50.52%),部分缓解11例(21.32%)。两组完全缓解率比较有统计学差异(P<0.05)。观察组的缓解时间(5.9±0.8)d,对照组为(9.1±0.3)d,组间比较有统计学差异(P<0.05)。结论痰热清联合头孢呋辛钠治疗老年人肺气肿的效果显著,值得临床推广使用。     

对比分析注射用头孢呋辛钠与注射用头孢唑林钠治疗急性细菌性呼吸道感染的疗效差异

目的:比较头孢呋辛钠与头孢唑林钠治疗急性细菌性呼吸道感染的疗效.方法:选取2016年5月～2017年5月收治的104例急性细菌性呼吸道感染患者,随机分为头孢呋辛钠组(52例)和头孢唑林钠组(52例),比较疗效和不良反应发生率.结果:在治疗总有效率方面,头孢呋辛钠组明显高于头孢唑林钠组(P<0.05);头孢呋辛钠组不良反应发生率为3.7％,头孢唑林钠组不良反应发生率为11.1％,差异有统计学意义(P<0.05).结论:与头孢唑林钠相比,头孢呋辛钠在治疗急性细菌性呼吸道感染方面临床疗效优势更明显,不良反应发生较少,值得推广.     

头孢呋辛钠联合无创正压通气治疗COPD合并呼吸衰竭患者的疗效观察

目的 ：探讨头孢呋辛钠联合无创正压通气(NIPPV)治疗慢性阻塞性肺疾病(COPD)合并呼吸衰竭患者的疗效。方法 ：将100例COPD合并呼吸衰竭患者随机分为对照组(n=50)和观察组(n=50),对照组单用NIPPV治疗,观察组联合头孢呋辛钠。对比2组动脉血气指标、肺功能指标、临床治疗有效率和不良反应发生情况。结果 ：治疗后,与对照组相比,观察组A-aDO₂、pH、PaO₂较高,OI、PaCO₂较低;FEV₁/FVC和FEV₁%pred较高。观察组总有效率高于对照组(96.0%vs 72.0%),不良反应发生率低于对照组(2.0%vs 18.0%),差异均有统计学意义。结论 ：头孢呋辛钠联合NIPPV治疗COPD合并呼吸衰竭,可有效改进患者临床症状,提升治疗效果,减少不良反应发生。     

观察头孢呋辛钠与痰热清联合治疗老年肺气肿的临床疗效

目的:观察并分析头孢呋辛钠与痰热清联合治疗老年肺气肿的临床疗效.方法:以我院收治的92例老年肺气肿的患者作为研究对象,采用随机的方法分为对照组、实验组(各46例),对照组采用头孢呋辛钠进行治疗,实验组在对照组的用药基础上加入痰热清进行治疗,将两组治疗效果进行对比.结果:采用头孢呋辛钠治疗的对照组总有效率为78.26%、联合头孢呋辛钠与痰热清进行治疗的实验组总有效率为93.48%,实验组的总有效率明显高于对照组;且与对照组相比,实验组的病情缓解时间、肺部X线恢复正常时间和体温恢复时间更为理想,差异具有统计学意义(P<0.05).结论:采用头孢呋辛钠与痰热清联合治疗老年肺气肿,疗效显著,值得推广.     

阿奇霉素治疗下呼吸道感染的药物经济学研究

目的:评价注射用阿奇霉素和头孢呋辛钠治疗下呼吸道感染的经济性,选择疗效佳费用低的药物治疗方案。方法:观察两种治疗方案治疗下呼吸道感染的疗效和成本,运用药物经济学的成本-效果分析方法进行评价。结果:阿奇霉素和头孢呋辛钠的效果(以总有效率表示)分别为91.7%,90.0%(P>0.05);两种治疗方案的成本-效果比(C/E)分别为859.33元、5029.48元,增量分析△C/△E为-219913.06元;在敏感度分析中,当头孢呋辛钠的价格降低到0元时,头孢呋辛钠的C/E为1126.75元。结论:国产阿奇霉素为最佳治疗方案,进口头孢呋辛钠的治疗方案在本研究中没有药物经济学价值。提示在医疗保险偿付治疗下呼吸道感染的药品范围中,完全可用国产阿奇霉素替代进口头孢呋辛钠。     

头孢呋辛钠治疗细菌性感染的疗效对照

目的评价国产注射用头孢呋辛钠治疗急性细菌性疾病的临床疗效和安全性,并与进口头孢呋辛钠进行比较.方法急性细菌感染性疾病患者40例,进行前瞻性多中心随机单盲平行对照试验,分别给予国产与进口头孢呋辛钠治疗.结果国产与进口头孢呋辛钠治疗急性细菌性感染疾病各20例,痊愈率分别为50.0%和55.0%,有效率80.0%和85.0%,细菌清除率85.7%和100.0%,细菌阴转率85.7%和100.0%,以上指标经统计学处理差异均无显著性(P＞0.05).结论国产注射用头孢呋辛钠是治疗急性细菌感染性疾病的一种安全、有效的抗生素,与进口头孢呋辛钠在临床疗效和细菌清除率方面具有等效性.     

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.

---

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.     

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.     

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.