加替沙星氯化钠注射液与注射用头孢美唑的配伍稳定性

目的考察加替沙星氯化钠注射液与注射用头孢美唑配伍的稳定性。方法在25℃与37℃下,观察8h内加替沙星氯化钠注射液(2g·L-1)与注射用头孢美唑(10g·L-1)配伍液的外观、pH值及紫外光谱的变化。用单波长法、一阶导数法分别测定加替沙星氯化钠注射液与注射用头孢美唑的含量。结果在8h内,配伍液外观基本不变,在6h后含量略有下降,而pH值有所变化。结论2种药物配伍8h内基本稳定,用单波长法、一阶导数光谱法分别测定其含量,方法简便,准确,实用。     

RP-HPLC考察注射用盐酸头孢吡肟与氟康唑氯化钠注射液配伍的稳定性

目的考察室温(20±1)℃下,注射用盐酸头孢吡肟与氟康唑氯化钠注射液配伍的稳定性。方法采用反相高效液相色谱法测定配伍液中头孢吡肟与氟康唑0～6 h内的含量变化,并观察配伍液的外观及pH值。结果注射用盐酸头孢吡肟与氟康唑氯化钠注射液6 h内配伍液外观、pH值及含量均无明显变化。结论在室温(20±1)℃下,注射用盐酸头孢吡肟与氟康唑氯化钠注射液配伍后6 h内可使用。     

应用联立方程组新解法考察加替沙星氯化钠注射液与注射用头孢硫脒配伍的稳定性

目的 考察注射用加替沙星氯化钠注射液与注射用头孢硫脒配伍的稳定性.方法 分别在37℃、25℃条件下,观察8h内加替沙星氯化钠注射液(0.2g·L-1)、注射用头孢硫脒(1g·L-1)配伍液的外观,pH值及紫外光谱的变化. 用联立方程组新解法(新Vierordt法)计算注射用加替沙星氯化钠注射液与注射用头孢硫脒的含量.结果 选择291nm和263nm作为加替沙星和头孢硫脒的测定波长.α=0.288668,β=0.098569.在37℃的条件下,4h内pH值,溶液颜色,含量基本不变,在25℃情况下,两药配伍8h内pH值,溶液颜色,含量基本不变.结论 两种药物配伍在37℃条件下4h内基本稳定,在25℃条件下8h内基本稳定,用联立方程组新解法测定其稳定性,方法 简便,准确,实用性强.     

注射用加替沙星与注射用头孢地嗪钠配伍稳定性考察

目的考察注射用加替沙星与注射用头孢地嗪钠分别在0.9%氯化钠注射液和5%葡萄糖注射液中配伍的稳定性。方法在室温(20±1)℃,观察两药配伍后的外观、pH、含量变化,高效液相色谱法测定配伍液中加替沙星和头孢地嗪钠含量。结果两药配伍后6 h内的外观、pH、含量均无明显变化。结论在室温条件下,注射用加替沙星与注射用头孢地嗪钠在0.9%氯化钠注射液和5%葡萄糖注射液中配伍稳定。     

加替沙星氯化钠注射液与注射用头孢美唑的配伍稳定性

目的考察加替沙星氯化钠注射液与注射用头抱美唑配伍的稳定性。方法在25℃与37℃下,观察8h内加替沙星氯化钠注射液（2g·L^-1）与注射用头抱美唑（10g·L^-1）配伍液的外观,pH值及紫外光谱的变化。用单波长法、一阶导数法分别测定加替沙星氯化钠注射液与注射用头抱美唑的含量。结果在8h内,两药在配伍液外观基本不变,在6h后含量略有下降,而pH值有所变化。结论两种药物配伍8h内基本稳定。用单波长法、一阶导数光谱法分别测定其稳定性,方法简便,准确,实用性广。     

注射用加替沙星与注射用更昔洛韦配伍的稳定性考察

目的:考察注射用加替沙星与注射用更昔洛韦分别在0.9%氯化钠注射液和5%葡萄糖注射液中配伍的稳定性.方法:在室温[(20±1)℃],观察8 h内加替沙星(2 g·L-1)与更昔洛韦(1.0 g·L-1)配伍液的外观、pH及紫外光谱的变化,用紫外双波长分光光度法测定2种药物的含量.结果:2种药物配伍后,8 h内的含量、pH及外观无明显变化.结论:注射用加替沙星与注射用更昔洛韦可以在0.9%氯化钠注射液和5%葡萄糖注射液中配伍使用.     

不同输液中头孢吡肟的稳定性考察

目的:考察注射用盐酸头孢吡肟与4种常用输液配伍的稳定性。方法:将注射用盐酸头孢吡肟按临床用药质量浓度与5%(50mg/mL)葡萄糖注射液、10%(100mg/mL)葡萄糖注射液、葡萄糖氯化钠注射液与0.9%(9.0mg/mL)氯化钠注射液配伍,并将配伍液分别置室温25℃下光照及避光放置,于不同时间(0,1,2,3,4,6h)时采用紫外分光光度法测定头孢吡肟的质量与pH值以及观察配伍液中外观变化。结果:在25℃下光照及避光放置,0~6h时配伍液外观、pH值及头孢吡肟质量均无明显变化。结论:注射用盐酸头孢吡肟与4种常用输液配伍后在25℃下光照及避光放置,6h内是稳定的。     

注射用头孢吡肟与多种注射液的配伍稳定性

目的：分别观察头孢吡肟与甲硝唑、维生素B6、氨茶碱、酚磺乙胺、地塞米松、利巴韦林注射液的配伍稳定性。方法：采用紫外分光光度法测定6h内配伍液中头孢吡肟的含量，同时观察外观并测定pH值。结果：头孢吡肟与氨茶碱、甲硝唑和维生素B6在0．9％氯化钠注射液中配伍。外观与头孢吡肟的含量均发生明显改变。而头孢吡肟与酚磺乙胺、地塞米松和利巴韦林在0．9％氯化钠注射液中配伍，6h内配伍液的外观、pH值及头孢吡肟的含量均无明显变化。结论：头孢吡肟与氨茶碱、甲硝唑和维生素B6不可配伍使用。与酚磺乙胺、地塞米松和利巴韦林可配伍使用。     

注射用加替沙星与头孢美唑配伍的稳定性考察

目的:考察注射用加替沙星与注射用头孢美唑分别在0.9%氯化钠注射液和5%葡萄糖注射液中配伍的稳定性。方法:在室温(20±1)℃条件下,分别观察及测定8h内配伍液的外观、pH值及紫外吸收光谱的变化,并用紫外双波长分光光度法测定加替沙星与头孢美唑钠的含量。结果:2药配伍后,8h内的外观、pH值、含量及峰形均无明显变化。结论:注射用加替沙星与注射用头孢美唑可在0.9%氯化钠注射液或5%葡萄糖注射液中配伍应用。     

头孢替唑钠、盐酸头孢甲肟在5%转化糖注射液中的配伍稳定性考察

目的考察注射用头孢替唑钠、注射用盐酸头孢甲肟分别与5%转化糖注射液配伍的稳定性,为临床合理用药提供依据。方法在室温(25±1)℃下,将两种注射用抗生素分别与5%转化糖注射液配伍,在8 h内,观察各配伍溶液的pH和外观变化,并采用HPLC法测定各配伍溶液中主药成分的相对含量。结果 8 h内,盐酸头孢甲肟、头孢替唑钠与5%转化糖注射液配伍后,头孢替唑钠的pH、外观和相对含量无明显变化;而盐酸头孢甲肟的pH及含量变化较大,配伍溶液颜色逐渐加深。结论在室温(25±1)℃条件下、8 h内,注射用头孢替唑钠与5%转化糖注射液的配伍液稳定;从医疗安全的角度考虑不提倡盐酸头孢甲肟与5%转化糖注射液配伍使用。     

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.

     

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.     

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.     

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.     

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.