葡萄糖酸依诺沙星与盐酸林可霉素配伍稳定性的研究

目的：研究葡萄糖酸依诺沙星注射液与盐酸林可霉素注射液的配伍稳定性。方法：考察溶液配伍前后的颜色、pH值、不溶性微粒等变化情况，并用UV法和HPLC法分别考察配伍前后葡萄糖酸依诺沙星和盐酸林可霉素的含量变化。结果：葡萄糖酸依诺沙星注射液与盐酸林可霉素注射液配伍．6h内溶液颜色基本无变化、pH值、不溶性微粒及含量无明显变化。结论：两药配伍后的理化性质稳定．在6h内可以配伍使用。     

葡萄糖酸依诺沙星注射液与利巴韦林注射液配伍稳定性的研究

目的研究葡萄糖酸依诺沙星注射液与利巴韦林注射液的配伍稳定性。方法考察溶液配伍前后的颜色、pH值、不溶性微粒等变化情况,并用UV和HPLC分别考察配伍前后葡萄糖酸依诺沙星和利巴韦林的含量变化。结果葡萄糖酸依诺沙星注射液与利巴韦林注射液配伍,6 h内溶液颜色基本无变化、pH值、不溶性微粒及含量无明显变化。结论两药配伍后的理化性质稳定,在6h内可以配伍使用。     

注射用葡萄糖酸依诺沙星在木糖醇注射液中的稳定性观察

目的观察室温（25℃）下注射用葡萄糖酸依诺沙星在木糖醇注射液中的稳定性。方法用紫外分光光度法测定配伍液中注射用葡萄糖酸依诺沙星的含量,并观察外观、pH值的变化。结果注射用葡萄糖酸依诺沙星与木糖醇注射液配伍后6h内其外观、pH值及含量均无明显变化。结论室温（25℃）下注射用葡萄糖酸依诺沙星在木糖醇注射液中稳定性良好。     

注射用葡萄糖酸依诺沙星在木糖醇注射液中的稳定性观察

目的 观察室温(25℃)下注射用葡萄糖酸依诺沙星在木糖醇注射液中的稳定性.方法 用紫外分光光度法测定配伍液中注射用葡萄糖酸依诺沙星的含量,并观察外观、pH值的变化.结果 注射用葡萄糖酸依诺沙星与木糖醇注射液配伍后6h内其外观、pH值及含量均无明显变化.结论 室温(25℃)下注射用葡萄糖酸依诺沙星在木糖醇注射液中稳定性良好.     

盐酸氨溴索注射液在葡萄糖酸依诺沙星注射液中的配伍稳定性考察

目的考察盐酸氨溴索注射液与葡萄糖酸依诺沙星注射液配伍的稳定性。方法在室温[（20±1）℃],避光条件下,盐酸氨溴索与葡萄糖酸依诺沙星配伍后0～6 h内测定pH,观察外观及性状变化,采用高效液相色谱法-二极管阵列检测器测定盐酸氨溴索与葡萄糖酸依诺沙星的含量变化。结果 6 h内混合液外观、pH及含量均无明显变化。结论在室温[（20±1）℃]避光条件下,盐酸氨溴索注射液与葡萄糖酸依诺沙星注射液6 h内可以配伍使用。     

依诺沙星注射液与替硝唑注射液的配伍稳定性考察

目的考察葡萄糖酸依诺沙星注射液与替硝唑注射液配伍的稳定性。方法取依诺沙星注射液与替硝唑注射液配伍后的溶液,采用紫外分光光度法,测定其在25℃下6 h内不同时间的吸收度,计算依诺沙星、替硝唑配伍前后的含量。扫描紫外吸收图谱,观察溶液的外观,测定pH值。结果在25℃下,0～6 h内配伍液外观、pH值和紫外吸收图谱无明显变化,依诺沙星和替硝唑的含量无明显变化。结论依诺沙星注射液与替硝唑注射液在25℃下可配伍使用。     

注射用葡萄糖酸依诺沙星与头孢哌酮钠舒巴坦钠及头孢匹胺钠的配伍变化

目的考察注射用葡萄糖酸依诺沙星分别与两种头孢菌素类抗生素混合发生的配伍变化.方法分别观察配伍液外观变化,采用酸度计测定pH值变化,应用紫外分光光度法测定葡萄糖酸依诺沙星含量变化.结果葡萄糖酸依诺沙星分别与两种头孢菌素类抗生素配伍时均出现浑浊,葡萄糖酸依诺沙星含量下降,下降的程度与其配伍浓度有关.结论葡萄糖酸依诺沙星与头孢匹胺钠及头孢哌酮钠舒巴坦钠存在配伍禁忌.     

依诺沙星注射液与奥硝唑氯化钠注射液配伍稳定性考察

目的考察葡萄糖酸依诺沙星注射液与奥硝唑氯化钠注射液配伍稳定性。方法采用紫外分光光度法,在依诺沙星注射液与奥硝唑氯化钠注射液配伍后,测定溶液在25℃下6h内不同时间的吸收度,计算依诺沙星与奥硝唑配伍前、后的含量。扫描紫外吸收图谱,观察溶液的外观并测定其pH值。结果在25℃下,0～6h内配伍液外观、pH值和紫外吸收图谱无明显变化,依诺沙星和奥硝唑的含量无明显变化。结论依诺沙星注射液与奥硝唑氯化钠注射液在25℃下可配伍使用。     

葡萄糖酸依诺沙星注射剂质量分析

目的评价葡萄糖酸依诺沙星注射剂的质量现状和问题。方法采用法定检验方法并结合探索性研究,对葡萄糖酸依诺沙星注射剂的质量现状进行评价。结果现行标准中的有关物质项目存在明显缺陷;部分药包材对葡萄糖酸依诺沙星质量产生不良影响;由于葡萄糖酸依诺沙星在水溶液中光照降解明显,大输液的杂质含量明显高于其他剂型。结论葡萄糖酸依诺沙星注射剂现行标准存在不足,需要改进;药包材和葡萄糖酸依诺沙星注射液（大输液）的质量需加以关注。     

依诺沙星注射液与酚磺乙胺注射液的配伍稳定性观察

目的观察葡萄糖酸依诺沙星注射液与酚磺乙胺注射液在5％葡萄糖注射液中配伍的稳定性。方法在25℃下,模拟临床常用浓度,将葡萄糖酸依诺沙星注射液与酚磺乙胺注射液在5％葡萄糖注射液中配伍,观察6h内配伍液的外观,测定pH值,扫描紫外吸收图谱,用紫外分光光度法测定依诺沙星和酚磺乙胺的吸收度,计算依诺沙星和酚磺乙胺含量。结果6h内配伍液的外观、pH值和紫外吸收图谱均无明显变化,依诺沙星和酚磺乙胺含量无明显变化。结论在25℃下,葡萄糖酸依诺沙星注射液与酚磺乙胺注射液在5％葡萄糖注射液中配伍稳定,可配伍使用。     

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.

     

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.