注射用司帕沙星的豚鼠过敏性试验

目的 观察豚鼠对1％注射用司帕沙星有无过敏性反应，为临床合理用药提供依据。方法 豚鼠首次腹腔注射1％司帕沙星后14d和21d静脉注射加倍量司帕沙星进行攻击，并加以评分。结果 注射用司帕沙星豚鼠过敏试验呈阴性。结论 注射用司帕沙星有无过敏性反应。     

甲磺酸帕珠沙星氯化钠注射液与质子泵抑制剂配伍稳定性研究

目的 分析甲磺酸帕珠沙星氯化钠注射液与质子泵抑制剂的配伍稳定性。方法 室温（25℃）条件下考察甲磺酸帕珠沙星氯化钠注射液分别与注射用奥美拉唑钠、注射用泮托拉唑钠和注射用兰索拉唑配伍后放置0,2,4,6,8 h的外观及pH值变化;采用HPLC和分光光度法测定含量和溶血率。结果 甲磺酸帕珠沙星氯化钠注射液与注射用奥美拉唑钠、注射用泮托拉唑钠和注射用兰索拉唑配伍后立即发生颜色变化并且随着配伍时间延长逐渐形成沉淀,配伍后溶液的pH值有明显变化,甲磺酸帕珠沙星氯化钠注射液的含量分别降为83%,76%和83%,溶血率明显增加。结论 甲磺酸帕珠沙星氯化钠注射液与注射用奥美拉唑钠、注射用泮托拉唑钠和注射用兰索拉唑存在配伍禁忌,因此甲磺酸帕珠沙星氯化钠注射液不能与质子泵抑制剂类药物同容器配制,如需联合使用时应在使用前后冲洗输液管路。     

复方司帕沙星滴眼液药效学试验与临床观察

目的：评价复方司帕沙星滴眼液的药效学与临床疗效。方法：以盐酸左氧氟沙星滴眼液为对照,进行家兔眼局部刺激性和药效学试验;观察对细菌性结膜炎、角膜炎患者的临床疗效。结果：复方司帕沙星滴眼液对兔眼无刺激性,对兔眼结膜、角膜细菌感染的治疗作用和对照药无差别,临床疗效与对照药相当。结论：复方司帕沙星滴眼液治疗急性、亚急性结膜炎和角膜炎是安全、有效的,值得进一步临床研究。     

注射用头孢西丁钠的不良反应考察

目的考察头孢西丁钠的溶血性、过敏性及其对静脉血管的刺激作用。方法以豚鼠及新西兰兔为实验动物，观察其对滴注部位有无红肿、充血、出血和坏死等刺激作用及溶血和过敏现象。结果滴注部位未出现明显的红肿、充血、坏死等刺激反应及过敏现象，对兔红细胞未产生溶血和凝集作用。结论注射用头孢西丁钠无血管刺激性、过敏性及溶血性。     

注射用氨苄西林钠舒巴坦钠临床前制剂安全性研究

目的：研究注射用氨苄西林钠舒巴坦钠对给药局部血管的刺激性及对全身产生的毒性（溶血与凝集）影响。方法：家兔耳静脉注射氨苄西林钠舒巴坦钠30mg／ml稀释液10ml／kg，每日1次，连续3日，肉眼观察及组织学检查评分判定；2％红细胞混悬液加入30mg／ml的注射用氨苄西林钠舒巴坦钠，观察是否出现溶血与凝集反应。结果：稀释液对家兔血管为轻度刺激性；注射用氨苄西林钠舒巴坦钠30mg／ml无溶血及凝集作用。结论：注射用氨苄西林钠舒巴坦钠30mg／ml对给药局部血管有轻度刺激性；对全身无毒性（溶血与凝集）反应。     

司帕沙星滴眼液的药效学实验研究

目的:探讨司帕沙星滴眼液的动物药效学.方法:观察该制剂对家兔眼局部用药的刺激性及其对兔细菌混合感染性眼部炎症的治疗作用.结果:该制剂对兔眼无刺激性,对动物眼金黄色葡萄球菌、大肠杆菌、淋球菌的混合感染有明显治疗作用,且与氧氟沙星滴眼液的疗效相当.结论:司帕沙星滴眼液对兔眼细菌混合性感染安全、有效.     

司帕沙星注射兔体药物动力学研究

目的　研究司帕沙星注射剂兔体药物动力学。 方法　10只日本大耳白兔静脉注射司帕沙星6 2mg/kg后 ,采用微生物法测定用药后不同时间血清药物浓度。 结果　 该药的兔体药 时曲线符合二房室模型 ,AUC为 (5 6 8± 1 16 ) /h·L-1,消除半衰期为 (3 6 5± 0 95 )h。 结论　本文结果为司帕沙星临床合理用药提供了理论依据。     

注射用夫西地酸钠与甲磺酸帕珠沙星注射液存在配伍禁忌

通过临床观察和实验研究,发现注射用夫西地酸钠续滴甲磺酸帕珠沙星注射液后输液皮管中即呈乳状。提示注射用夫西地酸钠与甲磺酸帕珠沙星注射液不宜配伍。     

甲磺酸帕珠沙星与利巴韦林在氯化钠注射液中的稳定性考察

目的：考察注射用甲磺酸帕珠沙星与利巴韦林注射液在氯化钠注射液中的配伍稳定性。方法：采用紫外分光光度法测定注射用甲磺酸帕珠沙星与利巴韦林注射液配伍后的含量,观察配伍液的外观变化及pH值。结果：室温条件下8h内配伍液的外观、pH值及甲磺酸帕珠沙星与利巴韦林含量均无明显变化。结论：注射用甲磺酸帕珠沙星与利巴韦林注射液可以在氯化钠注射液中配伍使用。     

注射用甲磺酸帕珠沙星细菌内毒素检查的方法考察

建立注射用甲磺酸帕珠沙星的细菌内毒素检查法.确定注射用甲磺酸帕珠沙星的细菌内毒素限值并进行干扰试验测定.注射用甲磺酸帕珠沙星对细菌内毒素检查有抑制作用,通过稀释的方法可排除干扰,其最大非干扰浓度为0.25mg·ml-1.     

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.     

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.     

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.     

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.