硫酸奈替米星滴鼻液的稳定性考察

目的：考察硫酸奈替米星滴鼻液的稳定性。方法：采用旋光法测定滴鼻液中硫酸奈替米星的含量;分别在高温、高湿、光照条件下放置,于规定时间取样,考察样品外观、装量、pH、含量及微生物限度的变化。结果：本品含量与温度及湿度相关性较大。光照的影响不明显。结论：硫酸奈替米星滴鼻液宜于常温阴凉处贮藏。     

硫酸奈替米星葡萄糖注射液稳定性研究

目的考察硫酸奈替米星葡萄糖注射液的稳定性。方法利用光照和高温、加速试验、长期试验测定对硫酸奈替米星葡萄糖注射液稳定性的影响。结果硫酸奈替米星葡萄糖注射液对光稳定性好,对于热在40℃稳定性良好,60℃稳定性稍差,加速试验,溶液外观颜色加深,降解产物5-羟甲基糠醛在3个月时已经超过规定,硫酸奈替米星的含量有所下降。长期试验,在室温放置九个月,产品外观、pH值、颜色、澄明度等项目没有显著变化。结论硫酸奈替米星葡萄糖注射液对光稳定,对热稳定性稍差但符合标准,加速试验和长期试验结果均符合要求。贮存时应置于阴凉干燥处。     

硫酸奈替米星及注射液初步稳定性试验

硫酸奈替米星及注射液初步稳定性试验汪素岩（浙江省药品检验所杭州３１０００４）任姿（温州制药厂质检科）药品稳定性考察是评价药品质量的一个重要指标之一，是为新药确定有效期，贮存条件的主要依据。本文对自制硫酸奈替米星原料药及注射液在室温强光照射、高温度、高...     

硫酸奈替米星葡萄糖注射液的生产工艺研究

目的　探讨硫酸奈替米星葡萄糖注射液的制备工艺,确定生产工艺参数和最佳生产工艺路线,为氨基糖苷类抗生素药物生产提供依据。方法　采用正交试验的方法优化生产工艺,并用室温留样试验方法进行初步稳定性考察,选择最佳工艺参数。结果　确定该产品生产工艺为加入适量的稳定剂,10 5℃,30min灭菌。结论　用该方法制备的硫酸奈替米星葡萄糖注射液质量稳定,有效期为2年。该生产工艺设计合理,可作为产品生产工艺规程执行。     

薄层色谱法检测硫酸奈替米星山梨醇注射液有关物质

目的 比较了多种硫酸奈替米星的薄层色谱条件，确定了分离效果较好、Rf值适宜的展开系统和灵敏度较高的显色剂，从而确定了较理想的硫酸奈替米星及有关物质薄层色谱检测法。方法 采用青岛海洋化工厂的硅胶G铺板，三氯甲烷-甲醇-浓氢溶液(2：1：0．3)为展开剂，1％碘的四氯化碳溶液为显色剂，均匀喷至板上立即显色。结果 确定较理想的硫酸奈替米星及有关物质薄层色谱检测法。结论 该法灵敏度高，分离效果好，显色快速，具有一定的特色。     

浊度法测定硫酸奈替米星及其制剂

目的:建立浊度法测定硫酸奈替米星及其制剂的含量方法,并进行方法学验证.方法:二剂量法:将金黄色葡萄球菌(CMCC(B)26 003)制备的菌悬液,接种于抗生素检定Ⅲ号培养基中,取9 mL培养液和1 mL不同浓度的硫酸奈替米星溶液于比色管中,37℃培养4 h左右,530 mn在线测定.结果:浊度与奈替米星浓度的10g值在0.16～2.5 μ·mL-1的范围内呈良好的线性关系(r=0.997 3);测得注射用硫酸奈替米星的平均回收率为101.1%(RSD=1.47%);硫酸奈替米星注射液的平均回收率为101.2%(RSD=2.14%).结论:方法准确,灵敏、省时.     

浊度法测定注射用硫酸奈替米星的含量

目的:建立浊度法测定注射用硫酸奈替米星的含量并进行方法学验证。方法:以金黄色葡萄球菌制作菌悬液,接种于抗生素检定Ⅲ号培养基中,取9 mL 培养液和1 mL 不同浓度的硫酸奈替米星置比色管中,37℃培养4 h 左右,530 nm 在线测定。结果:培养物浊度与奈替米星浓度的 log 值在0.6～1.6 u·mL~(-1)之间呈线性关系(r>0.99);测得奈替米星的平均回收率为100.7%(RSD=3.4%)。结论:该方法准确、可靠、灵敏度高,耗时短。     

盐酸山莨菪碱注射液与硫酸奈替米星注射液的配伍稳定性考察

目的考察盐酸山莨菪碱注射液(下称654-2)与硫酸奈替米星注射液(下称奈替米星)在5%葡萄糖注射液(下称5%GS)中的配伍稳定性。方法观察配伍液外观、测定配伍液pH值、紫外吸收光谱、采用双波长紫外分光光度法测定奈替米星含量。结果30℃时,654-2与奈替米星配伍6h内,外观不变,pH值未见明显改变,紫外吸收图谱几无改变,奈替米星含量稳定。结论654-2可与奈替米星配伍。     

影响注射用硫酸奈替米星稳定性因素的考察

硫酸奈替米星 (ｎｅｔｉｌｍｉｃｉｎｓｕｌｆａｔｅ)属氨基糖苷类抗生素 ,具有较强的广谱抗菌性 ,特别是对一些耐氨基糖苷类药物菌株的作用 ,具有较长的抗生素后效应和相对较轻的不良反应 ,抗菌活性优于庆大霉素。目前 ,在我国该药物制剂发展很快 ,中国药典 2 0 0 0年版尚未收载注射用硫酸奈替米星 ,仅收载了硫酸奈替米星注射液。由于抗生素类药物具有不稳定性 ,本实验考察了影响注射用硫酸奈替米星稳定性的各种因素 ,为生产、贮藏该制剂提供了参考依据。1　仪器与材料ＺＹ - 30 0Ａ抑菌圈测量仪 (北京先驱电脑有限公司 ) ;ＡＥ2 4 0微量天…     

硫酸奈替米星葡萄糖注射液充氮效果观察

目的：考察充氮对硫酸奈替米星葡萄糖注射液稳定性影响。方法：采用对比试验充氮组和未充氮组考察灭茵后其性状、颜色、pH值及含量变化。结果：充氮组比未充氪组更稳定,灭菌后色泽、pH值厦含量变化很小。结论：硫酸奈替米星葡萄糖注射液充氮能有效的减缓药液氧化分解。     

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.     

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.     

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.