HPLC法测定链麻滴鼻液中硫酸链霉素和盐酸麻黄碱的含量

目的建立测定链麻滴鼻液中硫酸链霉素和盐酸麻黄碱含量的高效液相色谱法,消除焦亚硫酸钠对硫酸链霉素含量测定的影响。方法色谱柱为Diamonsil C18柱(250mm×4.6mm,5μm);流动相为0.014mol·L-1庚烷磺酸钠的0.05mol·L-1磷酸二氢钾溶液-乙腈(78∶22);检测波长硫酸链霉素195nm,盐酸麻黄碱207nm;流速1.0mL·min-1。结果硫酸链霉素质量浓度在44.40³10.80μg·mL-1范围内,与其峰面积呈良好的线性关系。(r=0.999 8,n=7),平均回收率为103.4%(RSD=3.4%);盐酸麻黄碱质量浓度在20.224310.80μg·mL-1范围内,与其峰面积呈良好的线性关系。(r=0.999 8,n=7),平均回收率为103.4%(RSD=3.4%);盐酸麻黄碱质量浓度在20.224⁸0.896μg·mL-1范围内,与其峰面积呈良好的线性关系(r=0.999 9,n=7),平均回收率为99.5%(RSD=1.0%)。结论该方法专属性强、测定结果准确、精密度高、线性好,加入甲醛能够消除辅料中焦亚硫酸钠对硫酸链霉素含量测定的影响。     

链霉素滴鼻液的制备及质量标准研究

目的:制备链霉素滴鼻液,并建立其质量标准.方法:采用反相高效液相色谱法测定链霉素滴鼻液中链霉素的含量,并考查其稳定性.结果:所制备链霉素滴鼻液为无色澄明液体;链霉素在415.55～1 246.66 μg/ml范围内,峰面积与浓度呈良好线性(r=0.999 7),平均回收率为100.03%(RSD＝0.97%,n＝3).结论:该方法准确、可靠,可用于该制剂的质量控制.     

微生物法测定硫酸链霉素血药浓度参数

本文报道微尘物法测定硫酸链霉素血药浓度参数的方法.硫酸链霉素药代动力学符合双室模型,正常人肌注国产硫酸链霉素1g 后,取耳垂血进行测定,消除半衰期为3.18h,达峰时间1.18h,药物清除率4.487ml/min/kg.     

HPLC-ELSD法分析硫酸链霉素的含量

目的 建立一种硫酸链霉素的含量分析方法.方法 应用高效液相色谱.蒸发光散射检测法分析硫酸链霉素的含量.色谱条件:Waters XTerra C18色谱柱,规格:250mm×4.6mm,5μm;流动相:0.1mol/L三氟乙酸水溶液-0.1%(v/v)甲酸水溶液(40:60);检测器条件:汽化温度为105℃,雾化温度为50℃,气体流速1.90SLM.结果 硫酸链霉素样品中主成分与相邻杂质分离良好,主成分峰型及进样峰面积重现性良好,在选定进样量范围内线性良好.结论 本方法操作简单,方法的准确性、重现性均能很好的满足质量控制的要求.     

HPLC法测定链麻滴鼻液中链霉素和盐酸麻黄碱的含量

建立同时测定链麻滴鼻液中链霉素和盐酸麻黄碱含量的HPLC方法。采用反相高效液相色谱法。色谱柱为DiamonsilTMC18柱,流动相为0.014mol·L-1庚烷磺酸钠的0.05mol·L-1的磷酸二氢钾溶液-乙腈(82∶18),流速为1.5mL·min-1,检测波长为205nm。链霉素在0.4156～1.2467mg·mL-1范围内,峰面积与浓度呈良好线性(r=0.9997),盐酸麻黄碱在0.2174～0.6522mg·mL-1范围内,峰面积与浓度呈良好线性(r=0.9998),测得链霉素平均回收率为100.0%,RSD为0.97%(n=9),盐酸麻黄碱平均回收率为99.3%,RSD为0.78%(n=9)。本方法准确可靠,可有效控制产品质量。     

紫外分光光度法测定复方链霉素软膏中2组分的含量

目的:建立以紫外分光光度法测定复方链霉素软膏中硫酸链霉素和氨苯磺胺含量的方法。方法:采用麦芽酚-硫酸铁铵比色法,以硫酸铁铵为显色剂,于521nm波长处测定硫酸链霉素的吸收度;以0.1mol/L氢氧化钠溶液为溶剂,于251nm波长处测定氨苯磺胺的吸收度。结果:硫酸链霉素、氨苯磺胺检测浓度分别在200～950(r=0.9994)、1.464～7.784(r=0.9998)μg/ml范围内与吸收度呈良好的线性关系;平均加样回收率分别为99.1%(RSD=1.90%)、99.7%(RSD=1.60%)。结论:本方法简便、准确,可用于复方硫酸链霉素软膏的质量控制。     

DHPLC法和测序法检测结核分枝杆菌临床分离株链霉素的耐药性

目的我国是WHO认定的结核病高发区域之一。链霉素在我国已经使用50年以上,现在在结核病治疗中仍广泛使用。本工作采用变性高效液相色谱(DHPLC)法和测序法来分析结核分枝杆菌链霉素耐药基因rpsL和rrs基因突变,从而检测是否对链霉素耐药。方法215株结核分枝杆菌临床分离株(经常规方法证实,115株为链霉素耐药,100株为敏感),测定链霉素最小抑菌浓度(MIC),同时采用DHPLC和测序法检测rpsL和rrs基因突变。结果85.2%(98/115)的链霉素耐药株携有rpsL或/和rrs基因突变,其中rpsL基因突变占大多数(76.5%,88/115)。对98株带有基因突变的菌株的分析表明,rpsL,rrs基因的突变类型与MIC之间未见密切关系。100株敏感株未检出基因突变。DHPLC法与测序法结果完全一致。结论本工作建立的DHPLC法可以认为是结核分枝杆菌链霉素耐药分析的一种有效的工具。     

陡脉冲磁场促进磁性微球中链霉素体内释放的研究

目的:研究超顺磁性硫酸链霉素PLA-PEG共聚物微球(superparamagnetic streptomycin sulfatePLA-PEG block polymer microspheress,pSPM)在陡脉冲振荡磁场作用下体内药物释放规律。方法:用复乳化(W/O/W)溶剂挥发法制备spSPM,新西兰大白兔15只,随机分为3组,实验组为spSPM加用陡脉冲振荡磁场,2个对照组分别为spSPM和硫酸链霉素原料药溶液;臀肌注射spSPM后,定时取动物外周静脉血,采用高效液相色谱法(HPLC)测定硫酸链霉素的血药浓度,比较spSPM加陡脉冲振荡磁场s、pSPM和硫酸链霉素原料药溶液在3组动物体内的释放情况。结果:加用陡脉冲振荡磁场后spSPM中链霉素的释药量提高。结论:陡脉冲振荡磁场能促进spSPM中链霉素的释放。     

痢疾杆菌耐药性变异实验研究

关于痢疾杆菌对链霉素耐药性变异的实验研究,国内外学者对其形成机理,分为选择和适应两种解释。本文报告自己的实验结果,并对细菌耐药性变异的生物学机制问题进行探讨。实验材料和方法 (一)材料一、菌种:2a型福氏痢疾杆菌1号和4号,均为新近自菌痢患者分离。1号菌对链霉素500r/毫升耐药,1000r/毫升敏感;4号菌对链霉素5r/毫升耐药,10r/毫升敏感。二、链霉素:注射用硫酸二氢链霉素,每瓶1000000r,批号640530—1,上海第四药厂出品。三、培养基:肉膏液(简称肉汤)和肉汤     

超顺磁性硫酸链霉素PLA-PEG微球的体外抗结核分枝杆菌药敏实验

目的:检验制备的超顺磁性硫酸链霉素PLA-PEG微球(spSPM)的体外抗结核分枝杆菌活性,为靶向治疗儿童骨关节结核提供实验基础。方法:用制备的spSPM溶出液制成药敏培养基,与硫酸链霉素标准品制备的药敏培养基进行对照,采用绝对浓度法接种,观察比较其抑菌效果。结果:4周后,15株菌在空白培养基上均生长旺盛(+++~++++),在TCH培养基均为阳性(+),在PNB培养基均为阴性(-)。spSPM组高浓度(100 mg/L)培养基7株阴性,低浓度(10 mg/L)仅1株阴性。硫酸链霉素标准品溶液组培养基高浓度(100 mg/L)7株阴性,低浓度(10 mg/L)2株阴性。spSPM组与溶液组在分枝杆菌生长情况上差异均无统计学意义(高、低浓度培养,χ2分别为0.1408、0.0997,P均>0.05)。spSPM组耐药菌株为11株(73.33%),溶液组耐药菌株为12株(80.00%),两组耐药率比较差异无统计学意义(P>0.05)。结论:本实验制备的spSPM溶出液与硫酸链霉素标准品抑菌效果无明显差异,因此可应用于进一步的研究中。     

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.