荧光分光光度法测定奋乃静片的含量

目的建立奋乃静片的荧光分光光度法含量测定方法。方法以盐酸-乙醇溶液（取乙醇500mL，加盐酸10mL，加水至1000mL，摇匀）为溶剂，荧光光度法测定波长为λex=280nm，λem=380nm。结果奋乃静质量浓度线性范围是2．55～30．63μg／mL（r=0．9999），平均加样回收率为99．97％，RSD=0．51％（n=9）。结论本法专属性强、灵敏度高、重现性好，结果准确，适用于奋乃静片的质量控制     

荧光分光光度法测定盐酸多沙普仑注射液的含量

目的 建立盐酸多沙普仑注射液含量测定的荧光分光光度法。方法以水为溶剂,测定波长λex为270nm,λem为320nm。结果盐酸多沙普仑质量浓度在20．05～240．7μg／mL范围内与荧光强度呈线性关系（r=0．9999）,平均回收率为99．81％,RSD=0．60％（n=6）。结论荧光分光光度法专属性强、灵敏度高、重现性好,结果准确,适用于盐酸多沙普仑注射液的质量控制。     

荧光分光光度法测定何首乌及人参首乌胶囊中总葸醌的含量

目的：建立测定何首乌及人参首乌胶囊中总蒽醌含量的方法。方法：荧光分光光度法。以最佳pH条件的无水乙醇为溶剂，在λEX=440nm、λEM=515nm处测定总蒽醌含量。结果：在0．03～0．15p,g·mL^-1范围内，大黄素浓度和荧光强度有良好的线性关系，回归方程为F=194．36C＋2．9642，r=0．9996。平均回收率何首乌为98．1％，RSD为1．9％；人参首乌胶囊为98．6％，RSD为2．0％。测得总蒽醌含量何首乌中为0．522mg·g^-1，人参首乌胶囊中为0．443mg·g^-1。结论：本法简便快捷，准确灵敏，重复性好，可用于何首乌及人参首乌胶囊的质量控制。     

柱前衍生-高效液相色谱荧光法测定硫普罗宁片含量

目的：建立了柱前衍生-高效液相色谱荧光法测定硫普罗宁片含量。方法：供试品经N-（1-芘）马来酰亚胺（NPM）衍生化后，采用Kromasil C18柱（250mm×4.6mm，5μm），流动相为水（含0．02％磷酸和0．8％冰乙酸）-乙腈（52：48），pH=3．0；流速0，8mL·min^-1，在λex=330nm，λem=380nm处荧光检测。结果：硫普罗宁在5．0～50．0μg·mL^-1浓度范围内与其衍生化主产物峰面积呈良好的线性关系，r=0．9993，平均回收率为99．5％（RSD=1．0％）。结论：该法准确可靠，专属性强，能满足制剂质量控制的要求。     

紫外分光光度法测定西沙必利片的含量

目的;用紫外分光光度法测定西沙必利片中西沙必利的含量。为该药提供质量控制的方法。方法：紫外分光光度法。结果：西沙必利浓度在８．９～２６．８ｕｇ．ｍｌ＾－１范围内吸收度与浓度呈线性关系（ｒ＝０．９９９９,ｎ＝５）,回收率为１００．１％,ＲＳＤ＝０．７４％（ｎ＝６）。结论：紫外分光光度法作为西沙必利片含量测定方法,简便、准确、快速。     

紫外分光光度法快速测定那格列奈片的含量

目的采用紫外分光光度法快速测定那格列奈片的含量。方法用乙醇作空白，在259nm波长处照分光光度法测定吸收度。结果那格列奈质量浓度在0．1～1．2mg／mL范围内与吸收度线性关系良好，r=0．9997（n=5），平均回收率为99．47％，RSD=1．169％（n=9）。结论紫外分光光度法快捷、简便、灵敏，可作为该产品的快速测定方法。     

分光光度法测定咳特灵胶囊中总黄酮的含量

目的：建立咳特灵胶囊中总黄酮的含量检测方法。方法：采用分光光度法,检测波长为510nm。结果：芦丁在0．0387～0．1160mg·ml^-1范围内呈良好的线性关系（r=0．9997,n=5）;回收率为99．98％,RSD为2．05％（n=6）。结论：本法操作简便、快捷,结果准确。     

HPLC荧光检测法测定盐酸文拉法辛血药浓度及人体生物等效性研究

目的：建立测定健康受试者血浆样品中盐酸文拉法辛浓度的高效液相色谱法。方法：以Diamonsil C18（150mm×4．6mm，5μm）为色谱柱；流动相为乙腈-pH3．0磷酸盐缓冲液-三乙胺（33．5：66．5：1），流速1．0mL·min^-1，进样量为20μL，内标为马普替林。血浆样品经正己烷-异戊醇提取后荧光检测：λex=276nm，λem=596nm。结果：盐酸文拉法辛浓度在10～800ng·mL^-1范围内线性关系良好（r=0．9999），最低检出限为2ng·mL^-1，最低血药检测浓度为16．99ng·mL^-1（S／N〉3）。盐酸文拉法辛浓度30，150，600ng·mL^-1的萃取回收率（n=5）和方法回收率（n=5）分别在81．5％～91．1％和98．7％～112．6％范围内，日内和日间精密度的RSD（n=5）分别小于12％和10％。结论：本法可以用于测定血浆中盐酸文拉法辛浓度，方法准确、灵敏、快速，重现性好。     

分光光度法测定银锌凝胶中总磺胺嘧啶及磺胺嘧啶锌的含量

目的：建立银锌凝胶中总磺胺嘧啶及磺胺嘧啶锌的含量测定方法。方法：银锌凝胶以20％磷酸溶液提取后，采用紫外分光光度法，于307nm波长处测定总磺胺嘧啶含量。另将银锌凝胶以干法消解处理后与锌试剂反应，采用可见光分光光度法，于620nm波长处测定磺胺嘧啶锌含量。结果：磺胺嘧啶在0．00—67．55μg·mL^-1范围内，吸收度与浓度呈良好线性关系（r=0．9999）；平均回收率为102．0％（n=9，RSD=1．7％）；样品及对照品溶液于室温放置48h稳定。锌浓度在0．00～2．86μg·mL^-1范围内，吸收度与浓度呈良好线性关系（r=0．9999）；平均回收率为96．2％（n=9，RSD=1．3％）；结论：上述2种方法操作简单，灵敏度高，专属性强，结果准确，适用于测定银锌凝胶中主要成分的含量。     

高效液相色谱法同时测定脉络宁注射液中3种有机酸的含量

目的：建立用高效液相色谱法梯度洗脱同时测定脉络宁注射液中绿原酸、咖啡酸、肉桂酸含量的方法，并对3个批次脉络宁注射液中上述3种化合物进行定量分析。方法：采用Aglient Zorbax SB-C18柱（4．6mm×150mm）；流动相为乙腈-0．8％醋酸，梯度洗脱；流速为1mL·min^-1；检测波长为λ1=327nm（绿原酸、咖啡酸），λ2=278nm（肉桂酸）。结果：绿原酸、咖啡酸、肉桂酸的线性范围分别为2．695～26．95mg·L^-1（r=0．9997）、0．82～8．20mg·L^-1（r=0．9999）、0．94～9．4mg·L^-1（r=0．9999），回收率分别为101．21％，98．24％，99．56％。结论：本法灵敏快速，准确可靠，适合于同时测定脉络宁注射液中绿原酸、咖啡酸、肉桂酸含量的。     

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.     

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.     

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.