刺五加中游离型和结合型异皮定的高效液相色谱法研究

目的 :建立刺五加药材中异皮定含量测定方法。方法 :采用PhenomenexC1 8柱 ,乙腈 - 0 0 5mol·L- 1 磷酸二氢钾(2 2∶78)为流动相 ,流速 0 9mL·min- 1 ,检测波长 34 4nm。结果 :游离型和结合型异皮定加样回收率分别为 98 8%和10 2 5 % ,RSD分别为 2 3%和 2 9% (n =5 )。结论 :方法简便 ,结果准确可靠。     

高效液相色谱法测定中药升麻中阿魏酸和异阿魏酸的含量

目的 :测定中药升麻中阿魏酸和异阿魏酸的含量。方法 :反相高效液相色谱法。HypersilODS分析柱(2 5 0mm× 4 6mm ,5 μm) ,流动相 :甲醇 -水 -磷酸 (5 0∶15 0∶0 1) ,紫外检测波长 :32 0nm ,灵敏度 :1 0AUFS ,柱温 :2 4℃ ,流速 :1mL·min-1。结果 :阿魏酸在 0 0 42～ 2 10 μg (r =0 9993) ,异阿魏酸在 0 0 43～ 2 14μg (r =0 9994)范围内呈线性 ,阿魏酸和异阿魏酸平均回收率 (n =5 )分别为 98 76 % (RSD =1 6 % )和 98 32 % (RSD =1 8% )。结论 :本方法简便、精确、可靠。     

RP-HPLC法测定颠茄磺苄啶片中磺胺甲基异噁唑与甲氧苄啶含量

目的　采用反相高效液相色谱法测定颠茄磺苄啶片中磺胺甲基异唑与甲氧苄啶的含量。方法　RP HPLC法。SerialC18色谱柱 ;甲醇 0 0 5mol/L磷酸盐缓冲液 (2 5∶75 )为流动相 ;检测波长为 2 4 0nm ;外标法测定。结果　磺胺甲基异唑平均回收率为 98 8% ,RSD为 0 75 % ;甲氧苄啶平均回收率为 98 7% ,RSD为 1 0 1%。结论　该方法简便、准确、可靠 ,可用于颠茄磺苄啶片中磺胺甲基异唑及甲氧苄啶的含量测定。     

地尔硫和硝酸异山梨酯静脉注射治疗不稳定性心绞痛的比较

目的 :比较地尔硫与硝酸异山梨酯注射液治疗不稳定性心绞痛疗效及安全性。方法 :心绞痛病人 90例 ,分为地尔硫组 4 2例 ,以地尔硫注射液 5 0mg加入氯化钠注射液 2 5 0mL中 ,10～ 15mg·h- 1,drip ,qd× 7d。硝酸异山梨酯组 4 8例 ,以硝酸异山梨酯 2 0mg加入氯化钠注射液 2 5 0mL ,2 .5～ 4mg·h- 1,drip ,qd× 7d。结果 :地尔硫组总有效率为 81% ,心电图总有效率为 74 % ,硝酸异山梨酯组总有效率为 74 % ,心电图总有效率为65 % ,2组间差别无显著意义 (P >0 .0 5 )。但在自发性心绞痛中 ,地尔硫组较硝酸异山梨酯组胸痛次数明显减少 ,ST段变化也有改善。随访 2mo ,2组心血管事件无显著差异。结论 :地尔硫与硝酸异山梨酯注射液治疗不稳定性心绞痛疗效相近 ,对自发性心绞痛效果可能更明显     

HPLC法测定刺五加中游离异嗪皮啶和总异嗪皮啶的含量

目的建立刺五加含量测定方法。方法 :采用DiamonsilC18柱 ( 2 0 0mm× 4 8mmi d ,5 μm) ,流动相为乙腈 甲醇 水 冰醋酸 (V∶V∶V∶V =1 7∶3∶80∶1 ) ,流速 0 9mL·min-1,检测波长3 44nm。结果异嗪皮啶在 1 2 4～ 49 6mg·L-1内质量浓度与峰面积呈良好线性关系 ,游离型异嗪皮啶和总异嗪皮啶的平均回收率分别为 1 0 0 7% ,98 8% ,RSD分别为 2 5 %和 1 9%。结论本法可作为刺五加质量控制的手段之一。     

地尔硫与单硝酸异山梨酯注射液治疗急症高血压的比较

目的 :观察地尔硫及单硝酸异山梨酯针剂治疗急症高血压病人的疗效及安全性。方法 :采用随机、开放、对照方法。 60例急症高血压病人分为地尔硫与单硝酸异山梨酯组各 30例 ,分别静脉给予地尔硫及单硝酸异山梨酯注射液 ,均为 5～10 μg·min- 1,观察 0 ,10 ,2 0 ,30 ,60 ,12 0min各血压变化。结果 :地尔硫组和单硝酸异山梨酯组血压均显著下降 ,有效率分别为 73%和 80 % ,组间差异无显著意义 (P >0 .0 5 ) ,不良反应轻。结论 :地尔硫治疗急症高血压安全、有效 ,与硝酸异山梨酯相似     

复方磺胺甲噁唑片的胶束薄层色谱分析

以十二烷基硫酸钠 (SDS)水溶液为展开剂、聚酰胺薄膜为固定相 ,对复方磺胺甲唑片(复方新诺明 )中两组分进行定量分析 .磺胺甲基异唑 (SMZ)和甲氧苄氨嘧啶 (TMP)分别在4 0～ 12 0mmo/L和 3 5～ 10 5mmol/L范围内吸收峰面积和浓度呈良好的线性关系 .相关系数分别为 0 9995和 0 9998,回收率分别为 10 1 4%和 99 5 % ,RSD(% )分别为 0 5 8和 1 6 0 .     

心康平原料药的鉴别和含量测定

目的 :研究新的中药复方制剂心康平的质控指标。方法 :采用细胞膜色谱法对三七、丹参和当归进行有效成分的筛选 ,在此基础上对原料药中三七的 4种有效成分三七皂苷R1、人参皂苷Rg1、Re和Rb1进行薄层色谱鉴别 ,薄层展开条件为氯仿 -醋酸乙酯 -甲醇 -水 (15∶40∶2 2∶10 ) ;对丹参和当归中的丹参酮ⅡA 和藁本内酯用HPLC法同时进行了含量测定 ,色谱条件为KromasilODS柱 (15 0mm× 4 6mm ) ,甲醇 -水 (80∶2 0 )为流动相 ,流速 1mL·min-1,2 5 4nm下检测结果 :TLC鉴别方法专属性强。HPLC法测定丹参酮ⅡA 和藁本内酯的回收率分别为 98 9%和 10 0 9% ,RSD分别为 3 0 %和 2 5 %。结论 :本文方法可全面有效地控制心康平原料药及其制剂的质量     

HPLC法测定克癃胶囊中补骨脂素、异补骨脂素的含量

目的 　用 HPL C法测定克癃胶囊中补骨脂素、异补骨脂素的含量。方法 　色谱条件 :色谱柱 :C1 8柱 (2 5 0× 4.6mm,5μm) ,流动相 :甲醇 -水(60∶ 40 ) ,检测波长 2 45 nm。结果 　补骨脂素在 0 .0 964～ 0 .482 μg,异补骨脂素在 0 .0 868～ 0 .43 4μg范围内呈良好线性关系。平均回收率分别为10 0 .7%;98.9%,RSD分别为 1.3 9%;2 .11%。 结论　该方法准确可靠     

HPLC测定川芎药材中藁本内酯的含量

目的　采用HPLC法测定川芎药材中藁本内酯的含量。方法　用Luna 5 μSilica(2 )色谱柱 (15 0mm× 4 .6mm) ;流动相为正己烷 -乙酸乙酯 -氯仿 (92∶3∶5 ) ;流速 0 8ml·min-1;检测波长 32 0nm。结果　在 0 1～ 2 0 μg范围内 ,峰面积与进样量的线性回归方程为 :A =- 4 7 2 4 +2 72 2X(r =1.0 0 0 0 ) ;平均回收率为 10 0 7%。测得 3批川芎药材中藁本内酯的含量分别为1 5 5 %、1 33%和 1 70 %。结论　所建方法简便、准确、重复性好 ,可用于川芎药材中藁本内酯的含量测定。     

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.     

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.     

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.     

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.