反相高效液相色谱法测定人血清中曲昔派特浓度

目的：建立测定人血清中曲昔派特浓度的反相高效液相色谱法。方法：血浆样品用乙酸乙酯萃取后进样。选用美国Beckman 344型高效液相色 谱仪。Ultrasphere ODS(250mm*4.6mm,5um)色谱柱。流动相为甲醇－0．01mol.L^-1 pH2.5的磷酸二氢钠缓冲液（35：65）,流速1mL.min^-1,茶碱作内标,紫外检测波长254mm,内标法峰高定量。结果：本法高,中低浓度的萃取回收率为79．4％－81．1％,方法回收率为97．3％－105．0％,日内RSD＜5％,日间RSD＜10％。结论：本法快捷,灵敏,准确,适用于曲昔派特血药浓度测定及药代动力学研究。     

高效液相色谱法测定血清中富马酸奎的平浓度

目的：建立用高效液相色谱法（HPLC）测定血清中富马酸奎的平浓度的方法。方法：HPLC测定，流动相为甲醇－水－1mol.L^-1醋酸铵－5mol.L^-1氨水（400：100：5：1）的混合液体,pH9.7，流速1mL.min^-1，C18柱，紫外检测波长254nm，以外标法定量。结果：线性范围10－300ug.L^-1，最低检测限5ug.L^-1，平均提取回收率93．10％，日内与日间精密度平均分别为3．41％和4．16％,结论：用HPLC可以较好的对血清中富马酸奎的平进行定性和定量。     

反相高效液相色谱法测定盐酸乙哌立松片剂的含量

目的：建立高效液相色谱法测定盐酸乙哌立公片含量的方法。方法：酸盐乙哌立松片加甲醇,超声振荡,过滤后以ODS C18为分析柱,以甲醇－水－三乙胺（80：19．5：0．5,V／V）为流动相,托哌酮为内标,于254nm波长检测。结果：盐酸乙哌立松在0．4－1．6mg/ml浓度范围内线性关系良好（r=0.9999),平均回收率98．4％,RSD,1．2％,三批协酸乙哌立松片含量测定结果分别为标示量的97．8％,98．3％和98．9％,结论：方法快速,准确,专一性强,适用于盐酸乙哌立松片的含量测定。     

薄层扫描法测定复方维A酸胶囊中维A酸的含量

目的：建立复方维A酸胶囊中维A酸的含量测定方法。方法：在硅胶GF254板上,以氯仿－甲醇－甲酸（9：1．2：0．3）为展开剂,采用双波长反射法锯齿扫描测定,测定波长290nm,参比波长370nm。结果：通过方法学考察,点样量在1．02－5．10μg(r=0.9982)范围线性关系良好,平均回收率为96．9％。结论：提取方法简便,胶囊中其它中药成分无干扰,测定方法准确,可用于本制剂的含量测定及质量控制。     

高效液相色谱法测定阿昔洛韦软膏的含量

目的：建立高效液相色谱法测定阿昔洛韦软膏含量的方法。方法：反相高效液相色谱法,ODS柱,流动相为乙腈－水（15：85）,检测波长254nm。结果：阿昔洛韦0．025－0．250mg.mL^-1内线性关系良好,r=0.9997,平均回收率99．7％,RSD 1．02％,结论．：此法简便,专属性强,结果准确。     

紫外法测定磺胺嘧啶钠注射液的含量

目的：建立磺胺嘧啶钠注射液的含量测定的紫外分光光度法。方法：以0.1mol/L NaOH溶液为溶剂，254nm为测定波长。结果：测定浓度的线性范围为2－10μg/ml(r=0.9999)，平均回收率为99．8％－100．1％，RSD小于1．01％。结论：本法简单、快速、准确，可用于磺胺嘧啶钠注射液含量的测定。     

RP-HPLC测定立复欣注射液的含量

目的：建立一种快速简便的反相HPLC法测定立复欣注射液的含量,同时考察25度立复欣注射液在5％GS,0．9％NS和10％GNS中的稳定性,方法：采用Lichrospher 100(RP-8.5um*250mm)柱,以甲醇－乙腈－0．04M KH2PO4溶液（31．5：31．5：37）为流动相,流速1ml/min,柱温40度,254nm柴外检测;观察溶液的外观并用酸度计测定其PH值,结果：回收率为100．5：37）为流动相,流速1ml/min,柱温40度,254nm紫外检测,观察溶液的外观并用酸度计测定其PH值,结果：回收率为100．87％,RSD＝1．4％（n=5),在4－120mg/l范围内,峰面积对浓度呈良好的线性关系,r=0\99989,25度下样品在输液中的PH值,含量及颜色在0－6h内均无明显变化。结论：本法简速,灵敏底高,准确性好;25度,6h内样 在上述输液中稳定性好。     

反相离子对高效液相色谱法测定马来酸曲美布汀原料中各杂质及其制剂中各组分的含量

目的：分离和测定马来酸曲美布汀原料中各杂质及其制剂中各组分的含量。方法：反相离子对高效液相色谱法,以联苯双酯为内标,uBondapak C18柱,甲醇－0．01mol.L^-1磷酸二氢钾（含5mmol.L^-1 庚烷磺酸钠）－三乙胺（50：50：0．1,用磷酸调PH为3．1）为流动相,流速1mL.min^-1,二极管阵列检测器检测,检测波长为254nm。结果：马来酸曲美布汀40－800ug.mL^-1,苯甲醇30－500ug.mL^-1范围内,峰面积与其浓度呈良好的线性关系,片剂中马来酸曲美布汀的平均回收率为100．3％,RSD＝0．51％;注射液中马来酸曲美布汀的平均回收率为99．7％,RSD＝0．34％,苯甲醇为100．1％,RSD＝0．52％;n=6,结论：方法简便,快速,准确,可同时分离和测定马来酸曲美布汀原料中各杂质及其制剂中各组合的含量。     

HPLC测定复方氯已定漱口服液中氯已定和甲硝唑的含量

目的：建立一种用高效液相色谱法测定复方氯已定口服液中甲硝唑和醋酸氯已定含量的方法。方法：用C18ODS色谱柱，水－已腈－冰醋酸（70：30：1）为流动要，UV检测波长为254nm。结果：该方法回收率为甲硝唑99.02,RSD1.6%(n=5)。醋酸氯已定98．68％，RSD1．8％（n=5)，结论：本方法简便，快捷，灵敏，可作为该制剂质量控制的有效方法。     

RP—HPLC同时测定利福肼胺胶囊中三组分的含量

用RP－HPLC法测定利福肼胺胶囊中利福平、异烟肼和吡嗪酰胺含量。采用Delta pak C18色谱柱,流动相分别为甲醇－pH4．5磷酸盐缓冲液（75：25）和甲醇-pH 3．5磷酸盐缓冲液（6：94）,检测波长254nm。方法回收率为99．5％－100．2％,RSD均小于1．60％。     

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.