反相高效液相色谱法测定盐酸异丙肾上腺素注射液的含量

目的：建立HPLC法测定盐酸异丙肾上腺素注射液的含量。方法：采用Diamonsil^TM C18色谱柱（250mm×4．6mm，5μm），流动相为0．005mol·L。庚烷磺酸钠（pH3．0）-甲醇（65：35），流速1．0ml·min^-1，检测波长280nm，柱温35℃。结果：盐酸异丙肾上腺素在0．02～2mg·ml^-1范围内线性关系良好（r=0．9999，n=7），平均回收率为99．7％（n=9）。结论：本方法简便、快速、准确，专属性好，可用于盐酸异丙肾上腺素注射液的含量测定。     

HPLC法测定乙胺吡嗪利福异烟片中4组分含量

目的：建立高效液相色谱法，测定乙胺吡嗪利福异烟片中利福平、异烟肼、吡嗪酰胺和盐酸乙胺丁醇含量。方法：利福平、异烟肼和吡嗪酰胺用C18色谱柱（150mm×4．6mm，5μm），以-0．01M磷酸二氢钾溶液-乙腈为流动相进行梯度洗脱，流速1．0ml·min^-1，检测波长254nm。盐酸乙胺丁醇选用C18色谱柱（150mm×4．6mm，5μm），四氢呋喃-0．4％庚烷磺酸钠（含有0．016％硫酸铜，用磷酸调pH至4．5）（25：75）为流动相，流速1．0ml·min^-1，检测波长258nm。结果：利福平、异烟肼、吡嗪酰胺及盐酸乙胺丁醇线性范围分别为16～160μg·ml^-1（r=0．9999），16—160μg·ml^-1（r=0．9999），53—532μg·ml^-1（r=0．9998），80～320μg·ml^-1（r=0．9998），平均回收率为99．3％～99．5％。结论：方法简便，准确，可用于乙胺吡嗪利福异烟片中各组分的质量控制。     

HPLC法测定氨酚咖匹林片中三组分的含量

目的：建立一种HPLC方法，同时测定氨酚咖匹林片中对乙酰氨基酚、咖啡因、阿司匹林的含量。方法：以Phenomenex C18（4．6×250mm 5um）为色谱枉，以甲醇-水-三乙胺（60：40：0．5）用冰醋酸调节pH值至2．8±0．1为流动相，流速为1．0ml·min^-1，检测波长为270nm。结果：对乙酰氨基酚在0．06～0．36mg·ml^-1（r=1．0000），咖啡因在0．02～0．12mg·min^-1（r=0．9999），阿司匹林在0．1～0．6mg·ml^-1（r=1．0000）范围内均与峰面积呈良好的线性关系，平均回收率分别为99．7％，100．3％，99．2％。RSD分别为0．7％，1．1％，0．9％。结论：本法分离度好，快速，简便。可用于复方制剂中3种组分的同时测定。     

HPLC-ELSD测定心肌康颗粒中黄芪甲苷的含量

目的：建立用高效液相色谱法蒸发光散射检测器测定心肌康颗粒中黄芪甲苷的含量测定方法。方法：采用Kromasil ODS C18色谱柱（150×4．6mm 5um）；柱温：40℃；流动相为乙腈-水（32：68）；流速：1.0ml·min^-1；ELSD检测器，漂移管温度：105℃，气体（空气）流速：2．6ml·min^-1。结果：此法线性关系良好，平均加样回收率为98.06%，RSD=1.24％。结论：方法简便可靠，分离度好，可用于心肌康颗粒的质量控制。     

RP-HPLC法测定阿坎酸钙的含量

目的：建立反相高效液相色谱法测定阿坎酸钙含量的方法。方法：采用C18色谱柱（250mm×4．6mm,5μm）,以0．01mol·L^-1醋酸铵溶液（醋酸调pH为5）-甲醇（95：5）为流动相,流速0．5ml·min^-1,检测波长220nm。结果：阿坎酸钙在1．5～10．0mg·ml^-1浓度范围内线性关系良好（r=0．9995）,平均回收率为99．3％,RSD=1．0％（n=9）,最低检测限为14ng。结论：方法准确,重复性好,可有效的控制阿坎酸钙原料药的质量。     

RP-HPLC测定心脑康胶囊中阿魏酸和葛根素的含量

目的：建立心脑康胶囊中阿魏酸和葛根素的RP—HPLC含量测定方法。方法：色谱柱为DIKMA-C18（250mm×4．6mm，5μm），流动相为甲醇-1％的冰醋酸（30：70），流速为1．0ml·min^-1，检测波长为254nm，柱温为室温。结果：阿魏酸和葛根素的的线性范围分别为11．2-67．2μg·ml^-1（r=0．9994），9．0～54μg·ml^-1（r=0．9992），平均回收率分别为98．5％、98．2％，RSD为0．5％、0．8％（n=5）。结论：方法简便，结果准确，可作为心脑康胶囊的质量控制方法。     

RP-HPLC法同时测定茶碱麻黄碱胶囊中2组分的含量

目的：建立反相高效液相色谱法同时测定茶碱麻黄碱胶囊中茶碱和盐酸麻黄碱含量的方法。方法：色谱柱为C18柱（150mm×4．6mm，5μm），流动相为甲醇-0．06mol·L^-1磷酸二氢钾溶液（用磷酸调节pH至2．5）（13：87），流速为0．8ml·min^-1，检测波长为210nm，柱温35℃。结果：茶碱和盐酸麻黄碱浓度分别在18．4—183．8μg·ml^-1（r=0．9998）和4．1-40．8μg·ml^-1（r=0．9993）范围内与峰面积呈良好的线性关系，平均回收率分别为98．9％（RSD=1．1％）和97．6％（RSD=1．2％）。结论：方法简便、准确、重复性好，可用于该制剂的质量控制。     

HPLC法测定洁口净含漱液中替硝唑和醋酸氯己定的含量

目的：建立高效液相色谱法同时测定洁口净含漱液中替硝唑和醋酸氯己定的含量的方法。方法：色谱柱：Inertsil ODS-3（150mm×4．6nm，5μm）；流动相：0．1mol·L^-1磷酸二氢钠-乙腈（72：28），用磷酸调节pH为3．0；检测波长：254nm；流速：1．2ml·min^-1。结果：替硝唑和醋酸氯己定在0．01～0．093mg·ml^-1和0．01～0.090mg·ml^-1的浓度范围内与峰面积呈良好的线性关系，平均回收率分别为99．7％和99．1％，RSD分别为0．71％和0.73％。结论：本法简便快速，检测结果准确可靠，可有效控制制剂的质量。     

HPLC法测定小儿消咳片中小檗碱的含量

目的：建立HPLC法测定小儿消咳片中盐酸小檗碱的含量方法。方法：以迪马钻石C18（250mm×4．6mm，5μm）为色谱柱；流动相：乙腈-0．1％磷酸溶液（每100ml中加入0．1g十二烷基磺酸钠）（50：50）；流速：1．0ml·min^-1；柱温：30℃；检测波长349nm。结果：盐酸小檗碱线性范围为2～21μg·ml^-1（r=0．9996），平均回收率为98．4％，RSD为0．9％（n=6）。结论：方法适用于小儿消咳片中盐酸小檗碱的含量测定。     

HPLC测定维药祖卡木胶囊中大黄素、大黄酚的含量

目的：采用高效液相色谱法测定祖卡木胶囊中大黄素和大黄酚的含量。方法：采用Waters Symmetry C18（150mm×4．6mm，5μm）色谱柱，流动相：甲醇-0．1％磷酸溶液（80：20）；检测波长：254mm；流速1．0ml·min^-1；柱温35℃。结果：大黄素在0．8—6．6μg·ml^-1（r=0．9999，n=5）范围内，有良好的线性关系，平均回收率为98．8％（n=9），RSD为1．7％。大黄酚在2．0—10．2μg·ml^-1（r=0．9999，n=5）范围内，有良好的线性关系，平均回收率为101．3％（n=9），RSD为1．6％。结论：方法具有操作简单、准确的优点，能有效控制祖卡木胶囊的质量。     

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.