高效液相色谱法测定天麻素片中天麻素的含量

目的采用高效液相色谱法测定天麻素片中天麻素的含量。方法使用C18柱（Hypersil ODS2 5μm，4．6mm×200mm）。柱温30℃，流动相：甲醇-磷酸盐溶液[（0．1mol·L^-1磷酸二氢钾溶液和0．1mol·L^-1磷酸氢二钠溶液等量混合-水）（2：96）]（0．04：0．92）；检测波长220nm；流速0．96mL·min^-1.结果采用高效液相色谱法测定天麻素的含量，线性范围为9．654～22．526μg·mL^-1，r=0．9997；平均回收率为100．9％（RSD=0．5％）。结论用高效液相色谱法测定天麻素片中天麻素的含量，方法简便快速准确，能更好地控制产品质量。     

RP-HPLC测定康乐鼻炎片中马来酸氯苯那敏的含量

目的：建立RP—HPLC法测定康乐鼻炎片中马来酸氯苯那敏含量的方法。方法：采用Agilent ODS C18（250mm×4．6mm，5μm）色谱柱；流动相为甲醇-水-磷酸（45：55：0．2），检测波长为315nm，流速为1．0ml·min^-1。结果：马来酸氯苯那敏在5．0—47．9μg·m^-1浓度范围内与峰面积呈良好的线性关系（r=0．9999），平均回收率为97．7％，RSD=1．6％（n=5）。结论：方法简单、快速、可作为产品的质量控制方法。     

HPLC法测定复方金刚烷胺氨基比林片中马来酸氯苯那敏的含量及含量均匀度

目的：建立用HPLC法测定复方金刚烷胺氨基比林片中马来酸氯苯那敏的含量及含量均匀度。方法：色谱柱为DiamonsilC18柱（250mm×4．6mm,5μm）,流动相为0．0015％庚烷磺酸钠溶液（含三乙胺0．08％,用冰醋酸调pH至3．3）-甲醇-乙腈（31：47：22）,检测波长为262nm,流速为1．0ml·min^-1。结果：线性范围为0．10～0．70μg（r=0．9998）,平均回收率为100．4％,RSD为0．5％（n=6）。结论：方法简便准确、灵敏度高,重复性好,可用于复方金刚烷胺氨基比林片中马来酸氯苯那敏的含量及含量均匀度测定。     

HPLC法分别测定芍连胃乐片中芍药苷与盐酸小檗碱含量

目的：建立测定芍连胃乐片中芍药苷和盐酸小檗碱含量的高效液相色谱法。方法：芍药苷含量测定采用C18（200mm×4．6mm，5μm），流动相为乙腈：0．05mol·L^-1磷酸二氢钾溶液（15：85），检测波长为230nm。盐酸小檗碱含量测定采用C18（250mm×4．6mm，5μm），流动相为乙腈：0．033mol·L^-1磷酸二氢钾溶液（32：68），检测波长为265nm。结果：芍药苷在3．0—48．3μg·ml^-1范围内线性关系良好（r=1．0000），平均回收率为98．1％，RSD为0．5％；盐酸小檗碱在1．0～16．4μg·ml^-1范围内线性关系良好（r=1.0000），平均回收率为98．9％，RSD为1．0％。结论：本方法简便、可靠、准确。     

HPLC法测定康乐鼻炎片中马来酸氯苯那敏的含量

目的 建立康乐鼻炎片中马来酸氯苯那敏的含量测定方法。方法 色谱柱Thermo C18（250mm×4．6mm,5um）,用乙腈-甲醇-水-冰醋酸（35：35：30：0．5）（含十二炕基硫酸钠0．35％）为流动相,流速为1．0ml／min,检测波长为260nm。结果 本方法的线性范围10．3～76．9ug／ml（r=-0．9999）,平均回收率为97．6％,RSD为2．5％。结论 本方法可用于控制康乐鼻炎片中马来酸氯苯那敏的含量。     

高效液相色谱法测定复方樟脑酊中吗啡含量

目的：建立高效液相色谱法测定复方樟脑酊中吗啡含量的方法。方法：色谱柱为Kromasil100-5C18（4．6mm×250mm，5μm），流动相为0．05mol·L^-1磷酸二氢钾-0．0025mol·L^-1庚烷磺酸钠溶液-乙腈（5：5：2），检测波长220nm，流量1．0mL·min^-1，柱温30℃。结果：吗啡在4．241～21．20μg·mL^-1范围内，浓度与峰面积线性关系良好（r=0．9998）；样品的平均加样回收率为99．57％，RSD为1．21％（n=6）。结论：此方法简便、快速，可作为复方樟脑酊中吗啡的含量测定方法。     

赤鲜红褪色分光光度法测定马来酸氯苯那敏

目的：建立赤鲜红褪色分光光度法测定马来酸氯苯那敏的含量。方法：在弱酸性介质中，马来酸氯苯那敏（CPM）与赤鲜红（ET）或曙红Y（EY）阴离子借静电引力和疏水作用力而形成离子缔合复合物。结果：溶液的吸收光谱发生变化，赤鲜红体系发生明显的褪色作用，最大褪色波长位于525nm，CPM浓度在0．1～4．0μg·mL^-1范围内遵从比尔定律，ε为3．5×10^4L·mol^-1·cm^-1。结论：方法灵敏度较高，选择性好，操作简便快速，用于片剂及尿液中马来酸氯苯那敏的测定，结果满意。     

反相高效液相色谱法同时测定酚氨咖敏颗粒中四组分的含量

目的：建立测定酚氨咖敏颗粒中四组分的分析方法。方法：反相高效液相色谱法，采用Diamonsal C18柱（150mm×4．6mm，5μm），以甲醇-0．1％二乙胺（25：75）（用冰醋酸调pH至4．5）为流动相；检测波长：对乙酰氨基酚、咖啡因、氨基比林为275nm，马来酸氯苯那敏为215nm；流速：1．0mL·min^-1。结果：对乙酰氨基酚、咖啡因、氨基比林、马来酸氯苯那敏线性范同分别为25～400，6～120，20～320，3～50μg·mL^-1平均回收率（n=9）分别为99．35％，100．10％，101．20％，101．92％。结论：该方法分离度良好，灵敏度高，准确且简便易行。     

高效液相色谱法测定酚氨咖敏片中马来酸氯苯那敏含量均匀度

目的：探讨高效液相色谱法（HPLC）测定酚氨咖敏片中马来酸氯苯那敏含量均匀度的方法。方法：采用HPLC,Alltima C18（4．6min×250mm,5μm）;1％醋酸溶液（用二乙胺调节pH值至3．7）-甲醇（62：38）为流动相;检测波长260nm。结果：进样量在0．12-0．80μg与峰面积的线性关系良好（r=-0．9999）;平均回收率为99．75％,99．90％,99．68％;RSD为0．42％,0．25％,0．70％（n=3）,精密度、重复性良好。结论：所建方法准确、简便、快速,适用于酚氨咖敏片中马来酸氯苯那敏含量均匀度的测定。     

HPLC法测定咳特灵颗粒中马来酸氯苯那敏的含量

目的建直咳特灵颗粒的含量测定标准以控制产品质量。方法采用高效液相色谱法测定制剂中马来酸氯苯那敏的含量，高效液相色谱条件：Hypersil柱（4．6mm×250mm，5μl）、流动相为乙腈-0．3％十二烷基硫酸钠溶液-磷酸（65：35：0．02）：检测波长为262nm。结果高效液相法测定马来酸氯苯那敏，重复性好，精度高。结论该方法可用于咳特灵颗粒中的马来酸氯苯那敏的含量。     

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.     

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.