苦参饮片质量标准研究

目的:建立苦参饮片的质量标准。方法:采用薄层色谱(TLC)法对制剂进行定性鉴别,采用高效液相色谱(HPLC)法测定制剂中苦参碱和氧化苦参碱的含量。结果:TLC中斑点清晰、分离度好。苦参碱、氧化苦参碱的进样量分别在0.02494～0.64844μg(r=0.9999)、0.0734～1.9084μg(r=0.9999)范围内与各自峰面积积分值呈良好线性关系;二者平均回收率分别为102.9%、102.3%,RSD分别为6.9%、2.7%(n=6)。结论:所建标准可用于苦参饮片的质量控制。     

HPLC-DAD法测定商品苦参根茎和根中5个生物碱的含量

目的:测定商品苦参根茎和根中苦参碱、氧化苦参碱、槐果碱、氧化槐果碱、槐定碱的含量,主要了解苦参根茎中苦参碱和氧化苦参碱总量是否达到中国药典2010年版规定的不低于1.0%。方法:采用Welch Materials XtimateTM C18(4.6 mm×150mm,5μm)色谱柱,流动相A为10 mmol.L-1醋酸铵水溶液(0.1%氨水调至pH 9.2),流动相B为乙腈,梯度洗脱,流速1 mL.min-1,检测波长220 nm。结果:苦参碱进样量在0.1575～2.205μg(r=0.9999),氧化苦参碱在0.8985～12.58μg(r=0.9999),槐果碱在0.1360～1.904μg(r=0.9999),氧化槐果碱在0.4398～6.153μg(r=0.9998),槐定碱在0.2092～2.926μg(r=0.9998)范围内呈良好的线性关系;加样平均回收率(n=3)分别为101.0%～102.5%(RSD≤2.1%),100.8%～101.6%(RSD≤2.8%),102.3%～103.6%(RSD≤1.2%),102.2%～103.4%(RSD≤1.1%),102.4%～103.3%(RSD...     

麦味地黄胶囊质量标准提高研究

目的：修订并提高麦味地黄胶囊的质量标准。方法：采用薄层色谱法鉴别处方中麦冬、酒萸肉、牡丹皮和茯苓;采用高效液相色谱法同时测定酒萸肉中的莫诺苷、马钱苷和醋五味子中的五味子醇甲的含量。结果：麦冬、酒萸肉、牡丹皮和茯苓的薄层鉴别方法专属性强;莫诺苷、马钱苷和五味子醇甲的线性范围分别为0.02～0.63μg（r=0.9999）、0.02～0.62μg（r=1）、0.01～0.24μg（r=0.9999）,平均回收率分别为96.3%（RSD=0.6%）、97.7%（RSD=0.3%）、100.6%（RSD=1.9%）。     

妇康洗剂质量标准研究

目的:建立妇康洗剂的质量标准。方法:采用TLC法对处方中苦参、紫草、甘草、乌梅进行定性鉴别;采用HPLC法以乙腈-甲醇-0.1%磷酸溶液(三乙胺调pH至7.5)(12:5:83)为流动相;在检测波长220 nm处测定氧化苦参碱和苦参碱的含量。结果:TLC鉴别分离度良好,专属性强。氧化苦参碱在0.1946~2.9190μg,相关系数r为0.9999,线性关系良好;苦参碱在0.1134~1.7010μg,相关系数为0.9999,线性关系良好。平均加样回收率分别为99.63%(RSD为2.19%)、99.12%(RSD为1.33%)。结论:该方法简便、准确,重复性好,可有效控制妇康洗剂的质量。     

开喉剑喷雾剂的质量控制

目的：建立开喉剑喷雾剂的质量控制标准。方法：用薄层色谱法定性鉴别制剂中的八爪金龙;采用高效液相色谱法测定制剂中苦参碱的含量,色谱柱：Agilent ZORBAX NH2（250mm×4.6mm,5μm）,流动相：乙腈-异丙醇-3%磷酸溶液（82∶4.5∶13.5）,检测波长：220nm,流速：1.0mL·min-1,柱温：30℃。结果：薄层色谱斑点清晰,分离度好,阴性无干扰;苦参碱的线性范围分别为0.25872～2.58720μg（r=0.9999）,平均加样回收率（n=6）分别为102.51%,RSD分别为1.43%。结论：定性定量分析方法快速、准确、专属性强,本法更好地控制开喉剑喷雾剂的质量。     

白庀丸的质量标准

目的:建立白庀丸质量标准。方法:用薄层色谱法对处方中的川芎、当归、苦参、苍术进行定性鉴定;采用薄层扫描法对苦参中的氧化苦参碱进行含量测定。结果:薄层色谱中斑点清晰易于观察,氧化苦参碱在0.4～2.0μg范围内线性关系良好,r=0.999 8,平均回收率为97.1%,RSD为2.6%(n=5)。结论:方法简便准确,能有效控制制剂的质量。     

苦参配方颗粒质量控制研究

目的建立苦参配方颗粒的质量控制标准。方法采用薄层色谱(TLC)法鉴别苦参配方颗粒中苦参碱、槐定碱和氧化苦参碱。采用高效液相色谱(HPLC)法测定苦参配方颗粒中苦参碱和氧化苦参碱,色谱条件为Lichrospher-5NH2色谱柱(250mm×4.6mm,5μm);流动相:乙腈–无水乙醇–3%磷酸溶液(80∶10∶10);体积流量:1.0mL/min;柱温:30℃;检测波长:220nm;进样量:10μL。结果苦参碱、槐定碱和氧化苦参碱在TLC色谱图中相应的位置上显相同的斑点。苦参碱在0.15～1.58μg、氧化苦参碱在0.17～1.68μg呈良好的线性关系,回收率分别为98.3%、101.5%,RSD值分别为1.35%、1.73%。结论该方法快速、灵敏、准确,可用于苦参配方颗粒的质量控制。     

高效液相色谱法测定当归苦参丸中苦参碱和氧化苦参碱

目的建立测定当归苦参丸中苦参碱和氧化苦参碱含量的高效液相色谱法。方法采用Phenemonex C18（250mm×4．6mm，5μm）色谱柱，流动相：乙腈-0．1％三氟醋酸溶液（5：95），流速：1．0mL·min^-1，检测波长：208nm，柱温：35℃。结果苦参碱和氧化苦参碱线性范围分别为0．0512～0．3584μg（r=0．9990）和0．1924～1．3468μg（r=0．9999）；平均回收率分别为98．73%,100．14％（n=6）。结论该方法操作简单，重现性好，检测灵敏度、准确度高，且样品分离效果好。适用于当归苦参丸中苦参碱和氧化苦参碱的含量测定。     

连蒲胶囊中苦参含量测定方法研究

目的进行连蒲胶囊中苦参的含量测定方法研究。方法建立高效液相色谱-可变波长检测法（HPLC-VWD）测定制剂中苦参碱的含量。结果苦参碱在0.412μg-6.592μg·mL^-1范围内呈良好的线性关系,回归方程：A=1670.26x-9.28（r=0.9999,n=7）,回收率103.4%,RSD=1.0%（n=9）。结论本法简便快捷、准确可靠,可为连蒲胶囊的质量标准研究提供依据。     

蒙药肝乐康胶囊的质量标准研究

目的:建立蒙药肝乐康胶囊的质量标准。方法:采用薄层色谱(TLC)法对方中肋柱花、栀子、苦参进行定性鉴别;采用高效液相色谱法测定苦参中苦参碱和氧化苦参碱的含量:色谱柱为lnertsil NH2Columns C18(250 mm×4.6 mm,5μm),流动相为乙腈-3%磷酸水-无水乙醇(80∶10∶10,V/V),流速为0.1 ml/min,柱温为30℃,检测波长为220 nm。结果:肋柱花、栀子、苦参的斑点清晰、分离度好;苦参碱的进样量在0.2¹.2μg、氧化苦参碱在0.31.2μg、氧化苦参碱在0.3¹.8μg范围内与各自峰面积积分值呈良好线性关系;二者精密度、稳定性、重复性试验的RSD<1.72%;平均加样回收率苦参碱为102.00%(RSD=0.93%,n=6),氧化苦参碱为98.02%(RSD=0.78%,n=6)。结论:所建标准可用于蒙药肝乐康胶囊的质量控制。     

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.     

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.     

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.     

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.