心灵丸质量标准修订研究

目的：建立心灵丸（蟾酥、人工麝香、冰片、体外培植牛黄、熊胆、人参、三七等）的质量标准。方法：采用显微鉴别处方中的珍珠；采用GC及TLC分别对处方中的人工麝香、冰片等进行定性鉴别；采用HPLC法测定华蟾酥毒基和脂蟾毒配基的含量。结果：在GC图谱中可检测到与麝香酮对照品相同保留时间的色谱峰；在TLC图谱中可检出人参、三七等药材的特征斑点；华蟾酥毒基在0．0398～0．4776μg之间线性关系良好，r=0．9998，精密度试验RSD=0．3％（n=6），平均回收率为100．18％，（RSD=0．5％，n=6）；脂蟾毒配基在0．0419～0．5026μg之间线性关系良好，r=0．9998，精密度试验RSD=0．6％（n=6），平均回收率为97．00％，（RSD=0．9％，n=6）。结论：所采用的方法准确、可靠，可行性及重复性良好，能有效控制该制剂的质量。     

感冒灵流浸膏的质量标准研究

采用TLC对感冒灵流浸膏中的三叉苦、岗梅进行定性鉴别；用HPLC测定绿原酸的含量，制定了感冒灵流浸膏的质量标准。在TLC图谱中可检出三叉苦、岗梅的特征斑点；绿原酸在0．2～2．0μg范围内呈良好线性关系，r=0．9999，平均回收率为98．0％，(RSD=0．93％，n=5)。结果显示所建立的方法可行、重复性好，能有效地控制该制剂的质量。     

感冒解痛散质量标准研究

目的制订感冒解痛散的质量标准。方法用薄层色谱（TLC）法对处方中的苍术、甘草进行定性鉴别，用高效液相色谱（HPLC）法对橙皮苷进行含量测定。结果用TLC法能够检出苍术、甘草；含量测定方法中橙皮苷的线性范围为0．2～1．01μg，r=0．9997（n=6），平均回收率为97．9％，RSD=0．61％（n=9）。结论所建立的方法可准确地进行定性、定量检测，可用于该制荆的质量控制。     

可乐定透皮贴剂中有关物质的薄层色谱和高效液相色谱检测方法

目的：用薄层色谱法(TLC法)和高效液相色谱法(HPLC法)对可乐定透皮贴剂中有关物质进行检测。方法：TLC法：以硅胶G为吸附剂，正丁醇一水一冰醋酸(4：5：1)为展开剂。HPLC法：色谱柱为Waters Xterra RP C18，流动相为乙腈-碳酸氢铵水溶液(20：80)，检测波长210nm。结果：TLC法最小检出限为0．15μg；HPLC法最小检出限量为0．67ng。结论：两种方法都可用于可乐定透皮贴剂中有关物质的检测。TLC法操作简单，方便；HPLC法灵敏度高，检出限量低。     

宝儿康散质量标准修订研究

目的：建立宝儿康散（陈皮、太子参、甘草等）的质量标准。方法：采用显微鉴别处方中的芡实、山药；采用TLC分别对处方中的太子参、陈皮、甘草等进行定性鉴别；采用HPLC法测定橙皮苷的含量。结果：在TLC图谱中可检出太子参、陈皮、甘草等药材的特征斑点；橙皮苷在0．04412—1．3236μg之间线性关系良好，r=0．9999，精密度试验RSD=0．14％（n=6），平均回收率为102．63％，（RSD=0．92％，n=6）。结论：所采用的方法准确、可靠，可行性及重复性良好，能有效控制该制剂的质量。     

感冒灵流浸膏的质量标准研究

采用TLC对感冒灵流浸膏中的三叉苦、岗梅进行定性鉴别;用HPLC测定绿原酸的含量,制定了感冒灵流浸膏的质量标准。在TLC图谱中可检出三叉苦、岗梅的特征斑点;绿原酸在0. 2~2. 0μg范围内呈良好线性关系,r=0. 9999,平均回收率为98. 0%,(RSD=0.93%,n=5)。结果显示所建立的方法可行、重复性好,能有效地控制该制剂的质量。     

润肠丸（水蜜丸）的质量标准

目的：建立润肠丸（水蜜丸）的质量标准。方法：采用TLC法对处方中的羌活、大黄、当归进行了定性鉴别;用RP—HPLC法测定了大黄素、大黄酚的含量。结果：在TLC图谱中可检出羌活、大黄、当归的特征斑点;大黄素在0．011—0．110μg范围内呈良好的线性关系,r=0．9996;大黄酚在0．020—0．204txg范围内呈良好的线性关系,r=0．9995。结论：所建立的方法可行、重复性好,能有效的控制该制剂的质量。     

苁蓉补肾丸质量标准的建立

目的：研究建立苁蓉补肾丸的质量标准。方法：采用TLC法对处方中的何首乌、白术进行定性鉴别：用HPLC法测定毛蕊花糖苷的含量。结果：在TLC图谱中可检出何首乌、白术的特征斑点;毛蕊花糖苷在0．162～1．620μg范围内呈良好的线性关系,r＝0．9997,平均回收率为99．36％,RSD=0．49％（n=6）。结论：所建立的方法可行、重复性好,能有效的控制苁蓉补肾丸的质量。     

芪术归胃散的制备与质量控制

目的 研制芪术归胃散,建立其质量控制标准. 方法 以白芍、白及、三七等17味中药为主料,制备芪术归胃散. 用薄层色谱（TLC）法对陈皮进行鉴定,高效液相色谱（HPLC）法测定主要成分白芍中芍药苷的含量,建立该制剂的制备工艺及质量控制方法 . 结果 本品制备简单,在TLC图谱中可检出陈皮的特征色谱;其主要有效成分含量测定方法 可行. 结论 该制剂制备工艺可行,方法 可控.     

肝郁舒颗粒质量标准的研究

目的：建立肝郁舒颗粒的质量标准。方法：采用TLC法鉴别方中柴胡、白芍、枸杞子、枳壳、佛手；用HPLC法测定白芍中芍药苷的含量。结果：在TLC色谱中可检出柴胡、白芍、枸杞子、枳壳、佛手的特征斑点；芍药苷平均加样回收率为99．71％，RSD为1．6％。结论：所建鉴别方法专属性强，定量方法简便、准确。能有效地控制制剂的质量。     

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.