川贝枇杷糖浆的质量标准研究

目的:建立川贝枇杷糖浆的质量标准.方法:采用薄层色谱法鉴别川贝枇杷糖浆中的枇杷叶,采用毛细管气相色谱法测定该制剂中薄荷脑含量.结果:薄层色谱法可检出枇杷叶;毛细管气相色谱法测定该制剂中薄荷脑含量为0.012 1～0.302 4 mg·ml-1,线性范围为0.007 84～1.411 mg·ml-1;平均加样回收率100.3%(n=6),RSD=1.4%.结论:本法简便高效,结果准确可靠,可用于川贝枇杷糖浆的质量控制.     

枇杷止咳糖浆质量标准的建立

目的:建立了枇杷止咳糖浆的质量标准。方法:采用薄层色谱法鉴别本品中的桔梗、甘草、盐酸麻黄碱,采用高效液相色谱法测定本品中的盐酸麻黄碱含量。结果:TLC法可鉴别出桔梗、甘草、盐酸麻黄碱,特征斑点明显,无阴性样品干扰。HPLC法测定本品中盐酸麻黄碱方法准确度高、稳定性、重复性好。平均回收率为100.1%,RSD为1.06%(n=9)。结论:本文为枇杷止咳糖浆的质量控制提供了稳定可行的定性定量方法。     

半夏糖浆质量标准研究

目的研究半夏糖浆（麻黄、枇杷叶、陈皮等）内在质量的控制方法。方法采用薄层色谱（TLC）法对方中的枇杷叶、陈皮、甘草3味药材进行定性鉴别；用高效液相色谱（HPLC）法对方中麻黄的有效成分盐酸麻黄碱进行含量测定。结果定性鉴别薄层色谱特征明显，专属性强；方法学考察表明，盐酸麻黄碱进样量在0．0854-0．5126μg范围内与峰面积具有良好的线性关系（r=0.9999），平均回收率为99．30％（n=9），RSD=0.31％。结论方法准确、可靠、重现性好，可用于半夏糖浆的质量控制。     

清热止咳糖浆质量标准

目的：建立清热止咳糖浆的质量标准。方法：采用薄层色谱法对其中的麻黄,甘草,桔梗进行定性鉴别,以高效液相色谱法对其主要药材麻黄中的麻黄碱进行含量测定。结果：麻黄、甘草、桔梗的供试品薄层色谱中,在与对照品相同位置上显相同颜色的斑点;盐酸麻黄碱在1．71—54．65μg·ml^-1浓度范围内线性关系良好（r=1．0000）。结论：本方法简便、准确、灵敏、重复性好,可用于本品的质量控制。     

儿童咳颗粒质量标准研究

目的儿童咳颗粒的质量标准研究。方法采用薄层色谱法鉴别麻黄、百部、前胡,用高效液相色谱法测定儿童咳颗粒中麻黄碱的含量。结果能准确对麻黄、百部、前胡进行定性鉴别,薄层斑点清晰、重现性好;盐酸麻黄碱在在进样量为5.00～75.00μg范围内与峰面积积分值呈良好线性关系。含量测定回收率是101.17%,RSD=2.35%。结论该法简便、快速、准确,灵敏,可作为该制剂质量控制的有效方法。     

肺炎糖浆的质量标准研究

目的建立肺炎糖浆的薄层鉴别方法和含量测定方法。方法采用薄层色谱法对处方中连翘、金银花和玄参进行定性鉴别;采用HPLC法对君药麻黄中的盐酸麻黄碱进行含量分析。结果薄层色谱斑点清晰,阴性无干扰;制定了麻黄中盐酸麻黄碱含量标准。结论该方法简便快速,结果准确可靠,可作为该制剂的质量控制标准。     

桉叶止咳糖浆的质量标准研究

目的：对桉叶止咳糖浆的质量标准进行研究，提高质量标准控制水平。方法：采用薄层色谱法对桔梗、枇杷叶进行鉴别，用高效液相色谱测定盐酸麻黄碱的含量。结果：桔梗、枇杷叶的薄层色谱斑点清晰，分离度好，专属件强。阴性无干扰。盐酸麻黄碱测定方法经方法学验证，结果线性、精密度、重复性、溶液稳定性较好，方法可行。结论：提高后的质量标准方法町行，能够对桉叶止咳糖浆的质量进行控制。     

甘草麻黄碱片的质量控制方法研究

目的:建立甘草麻黄碱片的质量控制方法。方法:采用薄层色谱法对甘草麻黄碱片中甘草进行定性鉴别;采用高效液相色谱法测定甘草麻黄碱片中盐酸麻黄碱含量。结果:在薄层色谱中能检测出甘草;盐酸麻黄碱检测浓度在0.502～7.530μg/ml范围内呈良好的线性关系(r=0.9998),平均加样回收率为98.80%(RSD=0.42%)。结论:本方法可用于甘草麻黄碱片的质量控制。     

鼻炎灵喷雾剂的质量标准

目的建立鼻炎灵喷雾剂的质量标准。方法采用高效液相色谱法测定麻黄中盐酸麻黄碱的含量,采用薄层色谱法对麻黄、防风进行定性鉴别。结果盐酸麻黄碱含量在7.1~28.2μg.ml-1,呈良好的线性关系,平均回收率为99.19%,RSD为2.34%;以薄层色谱法对麻黄、防风进行专属定性分析。结论建立的方法可准确地进行定性、定量检测,重复性好,可作为鼻炎灵喷雾剂的质量控制。     

4个厂家83批复方桔梗麻黄碱糖浆(Ⅱ)的质量分析

目的:通过对4个厂家83批复方桔梗麻黄碱糖浆(Ⅱ)的国家评价性抽验结果进行分析,评价其质量。方法:采用法定检验方法和探索性研究进行样品检测,统计分析并评价。探索性研究内容包括采用高效液相色谱法测定防腐剂苯甲酸等的含量和盐酸麻黄碱的含量,处方抑菌效力检查研究,溶液pH值测定;采用旋光光度法测定蔗糖的含量,氯化铵含量与微生物污染之间联系的研究,采用顶空气相色谱法同时测定薄荷脑和乙醇的含量,采用薄层色谱法对桔梗流浸膏进行鉴别研究。结果:法定检验结果显示,在83批样品中,80批合格,3批不合格,合格率为96.4%。不合格项目分别为装量、微生物限度及氯化铵含量、氯化铵含量。法定检验联合探索性研究结果表明,本品存在处方抑菌效力不符合规定、部分原辅料未按处方量投料、产品质量不均等情况。建议修订本品质量标准:增加桔梗薄层色谱鉴别、p H值测定、防腐剂含量测定、薄荷脑含量测定;将盐酸麻黄碱含量测定方法修订为高效液相色谱法等。结论:复方桔梗麻黄碱糖浆(Ⅱ)样品总体质量较差,部分厂家的生产工艺及质量控制存在较大缺陷,质量标准有待提高。     

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.