GC法测定一种治疗关节炎成方制剂的SFE-CO2提取物中桂皮醛含量

目的用GC法测定追风透骨方SFE-CO2提取物中桂皮醛含量。方法GC法测定,HP-5石英毛细管色谱柱(30m×0.25mm)。结果桂皮醛线性回归方程结论:Y=367.82X 15.799,r=0.9993呈良好线性关系。结论本方法灵敏、稳定、可行。     

气相色谱-质谱法测定香桂化浊胶囊中桂皮醛的含量

目的建立气相色谱-质谱法测定香桂化浊胶囊中桂皮醛含量。方法采用HP-5弹性石英毛细管色谱柱(30 m×0.25 mm,0.25μm),载气:氦气,流速:1.0 m L·min-1,分流比:50∶1,程序升温,进样量1.0μL。结果香桂化浊胶囊中桂皮醛和其他成分的分离度良好,在0.02~4.00 mg·m L-1范围内线性关系良好,相关系数为0.999 4。桂皮醛的平均加样回收率为96.2%,RSD<2.11%。结论该方法操作简便,定量准确,适用于香桂化浊胶囊中桂皮醛的含量测定。     

HPLC法测定复方姜桂酊中桂皮醛的含量

目的:建立复方姜桂酊中桂皮醛的高效液相色谱测定方法.方法:采用Kromasil C18(250mm×4.6mm,5μm)色谱柱;以甲醇-水(68:32)为流动相,流速为1ml·min-1,检测波长为280nm.结果:桂皮醛的线性范围为0.03～0.26μg(r=0.9998);平均回收率为98.7(n=6)%,RSD为0.9%(n=6).结论:方法简便可行、重复性好,可用于本制剂中桂皮醛的含量测定.     

HPLC法测定小儿平喘配方颗粒和煎剂颗粒中桂皮醛的含量

目的:测定小儿平喘配方颗粒及煎荆颗粒中桂皮醛的含量。方法:采用高效液相色谱法,Hypersil ODS2柱,乙腈- 0.1%磷酸溶液(40:60)为流动相,检测波长250 nm。结果:桂皮醛在(0.089～0.89)μg范围内与峰面积之间线性关系良好(r =0.999 9);桂皮醛在小儿平喘配方颗粒中的回收率为101.40%,RSD为1.42%。结论:配方颗粒与煎剂颗粒的色谱图基本一致,配方颗粒中桂皮醛含量高于煎剂颗粒。     

RP-HPLC法测定小建中片中桂皮醛的含量

目的:建立测定小建中片中桂皮醛含量的方法。方法:采用反相高效液相色谱法。色谱柱为Waters C18柱,流动相为乙腈-水(34:66),流速为1.0 mL.min-1,检测波长为290nm,进样量为10μL,柱温为30℃。结果:桂皮醛进样量在0.03942～0.4731μg(r=0.9999)范围内与峰面积积分值线性关系良好;平均加样回收率为98.8%,RSD为0.8%(n=6)。结论:该方法快速简便、准确可靠,重复性好,可用于小建中片中桂皮醛的含量测定。     

高效液相色谱法测定生桂口服液中桂皮醛含量

目的建立生桂口服液中桂皮醛的含量测定方法。方法采用反相高效液相色谱法，色谱柱为Diamonsil C18柱（150mm×4．6mm，5μm），甲醇-水-冰醋酸（45：55：0、5）为流动相，流速为l、0mL／min，测定波长为274nm。结果方法的平均回收率为99、39％，RSD=0、27％，桂皮醛的线性范围是25．2～201、4μg／mL。结论所建立的方法准确、可靠，能满足该产品的质量控制要求。     

高效液相色谱法测定八味肉桂胶囊中桂皮醛和甘草酸的含量

目的建立高效液相色谱同时测定八味肉桂胶囊中桂皮醛和甘草酸含量的方法。方法 Hypersil-C18（250mm×4.6mm,5μm）色谱柱。流动相：3%冰醋酸-乙腈=28：72;流速：1.0mL.min-1;检测波长：285nm（0～15min）,250nm（15.1～30min）,柱温：室温。结果桂皮醛和甘草酸保留时间分别为10.4和20.9min,与各自相邻峰的分离度均〉1.5。以峰面积对进样浓度线性回归,桂皮醛回归方程：Y=0.01056X-2.878,r=0.9999,线性范围19.5～175.6μg.mL-1。甘草酸回归方程：Y=0.1396X＋0.9008,r=0.9997,线性范围6.85～61.65μg.mL-1。桂皮醛和甘草酸的回收率分别为100.4%和99.8%、RSD分别为2.78%和1.72%。结论本方法操作简便,测定结果准确可靠,可用于八味肉桂胶囊中桂皮醛和甘草酸的含量测定。     

HPLC法测定瑞克卫瑞消毒液中桂皮醛和丁香酚的含量

目的建立测定瑞克卫瑞消毒液中桂皮醛和丁香酚含量的高效液相色谱方法。方法色谱柱:采用Welchrom C18柱(250mm×4.6mm,5μm);流动相:甲醇-水(60∶40);流速:1.0mL.min-1;柱温:25℃;检测波长:280nm。结果桂皮醛在0.21～2.1μg(r2=0.999 1)范围内线性关系良好,平均加样回收率为101.3%,RSD为0.1%;丁香酚在0.42～4.2μg(r2=0.999 9)范围内线性关系良好,平均加样回收率为96.7%,RSD为0.3%。结论该方法简单、快速、重复性好,可用于瑞克卫瑞消毒液的质量控制。     

高效液相色谱法测定七味槟榔散中桂皮醛含量

目的 建立测定七味槟榔散中桂皮醛含量的高效液相色谱（HPLC）法,增加七味槟榔散的质量控制指标。方法 采用HPLC外标法,色谱柱为Agilent C18柱（250 mm×4.6 mm,5μm）,以乙腈-水（30∶70）为流动相,流速为1.0 mL/min,检测波长为290 nm。结果 桂皮醛进样量在0.02～0.10μg范围内与峰面积呈良好线性关系（r=1.000 0）,平均回收率为99.15%,RSD=0.12%（n=6）;精密度的RSD=0.33%,样品在12 h内稳定。结论 该方法简便、快速、灵敏,结果准确且重现性好,适用于桂皮醛的含量测定。     

不同产地肉桂HPLC指纹图谱研究及桂皮醛含量分析

目的建立肉桂的HPLC指纹图谱,并测定不同产地肉桂药材中桂皮醛含量。方法采用Phenomenex C18(250mm×4.6mm×5μm)色谱柱,乙腈-0.1%磷酸水溶液梯度洗脱;流速:1.0mL·min-1;检测波长:254nm。用国家药典委员会"中药色谱指纹图谱相似度评价系统(2004A)"处理,比较相似度时将桂皮醛的色谱峰屏蔽。结果 4批进口肉桂的相似度较高,而8批国产肉桂的相似度差异较大。不同产地肉桂药材桂皮醛含量差异较大。结论国产肉桂与进口肉桂指纹图谱比较,相似度差,可为肉桂药材的品种鉴定提供依据。     

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.