无蔗糖型双参活血通络颗粒的质量标准研究

目的:建立无蔗糖型双参活血通络颗粒的质量标准。方法:采用薄层色谱(TLC)法对无蔗糖型双参活血通络颗粒中的三七、丹参、五味子进行定性鉴别;采用反相高效液相色谱法测定制剂中丹参酮ⅡA的含量:色谱柱为SHIMADZU C18(250 mm×4.6mm,5μm),流动相为甲醇-水(75∶25,V/V),检测波长为270 nm。结果:TLC图中能清晰检出三七皂苷R1、丹参酮ⅡA和五味子甲素,鉴别专属性强,阴性对照无干扰。丹参酮ⅡA进样量在0.016 896⁰.337 920μg范围内与峰面积积分值呈良好线性关系(r=0.999 9);精密度、稳定性和重复性试验的RSD<1%;平均加样回收率为99.55%,RSD=0.41%(n=6)。结论:所建标准可用于无蔗糖型双参活血通络颗粒的质量控制。     

复方补骨脂酊的定性定量方法研究

目的建立复方补骨脂酊定性定量方法。方法采用TLC对复方补骨脂酊中补骨脂、白芷、丹参进行定性鉴别,采用HPLC进行含量测定,使用安捷伦TC-C_(18)色谱柱(250 mm×4.6 mm,5μm),乙腈-0.2%磷酸溶液为流动相进行梯度洗脱,检测波长246 nm,进样量10μL。结果薄层色谱斑点清晰,样品与对照药材和对照品在相应的位置上,分别显示相同颜色的荧光斑点;本品中补骨脂素、欧前胡素和丹参酮ⅡA平均含量分别为25.3425、10.1203、24.0054μg·mL~(-1),补骨脂素、欧前胡素和丹参酮ⅡA分别在10.4325~166.92μg·mL~(-1)(r=1.0000)、2.625~42μg·mL~(-1)(r=0.9998)及10.335~165.36μg·mL~(-1)(r=0.9999)与峰面积具有良好的线性关系,且平均加样回收率分别为99.9%(RSD=1.0%)、99.0%(RSD=0.80%)及99.7%(RSD=1.1%)。结论 TLC法可以用于本品补骨脂、白芷、丹参的鉴别,HPLC法可用于本品中补骨脂素、欧前胡素和丹参酮ⅡA的含量测定。     

丹黄胶囊的质量标准研究

目的建立丹黄胶囊的质量标准,为其质控提供依据。方法采用薄层色谱(TLC)法对制剂中的丹参、川芎、五味子和黄芪四味药材进行定性鉴别;采用高效液相色谱法测定制剂中丹参酮ⅡA的含量,色谱条件为C18色谱柱(5μm,250 mm×4.6mm),流动相为甲醇-水(80∶20),检测波长为270 nm,流速1.0 mL·min-1。结果薄层色谱鉴别方法专属性强;丹参酮ⅡA在1.77~15.93 mg·L-1范围内与峰面积呈良好的线性关系(r=0.999 9),丹参酮的平均回收率为99.55%,RSD=1.10%(n=6)。结论该方法准确、灵敏度高,所建标准可用于丹黄胶囊的质量控制。     

高效液相色谱法测定耳络通丸中丹参酮ⅡA的含量

目的采用高效液相色谱法测定耳络通丸中丹参酮ⅡA的含量.方法色谱柱为Kromasil C18柱(250 mm×4.6 mm,5μm),流动相为甲醇-水(8020),流速为1ml·min-1,检测波长为270nm.结果丹参酮ⅡA在0.1～0.8μg范围内线性关系良好(r=0.9995);平均回收率为97.6%(RSD1.9%,n=5).结论该法简便、快速、灵敏,可用于该制剂的质量控制.     

高效液相色谱法测定心舒丸中丹参酮ⅡA含量

目的 建立测定心舒丸中丹参酮ⅡA含量的高效液相色谱(HPLC)法.方法 色谱柱为Diamonsil C18柱(250mm×4.6mm,5μm),流动相为甲醇-水(73∶27),检测波长为270 nm,柱温28℃,流速1.0mL/min.结果 丹参酮ⅡA进样量在0.027 65～0.497 7μg范围内与峰面积线性关系良好(r =0.999 7),平均加样回收率为98.57％,RSD =0.70％ (n=6).结论 该法简便、灵敏、准确、专属、重现性好,为心舒丸的丹参酮ⅡA含量测定提供了可靠方法.     

七味抗体散质量标准研究

目的:建立七味抗体散的质量标准。方法:采用薄层色谱(TLC)法对方中黄芪、当归、丹参3味药材进行定性鉴别;用高效液相色谱法对方中丹参的主要成分丹参酮ⅡA进行含量测定。结果:TLC特征斑点明显。丹参酮ⅡA的检测浓度在5.44～32.64μg.mL-1范围内与峰面积积分值呈良好的线性关系(r=0.9998);平均回收率为99.54%,RSD=0.96%(n=9)。结论:所建质量标准可用于七味抗体散的质量控制。     

通脉丸的质量标准研究

目的:建立通脉丸的质量标准。方法:采用薄层色谱(TLC)法对制剂中丹参、当归、红花进行定性鉴别。采用高效液相色谱法测定制剂中阿魏酸的含量:色谱柱为Diamonsil C18,流动相为乙腈-0.1%磷酸(17∶83,V/V),流速为1 ml/min,检测波长为316nm,柱温为30℃,进样量为10μl。结果:丹参、当归、红花TLC图斑点清晰,分离度好。阿魏酸检测质量浓度线性范围为8~80μg/ml(r=0.999 8);精密度、稳定性、重复性试验的RSD<2%;加样回收率为97.2%~99.6%(RSD=1.2%,n=6)。结论:该研究所建标准可用于通脉丸的质量控制。     

降压抗栓胶囊的质量标准研究

目的建立降压抗栓胶囊的质量标准。方法采用TLC法对处方中丹参、川芎、甘草和酸枣仁进行定性鉴别;采用HPLC法测定丹参酮ⅡA的含量。色谱柱:Inertsil ODS-3色谱柱(250 mm×4.6 mm,5μm);流动相:甲醇-水(75∶25);检测波长:270 nm;流速:1.0 mL·min~(—1);柱温:25℃;进样量:5μL。结果 TLC图斑点清晰,分离度好,阴性无干扰;HPLC法中,丹参酮ⅡA的线性范围为10.375～166.000μg·mL~(—1)(r=0.999 9),平均回收率为100.6%,RSD值为0.9%(n=9)。结论该方法操作简便、专属性高,可作为降压抗栓胶囊质量控制的常用方法。     

反相高效液相色谱法测定丹参妇康颗粒中丹参酮Ⅱ A的含量

目的建立RP-HPLC测定丹参妇康颗粒中丹参酮Ⅱ A含量的方法.方法色谱柱为Reliasil C18(250 mm×4.6 mm,5 μm),以甲醇-水(75∶25)为流动相,检测波长为270 nm,柱温为30 ℃, 流速为1.0 mL·min-1.样品进样前经提取处理.结果线性范围为0.01～0.20 μg,r=0.999 7;测定丹参酮Ⅱ A含量平均回收率99.82%,RSD=2.55%(n=5).结论本方法简便,分离完全,结果可靠,适用于该制剂丹参酮Ⅱ A含量的测定.     

复方牡蛎合剂的质量控制

目的 建立复方牡蛎合剂的质量控制方法.方法 采用薄层色谱法（TLC法）对当归、白芍、丹参进行定性鉴别,用高效液相色谱法（HPLC法）测定丹参中丹参酮ⅡA的含量.结果 薄层色谱中斑点清晰,易于识别;丹参酮ⅡA线性范围是0.080 26～0.480 15μg,r=0.997 84（n=6）,平均回收率为99.7%,RSD为0.64%（n=6）.结论 该法简便、重现性好,可用于复方牡蛎合剂的质量控制.     

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.     

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.     

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.     

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.