厚术胶囊质量标准研究

目的:建立厚术胶囊的质量标准。方法:采用薄层色谱(TLC)法对方中苍术、三七、白芍和山楂药材进行定性鉴别;采用高效液相色谱法测定厚朴中厚朴酚、和厚朴酚的含量。结果:TLC斑点清晰,阴性对照无干扰。厚朴酚与和厚朴酚的进样量分别在0.080～0.400μg(r=0.9999)、0.048～0.240μg(r=0.9999)范围内与各自峰面积积分值呈良好的线性关系;平均回收率分别为98.42%、98.34%,RSD分别为0.63%、0.90%(n=6)。结论:所建标准可有效控制厚术胶囊的质量。     

RP-HPLC法同时测定消化胶囊中厚朴酚与和厚朴酚的含量

目的建立同时测定消化胶囊中厚朴酚与和厚朴酚含量的反向-高效液相色谱法。方法采用高效液相色谱仪。色谱柱:Amethyst C18-H(200 mm×4.6 mm,5μm),流动相为乙腈-水-冰醋酸(60∶38∶2,V/V/V),流速为1.0 ml/min,柱温为30℃,检测波长为294 nm。结果厚朴酚进样量在0.1048~2.0960μg范围内线性关系良好(r=1.0000),平均回收率(n=6)为98.72%(RSD=0.26%);和厚朴酚进样量在0.1014~2.0276μg范围内线性关系良好(r=1.0000),平均回收率(n=6)为96.73%(RSD=0.69%)。结论建立的反向-高效液相色谱法准确、快捷,简便,结果稳定,可用于消化胶囊的含量测定。     

HPLC法测定藿香正气片中厚朴酚与和厚朴酚的含量

目的 建立测定藿香正气片中厚朴酚与和厚朴酚的含量。方法 采用高效液相色谱法、以ODSC18为色谱柱,甲醇-乙腈-水(48;22：30)为流动相,检测波长294nm。结果 藿香正气片中厚朴酚的含量在11．36μg～56．80μg范围内线性关系良好(r=0．9992)、和厚朴酚(在5．20g～26．00g范围内)线性关系良好(r=0．9993),厚朴酚平均回收率100．8％,RSD=1．67％,和厚朴酚平均回收率101.2％,RSD=1.38%,结论 本方法测定简便、快速,测定结果准确。     

高效液相色谱法测定舒肝快胃丸中厚朴酚与和厚朴酚的含量

目的建立测定舒肝快胃丸中厚朴酚与和厚朴酚含量的高效液相色谱法。方法 色谱柱为Dikma DiamonsilC18柱(250mm×4.6mm,5μm);流动相为甲醇-水-冰醋酸(82∶18∶0.25);检测波长为294nm:柱温:35℃,流速:1.0mL·min-1。结果厚朴酚进样量在0.100～1.25μg与峰面积线性关系良好,r=0.999 9,平均回收率为98.4%,RSD=1.2%;和厚朴酚进样量在0.091 70～1.14μg与峰面积线性关系良好,r=0.999 3,平均回收率为98.6%,RSD=1.3%(n=6)。结论该方法专属性强,操作简便,重现性好,适合舒肝快胃丸的质量控制。     

RP—HPLC同时测定菝葜药材中总槲皮素和山柰酚含量

目的:建立同时测定菝葜药材中槲皮素和山柰酚含量的反相高效液相色谱法。方法:色谱柱:Lichrospher C_(18)柱(250 mm×4.6 mm,5 μm),流动相:甲醇-0.5%磷酸水溶液(55:45),流速:1.0 mL·min~(-1),检测波长:365 nm。结果:槲皮素在2.97～29.7μg·mL~(-1)浓度范围内线性关系良好(r=0.9999),山柰酚在3.01—30.1μg·mL~(-1)浓度范围内线性关系良好(r=0.9999),方法回收率分别为98.9%和99.7%。结论:本方法简便、准确,灵敏度高,重复性好,可为评价菝葜药材质量提供依据。     

胃肠康胶囊质量标准研究

目的建立胃肠康胶囊的质量标准.方法采用薄层色谱（TLC）法对方中粉葛进行定性鉴别;采用高效液相色谱（HPLC）法测定了方中君药厚朴中厚朴酚与和厚朴酚的总含量.结果薄层鉴别专属性强;厚朴酚在0.094 9～1.423 2 μg范围内、和厚朴酚在0.040 2～0.602 4 μg范围内,呈良好的线性关系.厚朴酚平均加样回收率为101.18%,RSD＝1.08%;和厚朴酚的平均加样回收率为100.47%,RSD＝1.89%.结论该法快速、简便、准确、重现性好,可用于控制胃肠康胶囊的质量.     

复方天麻颗粒质量标准的研究

目的:建立复方天麻颗粒的质量标准。方法:采用薄层色谱法对方中五味子、麦冬进行鉴别。用高效液相色谱法对天麻中有效成分天麻素进行含量测定。色谱柱为 Kromasil-C_(18)柱(4.6 mm×250 mm,5 μm),柱温25℃;流动相为乙腈-0.05%磷酸溶液(2.5:97.5),流速1.0 mL·min~(-1);检测波长为220 nm。结果:薄层鉴别,色谱特征斑点明显;高效液相色谱法测定,天麻素在0.21～0.83 μg范围内线性关系良好(r=0.9999),平均回收率为98.2%(RSD=1.6%,n=6)。结论:本方法可有效地控制复方天麻颗粒的质量。     

高效液相色谱法测定唇齿清胃丸中大黄素和大黄酚含量

目的建立测定唇齿清胃丸中大黄素和大黄酚含量的高效液相色谱法。方法采用高效液相色谱法,Agilent Zorbax XDB-C18色谱柱(4.6mm×150mm,5μm);流动相:甲醇-0.01%磷酸(80∶20);流速:1.0mL.min-1;紫外检测波长:254nm。结果大黄素和大黄酚线性范围分别为0.01078~0.4312μg、0.02315~0.9260μg范围内呈良好的线性关系(均为r=0.9999),平均回收率分别为98.7%、99.4%(n=9),RSD=1.5%、RSD=1.2%。结论本方法操作简便,结果准确、可靠。     

HPLC法同时测定开胸顺气丸中橙皮苷、和厚朴酚与厚朴酚的含量

目的:建立同时测定开胸顺气丸中橙皮苷、和厚朴酚与厚朴酚含量的方法。方法:采用高效液相色谱法。色谱柱为Agi-lentZORBAXSB-C18柱,流动相为甲醇(A)-5%冰醋酸溶液(B)(梯度洗脱),流速为1.0mL·min-1,柱温为40℃,进样量为10μL,检测波长0～20min为284nm、20～65min为294nm。结果:橙皮苷进样量在0.1717～4.292μg范围内(r=0.9998)、和厚朴酚进样量在0.04004～1.001μg范围内(r=0.9994)、厚朴酚进样量在0.09280～4.640μg范围内(r=0.9998)与各自峰面积积分值均呈良好的线性关系;平均回收率分别为99.88%、99.34%、99.34%,RSD分别为0.67%、1.10%、0.86%(n=6)。结论:本法简便、准确、重复性好、精密度高,可更好地控制开胸顺气丸的质量。     

HPLC法测定胃健宁胶囊中和厚朴酚及厚朴酚的含量

目的建立胃健宁胶囊中和厚朴酚及厚朴酚的检测方法。方法色谱条件为C18色谱柱;流动相:乙腈-水-冰醋酸(60∶40∶1)(V∶V∶V);流速:1.000 mL·min-1;检测波长:294 nm。结果胃健宁胶囊中和厚朴酚在0.02⁰.32μg(r=0.999 6)范围内线性关系良好,平均回收率为96.58%,RSD为1.78%(n=9);厚朴酚在0.019 60.32μg(r=0.999 6)范围内线性关系良好,平均回收率为96.58%,RSD为1.78%(n=9);厚朴酚在0.019 6⁰.313 6μg(r=0.999 8)范围内线性关系良好,厚朴酚的平均回收率为97.29%,RSD为1.39%(n=9)。结论该方法简便,准确度高,可有效控制胃健宁胶囊的质量。     

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.     

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.