桑芎胶囊定性定量分析研究

目的 建立桑芎胶囊定性定量研究方法。方法 采用薄层色谱对处方中桑白皮、黄芩等药材进行鉴别,采用高效液相色谱法对处方白芷中欧前胡素进行含量测定,C₁₈色谱柱（4.6 mm×250 mm,5 μm）,乙腈（A）-水（B）,梯度洗脱,流速为1.0 mL·min^-1;柱温为30 ℃;欧前胡素测量波长为250 nm。结果 桑白皮和黄芩的薄层色谱鉴别方法可行,在薄层色谱中能检出桑白皮、黄芩,欧前胡素在0.038 72～0.774 4 μg范围内线性关系良好,阴性样品试验无干扰,精密度、稳定性及加样回收试验均符合要求（欧前胡素的平均回收率为98.5%,RSD=0.5%）。结论 本试验操作简便、稳定、可靠性高,可为桑芎胶囊质量标准的提高提供依据。     

胃纳欣颗粒的质量标准研究

目的 制定胃纳欣颗粒质量控制标准。方法 采用薄层色谱(TLC)法对胃纳欣颗粒中半夏、茯苓、甘草、枳壳、白芷进行定性鉴别;采用反相高效液相色谱(HPLC)法对柚皮苷进行定量测定。结果 半夏、茯苓、甘草、枳壳、白芷可用TLC法进行定性鉴别;HPLC法测定柚皮苷可达基线分离,紫外检测器在0.0844~0.2954μg时线性良好,回归方程:Y=2×10⁶X+14691,r=0.9993,6次测定平均加样回收率为98.74%,RSD为1.20%。结论 该法可准确定性、定量,能有效控制该制剂的质量。     

桃红通脉颗粒质量标准提高研究

目的 提高桃红通脉颗粒的质量标准。方法 采用薄层色谱（TLC）法对赤芍、地黄、甘草进行薄层鉴别,以及采用高效液相色谱法对主药桃仁的有效成分苦杏仁苷进行鉴别;采用高效液相色谱法测定芍药苷的含量,色谱柱为Agilent HC-C₁₈柱（250 mm×4.6 mm,5 μm）,流动相为乙腈-水（13：87）,流速为1.0 ml/min,柱温为30℃,检测波长为230 nm。结果 赤芍、地黄、甘草的TLC图均斑点清晰,阴性无干扰;芍药苷在1.79~57.28 μg/ml范围内浓度与峰面积线性关系良好（r=0.999 9）,平均回收率为99.99%,RSD为2.05%（n=9）。结论 提高桃红通脉颗粒质量标准后,鉴别方法重现性更好,优化了芍药苷的含量测定方法,增强了成品质量的可控性。     

仙芪扶正颗粒定性定量方法研究

目的 建立对仙芪扶正颗粒进行质量控制的方法。方法 采用薄层色谱(TLC)对黄芪、陈皮、枸杞子、地榆进行定性鉴别。采用高效液相色谱(HPLC)法对处方中陈皮所含指标性成分橙皮苷进行定量分析,C₁₈色谱柱;乙腈-0.01%磷酸（20:80）;检测波长为283 nm,恒温箱温度：30 ℃;流速1.0 mL·min^-1。结果 薄层色谱法可以准确的对黄芪、陈皮、枸杞子、地榆进行鉴别,且专属性较好;橙皮苷进样量在0.114 5～2.29 μg范围内线性关系良好。在回收率试验中橙皮苷的回收率为99.1%(RSD=0.5%,n=6）。结论 该方法操作简单、重现性好,可用于仙芪扶正颗粒的质量控制。     

复方醋酸氯己定软膏质量标准研究

目的 提高复方醋酸氯己定软膏的质量控制标准。方法 增补处方中薄荷脑、樟脑的薄层色谱(TLC)法鉴别;建立高效液相色谱法同时测定处方中醋酸氯已定、盐酸丁卡因含量的方法。结果 薄荷脑、樟脑薄层色谱斑点清晰,可用于鉴别;醋酸氯己定在10.01~160.14 μg/ml范围内线性关系良好,平均回收率为101.5%,RSD为1.8%;盐酸丁卡因在10.01~160.14 μg/ml范围内线性关系良好,平均回收率为100.5%,RSD为2.8%。结论 提高后的质量标准可行。     

香苏胃痛胶囊质量标准研究

目的 建立香苏胃痛胶囊的质量标准。方法 采用薄层色谱（TLC）法定性鉴别处方中甘草、延胡索、茯苓、香附;采用HPLC法测定延胡索乙素的含量。色谱柱为Welchrom C₁₈（4.6 mm×250 mm,5 μm）;以乙腈-0.1%磷酸（三乙胺调pH 6.0）（40∶60）为流动相;检测波长为280 nm;柱温：30℃;流速：1 ml/min。结果 薄层定性鉴别斑点清晰,分离效果良好,专属性强;延胡索乙素在1~80 μg/ml范围内与峰面积呈良好的线性关系（r=0.999 9）。平均加样回收率为99.1%,RSD为1.28%（n=6）。结论 本方法结果准确、操作简单,专属性和重复性良好,可作为该制剂的质量控制标准。     

芪黄扶正颗粒的质量控制方法研究

目的 建立芪黄扶正颗粒的质量控制方法。方法 采用TLC法对方中黄芪、熟地黄、山茱萸、当归、川芎、赤芍、牡丹皮、麦门冬进行定性鉴别;采用HPLC法对臣药山茱萸中马钱苷进行含量测定。结果 建立了主要药味的TLC鉴别方法,斑点清晰,阴性无干扰;马钱苷在4.02~80.40 μg/ml范围内线性关系良好（r=0.999 9）,平均加样回收率为99.02%,RSD为0.64%（n=9）。结论 本研究建立的质量控制方法准确、可靠、专属性强,为芪黄扶正颗粒的质量控制奠定了基础。     

五虎凝胶贴膏质量标准研究

目的 建立五虎凝胶贴膏的质量标准。方法 采用薄层色谱法（TLC）对处方中白芷、当归、防风、红花、制天南星进行定性鉴别；采用HPLC同时测定处方中羟基红花黄色素A、阿魏酸、升麻素苷、5-O-甲基维斯阿米醇苷、欧前胡素、异欧前胡素的含量，色谱柱为Agilent Eclipse Plus C₁₈（250 mm×4.6 mm，5μm），流动相甲醇-0.025%磷酸，梯度洗脱，流速为1.0 mL·min^-1；柱温28℃；检测波长403，300，254 nm。结果 处方中所有药味薄层斑点清晰，分离度好，阴性无干扰；6种化合物在各自的范围内线性关系良好（r ≥ 0.999 5），平均加样回收率96.30%~100.56%，RSD为1.06%~1.65%。结论 建立的TLC鉴别方法专属性强、分离度好；HPLC测定方法准确稳定、重复性好，可用于五虎凝胶贴膏的质量控制。     

景天止痛膏质量标准研究

目的 修订景天止痛膏质量标准中的测定方法。方法 采用薄层色谱法（TLC）对当归、川芎、元胡、三七总皂苷进行定性鉴别,应用高效液相色谱法（HPLC）测定制剂中三七皂苷R₁、人参皂苷Rg₁、人参皂苷Rb₁的含量。结果 TLC法鉴别专属性强,分离度好;三七皂苷R₁在0.1604～2.0050μg (r=0.999)、人参皂苷Rg₁在0.8003～10.0035μg (r=1.000)、人参皂苷Rb₁在0.6182～7.7275μg (r=1.000) 范围内呈良好的线性关系,加样回收率分别为101. 43% 、98.75% 、100. 95% ,相对标准偏差（RSD）分别为2.56% 、2.71% 、2.75%。结论 本方法准确可靠、灵敏度高,可用于景天止痛膏的质量控制。     

乌金胶囊的质量标准研究

目的 建立乌金胶囊的质量控制方法。方法 采用薄层色谱（TLC）法对乌金胶囊中的臣药郁金和使药山楂进行定性鉴别;采用高效液相色谱-蒸发光散射检测（HPLC-ELSD）法测定乌金胶囊中通关藤苷H的含量,色谱柱：Waters Xbridge C₁₈柱（100 mm×3.0 mm,3.5 μm）,柱温：35 ℃,流动相为水-乙腈（50：50）,等度洗脱;流速为0.8 ml/min;采用ELSD检测器进行检测,蒸发器温度：35 ℃,雾化器温度：60 ℃,氮气流速：1.50 L/min,运行时间：5 min。结果 TLC法鉴别郁金、山楂,色谱斑点清晰,阴性样品无干扰;通关藤苷H出峰时间为2.98 min,且在11.60~580.00 μg/ml范围内线性关系良好（r=0.999 0）,加样回收率为101.54%。结论 本实验建立的TLC法鉴别郁金、山楂,操作步骤简单;建立的HPLC-ELSD联用方法专属性强,灵敏度高,重复性好,可作为乌金胶囊质量控制的方法。     

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.     

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.