HPLC法测定川芎-当归药对中酚酸类成分的含量

摘 要 目的： 测定川芎 当归药对水提液中酚类物质含量。方法: 采用离子抑制高效液相色谱法测定川芎 当归药对水提液中阿魏酸、原儿茶酸和绿原酸含量。结果: 川芎 当归药对中原儿茶酸、阿魏酸和绿原酸分别在0.90～14.40,1.25～20.00,1.00～16.00 μg·mL^-1范围内与峰面积呈良好线性关系;平均回收率分别为97.16%、94.98%、98.14%(n=9)。结论:离子抑制高效液相色谱法方法简便、准确、快速、重复性好,可用于川芎 当归药对酚类物质的质量控制。     

大鼠左旋多巴给药后纹状体高香草酸水平变化

目的:探讨左旋多巴给药后大鼠纹状体细胞外液高香草酸浓度随时间变化规律。方法:大鼠单次灌胃给予左旋多巴48mg.kg-1和苄丝肼12mg.kg-1后,采用脑微透析活体取样和高效液相色谱技术,测定给药后6h内不同时间点大鼠纹状体细胞外液高香草酸和左旋多巴浓度。结果:左旋多巴+苄丝肼给药后大鼠纹状体细胞外液高香草酸水平升高明显迟于左旋多巴,显示左旋多巴代谢为高香草酸需一定时间;左旋多巴水平在给药4h后基本恢复到基础水平,而高香草酸水平给药6h后仍远高于给药前水平。结论:大鼠如以左旋多巴48mg.kg-1和苄丝肼12mg.kg-1每6h一次给药,高香草酸水平可能存在蓄积现象,其临床意义有待进一步研究。     

正交试验法优选金铃子颗粒提取工艺

摘 要 目的：：优选金铃子颗粒的提取工艺。 方法: 用正交试验法考察加水量、煎煮时间、煎煮次数等因素对提取工艺的影响,以干浸膏得率和延胡索乙素含量为考察指标,烘干法测定干浸膏得率,高效液相色谱法测定延胡索乙素含量。 结果: 加10倍量水,煎煮1 h,煎煮 3 次为最佳提取工艺。 结论: 优选的工艺合理可行、重复性良好、提取效率高,适合于工业化生产。     

联苯苄唑栓剂制备工艺与质量评价研究

摘 要 目的：优选联苯苄唑栓剂的制剂工艺,并评价其质量。方法: 以栓剂外观、硬度、融变时限等为评价指标,优化栓剂的基质、药物粒度、注模温度、搅拌条件等工艺条件,并采用HPLC法测定联苯苄唑含量。结果: 优选出的最佳处方组成为：混合脂肪酸甘油酯 36为基质,联苯苄唑过100目筛,最佳成型温度为 45℃。用以上方法制备的栓剂,其性状、融变时限、硬度、含量测定等质量可控。结论: 该栓剂处方设计合理,制备工艺合理可行,质量控制方法可靠。     

多指标评价不同加工方法对湖北野生川党参质量的影响

摘 要 目的： 采用多指标评价不同产地加工方法对竹山当地野生党参质量的影响。方法: 采用正交设计试验,以干膏得率、党参炔苷含量、党参多糖含量为指标筛选最佳工艺,采用高效液相色谱法测定党参炔苷和党参多糖的含量。结果: 采用循环干燥控制温度 70℃充分烘干,揉搓1次的加工方法最佳。结论: 本试验优选的加工方法简单实用,比较有推广价值。     

HPLC测定鸡血藤片中原儿茶酸的含量

摘 要 目的:建立鸡血藤片中原儿茶酸含量的高效液相色谱法。方法: 采用Inertsil C₁₈（250 mm×4.6 mm 5 μm）色谱柱,以甲醇∶水∶冰醋酸（25∶75∶0.2）为流动相,检测波长为260 nm,流速为0.8ml·min^-1。结果:原儿茶酸进样量在0.010～0.063 μg范围内与峰面积线性关系良好,r=0.999 4（n=6）。方法平均回收率为99.23%,RSD为0.35%。结论:高效液相色谱法简便、灵敏、稳定、准确,无其他成分干扰,可作为鸡血藤片质量控制的有效方法。     

妇洁洗液质量标准的建立

摘 要 目的： 对妇洁洗液的质量标准进行研究。方法: 采用薄层色谱法对处方中主药苦豆子、蛇床子、冰片进行定性鉴别,采用高效液相色谱法对苦豆子中苦参碱的含量进行定量测定。结果: TLC色谱斑点清晰,阴性样品无干扰,鉴别法专属性强;HPLC测定苦参碱在0.013 0~1.300 0mg·mL^-1范围内呈良好线性关系,平均回收率为97.1 %, RSD为1.7%（n=6）。结论:该方法准确、重复性好,可有效控制妇洁洗液的质量。     

糖肝煎浓缩丸水提部分的提取工艺研究

摘 要 目的：优选糖肝煎浓缩丸水提部分的提取工艺参数。方法: 以芍药苷含量和浸膏得率作为评价指标, 芍药苷含量采用高效液相色谱法,色谱条件：色谱柱:WondaSil C₁₈柱(250 mm×4.6 mm,5 μm);流动相：乙腈-0.15%磷酸溶液(16∶84);流速：1.0 ml·min^-1;柱温:30℃;检测波长：230 nm。以加水量、煎煮时间和煎煮次数作为考察因素,采用正交设计法进行方差分析优选水提取工艺参数。 结果: 优选的提取工艺为加12倍量水,提取3次,每次1 h。结论:优选的提取工艺合理、稳定、可行,为糖肝煎浓缩丸提取工艺提供了试验依据。     

苄丝肼对大鼠纹状体细胞外液左旋多巴药动学的影响

目的探讨苄丝肼对左旋多巴大鼠纹状体细胞外液药动学影响。方法大鼠随机分3组（每组7只）：左旋多巴合并苄丝肼组,大鼠灌胃给予左旋多巴48mg·kg^-1和苄丝肼12mg·kg^-1;单用左旋多巴组,大鼠灌胃给予左旋多巴48mg·kg^-1;生理盐水对照组,大鼠灌胃给予等体积生理盐水。采用脑微透析活体取样和高效液相色谱技术,测定给药后6h内不同时间点大鼠血浆和纹状体细胞外液左旋多巴浓度,应用3P87药动学程序拟合药动学参数。结果左旋多巴在血浆及纹状体细胞外液药-时曲线符合一室模型。单用左旋多巴在纹状体细胞外液t1/2、tmax、ρmax和AUC0→∞分别为（21．55±13．74）min、（46．82±27．49）min、（9．283±2．130）μg·L^-1、（2762±1257）μg·L^-1;左旋多巴合用苄丝肼组纹状体细胞外液t1/2、tmax、ρmax和AUC0→∞分别为（83．50±10．24）min、（49．97±11．72）min、（119．62±81．12）μg·L^-1、（18431±9115）μg·L^-1。其中,除tmax外,单用左旋多巴组t1/2、ρmax和AUC0→∞均显著小于左旋多巴合用苄丝肼组（P〈0．01）。结论苄丝肼可显著提高左旋多巴进入纹状体药量。     

HPLC测定硝酸甘油片的含量及含量均匀度

目的:测定硝酸甘油片的含量及含量均匀度。方法:高效液相色谱法,以外标法定量。甲醇-水(60:40)为流动相。结果:加样回收率为100.0%, RSD为0.067%(n=12);模拟片回收率为99.9%, RSD为0.18(n=13)。结论:方法简便、快捷、准确,可作为含量及含量均匀度的检测方法。     

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.     

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.     

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.