复方三棱胶囊的提取工艺研究

目的优选复方三棱胶囊提取工艺的最佳条件,以保证临床用药的安全、有效。方法采用正交试验法优选了挥发油的提取,并利用B-环糊精包合技术达到了防止莪术油挥发,增大水溶性,提高生物利用度的目的,使复方三棱胶囊达到现代的制剂生产标准。结果复方三棱胶囊的质量标准符合《中国药典》一部（2005年版）标准。结论复方三棱胶囊处方合理、制备简单科学、提取工艺准确、使用安全可靠。     

复方三棱颗粒剂的制备工艺研究及其可行性考察

目的确定复方三棱颗粒剂的制备工艺。方法以正交法优选复方三棱颗粒剂的最佳提取和制剂工艺条件。结果取处方量的三棱、川芎等八味中药,加水煎煮二次,每次1h,合并煎液,静置,滤过,减压浓缩至相对密度为1.3～1.4（70℃）的清膏,加入适量的糊精及甜菊素,用3%聚维酮K30的90%乙醇溶液制成颗粒,干燥,即得。结论该制备方法简单可行,所得制剂质量稳定,可作为复方三棱颗粒剂的制备工艺。     

复方三棱胶囊的药理和毒理学研究

目的：本课题对复方三棱胶囊进行了毒理学和药理学研究,为中药复方三棱胶囊治疗不孕症提供依据。方法：建立多种动物模型,通过对醋酸所致小鼠扭体反应、角叉菜胶所致大鼠足肿胀、醋酸所致小鼠腹腔毛细血管通透性影响等试验,研究复方三棱胶囊的药理和毒理作用。结果：复方三棱胶囊具有较好的抗菌消炎镇痛作用。结论：复方三棱胶囊治疗不孕症,安全可靠,药效显著。     

复方钩藤胶囊的制备及临床应用

目的:制备复方钩藤胶囊,并验证其临床疗效.方法:采用直接粉碎成细粉及提取挥发油、水煎煮、浓缩、干燥等工艺制备胶囊,并收集临床病例.结果:治疗总有效率为91.8%.结论:本品生产操作简便,质量控制可行,疗效显著,值得推广使用.     

艾叶挥发油β-环糊精包合物口含片的制备与质量检查

目的:筛选艾叶挥发油β-环糊精包合物口含片的制备工艺。方法:用正交实验法筛选制备艾叶挥发油超分子包合物口含片所需的辅料;用对比实验确定复方艾叶油β-环糊精包合物口含片最佳处方。结果:最佳处方为:艾叶油β-环糊精包合物:葡萄糖:甘露醇:柠檬酸:淀粉糊用量64:24:2:2:34;TLC结果均显示艾叶挥发油和口含片中提取的艾叶挥发油化学成分无改变。结论:口含片所含挥发油成分无变化且光洁度、可压性和口感均较好,处方可行。     

中药复方三棱颗粒的研制及成型工艺优化

目的：制备中药复方制剂"复方三棱颗粒",并优选其提取及制备工艺。方法：采用超临界二氧化碳萃取法（supercritical CO₂ fluid extraction,SFE-CO₂）萃取三棱、川芎挥发油,通过正交试验法优选萃取工艺条件;将萃取完挥发油的药渣与其余六味药材（制大黄、黄芪、杜仲、金樱子、连翘、蒲公英）共同采用冷凝回流法提取,采用正交试验法优选提取工艺条件;提取液进一步浓缩并制备成颗粒剂。结果：SFE-CO₂萃取挥发油的最佳工艺：萃取压力为25 MPa,萃取温度为50℃,萃取时间为2 h;回流提取最佳工艺：乙醇浓度为50%（V/V）,料液比为1∶12,提取时间为1 h,提取3次;成功制备了复方三棱颗粒剂,收得率为90.80%。结论：所采用提取工艺简单合理,提取效率高,颗粒剂制备工艺可行,为复方三棱颗粒剂制备工艺的确定及生产条件的控制提供了科学的实验依据。     

脑康胶囊的制备和质量控制

目的制定脑康胶囊的制备工艺,建立脑康胶囊的质量控制方法。方法药材按处方提取挥发油、煎煮、浓缩、粉碎成粉末,装胶囊而成。用显微和薄层色谱方法鉴别方中的主要药味。结果制备工艺可行,显微和薄层色谱鉴别专属性好,方法可行。结论该工艺适用于生产,质量控制方法可行。     

脑康胶囊的制备和质量控制

目的 制定脑康胶囊的制备工艺,建立脑康胶囊的质量控制方法.方法 药材按处方提取挥发油、煎煮、浓缩、粉碎成粉末,装胶囊而成.用显微和薄层色谱方法鉴别方中的主要药味.结果 制备工艺可行,显微和薄层色谱鉴别专属性好,方法可行.结论 该工艺适用于生产,质量控制方法可行.     

探究挤出滚圆法制备中药微丸的效果

目的:对应用挤出滚圆法制备中药复方杞芪微丸的效果进行探讨和分析。方法:采用新型挤出滚圆造粒机行复方杞芪微丸制备并对不同处方微丸的体外溶出度、收率以及粉体化学性质进行考察和分析。结果:3种处方微丸质量和收率均非常理想,处方A微丸质量和收率优于处方B和处方C,随着载药量的不断上升,微丸的流动性和圆整度会出现下降,收率会相应降低。3种处方微丸1小时内溶出度均超过80%,胶囊在40min内溶出度即可达到80%,杞芪微丸具有更佳的溶解度,制剂效果更优。结论:应用挤出滚圆法制备中药复方杞芪微丸具有较高的收率和较好的质量,而且具有非常理想的体外溶出效果,值得研究和应用。     

复方补钙口服液的制备及临床疗效观察

目的:研究复方补钙口服液的制备,并观察其临床疗效。方法:确定复方补钙口服液的处方、制备工艺、质量控制,对155例患者进行临床观察。结果:处方配伍及制备工艺合理,临床观察有效率达90.32%,未见不良反应。质量可控。结论:该制剂稳定性好、处方设计合理,制备工艺简便,临床疗效满意。     

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.

---

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.     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

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.