正交设计优化枳实中3种二氢黄酮苷的提取工艺

目的优化枳实中柚皮苷、新橙皮苷、橙皮苷的提取工艺。方法采用L9(34)正交试验,以柚皮苷、新橙皮苷、橙皮苷的含量为评价指标,以乙醇浓度、提取时间、提取次数、乙醇用量为考察因素。优化枳实的提取工艺。结果最佳提取工艺即用8倍量50%乙醇提取1次,每次1.5 h。应用此工艺可得到最大量的柚皮苷、橙皮苷、新橙皮苷。结论本试验方法快捷简单,重复性好;优化得到的工艺稳定可行。     

响应面分析法优化通宣理肺口服液中3种有效成分提取工艺

目的采用响应面法优化通宣理肺口服液中柚皮苷、橙皮苷和黄芩苷的提取工艺。方法采用Box–Behnken设计试验,结合振荡提取法,在单因素试验的基础上,研究甲醇浓度、提取时间、提取温度对3种有效成分提取量的影响。结果获得的最佳工艺条件为:甲醇浓度为70%,提取时间为32 min,提取温度为36℃。经验证试验,柚皮苷、橙皮苷和黄芩苷的提取量分别为2.266、0.8367和0.1612 mg·m L-1。结论采用响应面分析优化通宣理肺口服液中3种有效成分的提取工艺准确可靠,可为生产实际提供依据。     

正交试验法优选舒尔颗粒的水提工艺

目的 优化舒尔颗粒的水提工艺。方法 采用高效液相色谱法测定盐酸小檗碱、柚皮苷的含量,以盐酸小檗碱、柚皮苷的转移率以及浸膏得率为综合考察指标,采用正交试验考察加水量、提取时间、提取次数的影响,优化舒尔颗粒的最佳水提工艺并进行验证试验。结果 最佳提取工艺为,加10倍量水,每次提取1 h,提取3次。验证试验显示,盐酸小檗碱转移率、柚皮苷转移率以及浸膏得率的RSD均<2%(n=3)。结论 通过正交试验优选的提取工艺稳定可行,为舒尔颗粒大生产提供依据。     

麻杏咳喘颗粒的水提工艺优化

目的 优选麻杏咳喘颗粒的水提工艺。方法 以药效成分盐酸麻黄碱、岩白菜素、升麻素苷、5-O-甲基维斯阿米醇苷、柚皮苷、橙皮苷含量及出膏率为考察指标，采用层次分析（AHP）-熵权法确定各指标权重，并计算综合评分作为响应值，在单因素实验的基础上采用Box-Behnken响应面法对各指标进行考察，优选麻杏咳喘颗粒的最佳水提工艺，并进行工艺验证。结果 优选出麻杏咳喘颗粒的最佳水提工艺为浸泡时间40 min，加水量8倍，总提取时间180 min。经3次验证实验结果显示，综合评分为94.82分（RSD=0.96%,n=3），与预测值94.64分差异较小。结论 优化后的麻杏咳喘颗粒水提工艺稳定可靠，可为该制剂的进一步开发提供参考。     

养阴清胃口服液水提工艺的研究

目的 :优选养阴清胃口服液的水提工艺。方法 :考察提取时间对挥发油提取的影响 ;采用正交试验 ,以浸出物重量和芍药苷含量为指标考察水提工艺条件。结果与结论 :养阴清胃口服液的最佳水提工艺为处方药材煎煮前浸泡30min ,然后对防风和藿香先提取挥发油2h ,再将药渣同其它药材共同煎煮 ;加8倍药材量的水提取3次 ,每次1 .5h。     

正交试验法优选骨痛胶囊的提取工艺

目的对骨痛胶囊的提取工艺进行优化。方法采用L9(34)正交设计,以复方骨痛胶囊的浸膏得率和君药骨碎补有效成分柚皮苷含量为考察指标,考察药材粒径、加水量、提取时间、提取次数4个因素对提取的影响。结果最佳提取工艺是以原药材饮片,水提3次,分别为1.5,1,0.5 h,加水量依次为12,10,8倍。结论该工艺重复性好,成品质量稳定且柚皮苷含量高,对进一步工艺开发有较好的参考价值。     

感冒口服液制备工艺研究

目的确定感冒口服液的最佳制备工艺条件。方法通过考察提油时间及收油率，筛选出挥发油的最佳提取条件；以绿原酸的含量和浸膏得率为指标，采用正交试验法考察水提工艺条件；以绿原酸的含量为考核指标考察感冒口服液醇沉、水沉的最佳工艺条件。结果最佳工艺条件为煎煮2次，每次1h，加水量为10倍，醇沉浓度为60％，水沉时药液量：加水量为1：1。结论该试验结果可靠，筛选出的最佳工艺条件适合批量生产。     

正交设计优选银屑片的提取工艺

目的:研究银屑片的最佳水提工艺。方法:采用正交试验,以溶剂量、提取时间、提取次数和浸泡时间4个因素,每个因素选取3个水平进行试验,以栀子苷含量和浸膏得率为综合考察指标。结果:采用溶剂量为8倍,提取3次,回流时间2 h,不浸泡为最佳提取工艺。结论:该制备工艺合理、可行。     

利胆消炎颗粒提取工艺的实验研究

目的 优选利胆消炎颗粒的最佳提取工艺.方法 醇提取工艺以出膏率和大黄素为考察指标,水提取工艺以出膏率和黄芩苷含量为考察指标,分别采用正交设计法对其提取工艺条件进行优选.结果 利胆消炎颗粒醇提最佳工艺条件:加10倍量60%乙醇,回流提取2次,每次2 h;水提最佳工艺条件:加10倍量水,煎煮3次,每次2 h.结论 优选出的提取条件科学合理,适合工业化生产.     

正交试验优选枳实中柚皮苷的提取工艺

目的:优选枳实中柚皮苷的提取工艺。方法:采用单因素试验考察提取溶剂及溶剂浓度对枳实中柚皮苷转移率的影响。以溶剂用量、提取次数、提取时间为考察因素,以柚皮苷转移率为评价指标,采用L9(34)正交试验优选提取工艺。结果:最佳提取工艺为6倍量的70%乙醇提取3次,每次30 min。结论:该工艺稳定,提取率高,可供大规模工业化生产参考。     

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.     

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.