正交试验法优选三仁通便合剂提取工艺

摘 要 目的：优选三仁通便合剂的最佳提取工艺。方法: 以加水量、煎煮时间、煎煮次数为考察因素,以苦杏仁苷含量及出膏率为指标,采用L₉(3⁴)正交试验法,优选三仁通便合剂的最佳提取工艺。结果: 确定三仁通便合剂最佳提取工艺为：加水煎煮2次,每次8倍量水煎煮1.5 h。结论:本试验为三仁通便合剂的提取工艺提供了科学的试验数据支持,并通过验证性试验论证了该优选工艺的稳定可行。     

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。     

正交试验法优选芪葛颗粒的提取工艺

摘 要 目的：优化芪葛颗粒的提取工艺。方法: 建立芪葛颗粒中黄芪甲苷、葛根素2 种成分测定的HPLC 方法。采用 L9(34)正交设计,以黄芪甲苷、葛根素 2 种成分含量综合评分法进行数据分析,对芪葛颗粒的加水量、提取时间和提取次数3个因素进行优化。结果: 最佳提取工艺为：加入 12倍水,提取3次,每次 30 min。结论: 优选芪葛颗粒提取工艺能较好地保证制剂的质量。     

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。     

正交试验法优选更年安舒颗粒提取工艺

摘 要 目的： 优选更年安舒颗粒的提取工艺。方法: 采用正交试验设计法,以松果菊苷及特女贞苷含量为指标综合评价,考察加水量、提取时间、提取次数对提取工艺的影响。结果: 最佳提取工艺为加水煎煮2次,每次2 h,每次加8倍量的水。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。     

宣肺止咳颗粒的水提醇沉工艺考察

摘 要 目的：优选宣肺止咳颗粒的水提醇沉工艺。方法: 以橙皮苷量、射干苷量和干膏得率的综合评分为指标,通过正交试验,考察加水量、煎煮时间、煎煮次数对水提工艺的影响,考察相对密度、醇沉浓度、醇沉时间对醇沉工艺的影响。结果:优选的水提工艺为首次加10倍量水煎煮1.5 h,第2,3次分别加8倍量水煎煮0.5 h;优选的醇沉工艺为水提液浓缩至相对密度1.05（60 ℃）,醇沉至乙醇体积分数80%,冷处静置18 h。结论:优选的提取、 醇沉工艺稳定可行,为宣肺止咳颗粒的规范化生产提供参考。     

参芪利心胶囊的提取工艺研究

摘 要 目的：通过药效学评价结合正交试验多指标综合评分法优选参芪利心胶囊最佳提取工艺。方法: 采用腹腔注射多柔比星法建立充血性心力衰竭（CHF）模型,以CHF大鼠左室收缩末期内径（LVEDD）、左室舒张末期内径（LVESD）、短轴缩短率（FS）和左室射血分数（LVEF）为指标,筛选样品提取工艺（A工艺为药材全煎煮;B工艺为太子参细粉与其他药材煎煮后混合）。通过单因素考察并设计正交试验,以黄芪甲苷、丹参酮ⅡA含量和煎煮物重量为指标,考察加水量、煎煮次数、煎煮时间对提取工艺的影响并对其进行优化。结果: 药效学实验表明B工艺样品对CHF大鼠心脏症状及心功能改善作用更佳。该工艺中其他药材最优提取条件为每次加12倍量水煎煮1 h,共煎煮3次。验证试验结果显示黄芪甲苷、丹参酮ⅡA的平均提取率分别为61.82%、50.07%,平均煎煮物重量为6.02 g。结论:参芪利心胶囊最优的提取工艺科学合理、稳定可靠。     

正交试验优化消渴安糖方的水提取工艺

摘 要 目的：优化消渴安糖方的水提工艺。方法: 采用正交试验法,以浸膏得率和黄芪甲苷含量作为考察指标,以加水量、提取时间、提取次数为考察因素,采用正交试验优化消渴安糖方的水提取工艺并进行验证。结果: 加水量对黄芪甲苷的提取含量具显著性影响（P<0.05）,最佳水提工艺为12倍加水量,水提取3次,每次0.5 h,3次工艺验证试验中浸膏得率平均值为38.33%（RSD＝1.22%,n=3）,黄芪甲苷平均含量为0.082 8 mg·g-1（RSD=3.37%,n＝3）。结论:该优化提取工艺稳定、可行,可为消渴安糖方口服制剂的制备提供实验依据。     

小儿银翘颗粒提取工艺考察

摘 要 目的：以正交试验法确立小儿银翘颗粒的最佳提取工艺。方法: 采用正交试验法, 以连翘酯苷A、绿原酸的含量为指标, 考察了加水量、提取次数、提取时间三因素对连翘酯苷A、绿原酸的提取量的影响。结果: 小儿银翘颗粒的最佳提取工艺为以8倍量、6倍量、6倍量水煎煮三次,提取时间分别为1.5,1,1 h。结论:该提取工艺简单、合理、可行。     

和胃颗粒中槟榔碱的提取工艺优选

目的 优选和胃颗粒中槟榔碱的最佳提取工艺。方法 应用单因素试验考察药材饮片的浸泡时间及吸水率,以槟榔碱提取率和出膏率的综合评分为指标,通过正交试验考察加水量、煎煮时间、煎煮次数对和胃颗粒提取工艺的影响,并采用高效液相色谱法测定槟榔碱的含量及其溶出度。结果 和胃颗粒中槟榔碱的最佳提取工艺为加水煎煮2次,第一次加水6倍量,煎煮1 h,趁热滤过;第二次加水5倍量,煎煮1 h,趁热滤过,合并滤液。结论 该提取工艺合理、可靠,适用于和胃颗粒的工业生产。     

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.     

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.