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。     

经舒宁颗粒提取纯化工艺优选

摘 要 目的:优选经舒宁颗粒的提取纯化工艺。方法: 以芍药苷的转移率和浸膏得率作为评价指标,采用正交试验对水提条件进行优选,以醇沉前后芍药苷的转移率和干膏量对醇沉条件进行考察。结果:优选出最佳的工艺条件是8倍量的水,提取3次,每次2.5 h,醇沉浓度为70%。结论:优选出的工艺稳定,可行,适合该制剂的批量生产。     

正交试验优选乳癖消颗粒中三七和玄参的提取工艺

摘 要 目的：优选乳癖消颗粒中三七和玄参的提取工艺。方法: 以人参皂苷Rg1、人参皂苷Rb1和哈巴俄苷的转移率及干膏得率为综合评价指标,通过L9（34）正交试验考察溶剂量、乙醇浓度、提取时间及提取次数对乳癖消颗粒中三七、玄参醇提工艺的影响。采用HPLC法同时测定3种指标成分的含量。结果: 最佳提取工艺为用8倍量60%的乙醇提取两次,每次2 h。人参皂苷Rg1、人参皂苷Rb1和哈巴俄苷的转移率分别为（79.48 SymbolqB@ 1.561）%, （42.62 SymbolqB@ 0.68）%和（44.89SymbolqB@ 0.58）%（n=3）,干膏得率（20.99SymbolqB@0.41）%。结论: 该优选工艺稳定可行,可用于提取乳癖消颗粒中的三七和玄参。     

伤科止痛油提取工艺的优选

摘 要 目的：优选伤科止痛油最佳提取工艺。方法: 以毛蕊花糖苷和没食子酸提取量的综合评分为指标,采用L9（34）正交试验考察乙醇浓度、浸泡时间、提取次数和提取时间对伤科止痛油的提取工艺的影响。结果:最佳提取工艺为用65%乙醇浸泡1 h后,再回流提取3次,第一次1.5 h,第二、三次1 h;毛蕊花糖苷和没食子酸提取量分别为0.870 8、0.717 8 mg·ml-1。结论:优选所得的提取工艺简单易行,科学合理。     

正交设计法优选童便炮制马钱子的工艺

摘 要 目的：优选童便炮制马钱子的工艺。方法: 通过L9(34)正交设计考察童便种类、童便用量、童便浸泡时间、烘干温度4个因素,以高效液相色谱法测定马钱子碱和士的宁含量作为考察指标,进行加权综合评分。采用方差分析对童便炮制马钱子工艺进行优选。结果:童便炮制马钱子的影响因素中浸泡时间的影响最明显,其余三因素对马钱子碱和士的宁含量无明显影响。最佳炮制工艺为A1B1C3D3。结论:童便炮制马钱子的最优工艺为选用3岁童便,3倍童便量,浸泡时间为10 d,烘干温度为90 ℃。 本方法稳定,可靠,可用于马钱子的炮制新工艺。     

四味生津颗粒的提取工艺实验研究

目的优选四味生津颗粒的最佳提取工艺。方法水提工艺及醇沉工艺都以芍药苷和甘草酸的总量为考察指标进行正交实验。结果四味生津颗粒的最佳水提工艺为:加水10倍量,煎煮3次,每次2 h;最佳醇沉工艺为:水提液浓缩至清膏相对密度为1.05,醇浓度为70%,静置24 h。结论优选出的提取工艺稳定可行。     

芪山无糖颗粒剂的提取工艺优化

摘 要 目的：研究芪山无糖颗粒的最佳提取工艺。方法: 应用L9（34）正交设计法对水提取工艺进行优选,以总黄酮、黄芩苷、盐酸小檗碱含量为指标,考察煎煮时间、煎煮次数、加水倍数对提取工艺的影响。结果: 最佳工艺条件为：加水量为10倍药材量,煎煮2次,每次1 h。结论: 优选出芪山无糖颗粒剂的最佳提取工艺,该工艺稳定可行,有效成分含量高。     

清脉颗粒醇沉工艺的正交优选

目的：优选清脉颗粒的醇沉工艺。方法：选取药液相对密度,醇沉浓度及醇沉时间为考察因素,以干浸膏得率,薯蓣皂苷元苷含量为考察指标,采用正交试验优选醇沉工艺。结果：优选的醇沉工艺为药液浓缩至相对密度1.13 - 1.18 g·;ml-1,加乙醇至乙醇体积分数为60%,醇沉24 h。结论：优选的工艺稳定可行,为清脉颗粒的临床应用提供试验依据。     

乳块散结颗粒制备工艺研究

目的 筛选乳块散结颗粒的制备工艺。方法 以丹参素转移率为指标,采用正交试验筛选乳块散结颗粒水提工艺,并考察了醇沉浓度、静置时间和制剂的赋形剂。结果 乳块散结颗粒的最佳提取工艺为药材加8倍量水提取2次,每次2 h;醇沉浓度为75%,静置时间为48 h,赋形剂为可溶性淀粉与糊精（1:1）。结论 优选的乳块散结颗粒制备工艺稳定、可行。     

星点设计-效应面法优化复方茵陈合剂的醇沉工艺

目的 采用星点设计-效应面法优化复方茵陈合剂的醇沉工艺。方法 以栀子苷含量和固形物去除率的总评归一值为指标,通过单因素实验考察药液相对密度、醇沉浓度、醇沉时间和搅拌速度对醇沉工艺的影响,结合医院制剂生产特点,通过趋势分析确定影响醇沉工艺的关键因素,最后采用星点设计-效应面法对关键因素进行进一步的研究与探讨。结果 当药液相对密度为1.07,醇沉浓度为84%、醇沉时间为8 h,搅拌速度为1762 r/min时醇沉工艺达到最优。结论 采用星点设计-效应面法优化了复方茵陈合剂的醇沉工艺,有助于进一步提升复方茵陈合剂工艺的稳定性。     

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.     

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.