黄麦合剂中淫羊藿苷、二苯乙烯苷、金丝桃苷的稳定性考察

摘 要 目的：考察黄麦合剂中淫羊藿苷、二苯乙烯苷、金丝桃苷的稳定性。方法: 以黄芪甲苷、巴戟天药材的TLC鉴别试验,以及淫羊藿苷、二苯乙烯苷、金丝桃苷的HPLC色谱法含量测定为指标,考察黄麦合剂在加速试验及长期试验条件下的稳定性。结果: 在加速试验及长期试验条件下,黄芪甲苷、巴戟天药材以及淫羊藿苷具有良好的稳定性;二苯乙烯苷、金丝桃苷在加速试验、长期试验条件下稳定性差。结论:黄麦合剂各成分中二苯乙烯苷、金丝桃苷稳定性不佳,应尝试改造成固体剂型,以保证稳定性。     

天地精丸质量标准的建立

摘 要 目的：建立天地精丸的质量标准。方法: 显微鉴别天地精丸中的粉碎药材,采用TLC 法对天地精丸中的黄精和女贞子进行薄层鉴别;采用HPLC法测定天麻素的含量。结果: 显微方法能鉴别地龙、石菖蒲特征片断;薄层鉴别分离度好,易于识别。天麻素在19.80～158.40 μg·mL^-1浓度范围内,线性关系良好（r=1.000 0）,平均加样回收率为98.33%,RSD为0.45%（n＝6）。结论:本方法简便、重复性好,可用于天地精丸的质量控制。     

扶正抗瘤丸的质量标准

摘 要 目的： 为提高扶正抗瘤丸的质量,现进一步完善其质量控制标准。方法: 对方中虎杖、丹参、黄芪、当归和川芎5味药进行薄层色谱鉴别,同时采用高效液相色谱法对方中黄芩苷进行含量测定。结果: 薄层色谱中斑点清晰,专属性强;黄芩苷在31~310 μg·mL^-1范围内成良好的线性关系,平均回收率为101.11%（RSD=1.26%,n=9）。结论:本方法简便、准确、可靠、重现性好,可用于扶正抗瘤丸的质量控制。     

Box-Behnken响应面法优化高压蒸法炮制何首乌工艺

摘 要 目的：通过Box-Behnken响应面法优化高压蒸法炮制何首乌工艺,并与传统炮制工艺进行比较。方法: 以蒸制温度、蒸制时间和干燥温度作为考察因素,以多糖含量、二苯乙烯苷含量和两指标归一化值作为评价指标,采用Box-Behnken响应面法考察了各个因素对高压法炮制工艺何首乌中多糖和二苯乙烯苷含量的影响,并比较高压蒸法炮制品与传统炮制品中多糖和二苯乙烯苷含量的差异。结果:高压蒸法炮制何首乌的最佳工艺为：蒸制温度为125.4 ℃、蒸制时间为3.1 h、干燥温度为52 ℃。优化的高压蒸法炮制的何首乌中多糖和二苯乙烯苷含量分别为传统炮制法的1.24和5.26倍。结论:利用Box-Behnken响应面法优化高压法炮制何首乌,方法简便,预测性良好。     

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。     

生化丸质量标准的提高和优化

摘 要 目的：优化生化丸的提取工艺并建立薄层鉴别和高效液相测定有效成分的最佳方法,为定量和定性分析生化丸的质量提供有效手段和可靠依据。方法: 采用TLC法对生化丸中主要药材当归、川芎、甘草进行鉴别;采用HPLC法测定生化丸中阿魏酸的含量,色谱柱：Agilent 5 TC C18(2)（250 mm×4.6 mm,5 μm）;流动相：甲醇 5.0%冰醋酸溶液（25∶75）;检测波长：322 nm;流速：1.0 ml·min-1;柱温：室温。结果: TLC 图谱中可检出当归、川芎、甘草的特征图谱,阿魏酸质量浓度在1.28~20.51 μg·ml-1内线性关系良好,r =0.999 9;平均回收率为98.47%,RSD=0.36% (n= 6)。结论: 采用此种方法,能高效提取生化丸中有效成分,方法可行、准确、重复性好,可用于生化丸的质量控制。     

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。     

清热安宫丸质量标准研究

摘 要 目的: 研究完善清热安宫丸的质量标准。方法: 薄层色谱法鉴别制剂中的黄连、黄芩,HPLC法测定制剂中黄芩苷的含量,采用Waters C₁₈色谱柱(250 mm×4.6 mm,5 μm);流动相为甲醇-0.2%磷酸(45∶55),流速为1.0 ml·min^-1;检测波长为315 nm,柱温为30℃,进样量为10 μl。用滴定法测定朱砂的含量。结果:鉴别阴性对照均无干扰;含量测定方法中黄芩苷的线性范围为0.029～0.870 μg（r=0.999 9）,回收率为99.2%（RSD=0.67%,n=6）,朱砂的含量测定平均回收率为100.5％（RSD=0.45%,n=6）。结论:所建方法简单、可靠,可作为清热安宫丸的质量控制标准。     

Box-Behnken 设计 效应面法优化益安宁丸中尿苷和腺苷的提取工艺

摘 要 目的：采用Box-Behnken 效应面法,优选益安宁丸中尿苷和腺苷的提取工艺。 方法: 以乙甲醇浓度、提取时间、料液比为自变量,以尿苷与腺苷含量的总评“归一值”为因变量,通过对自变量各水平进行多元线性回归及二项式拟合,采用响应面法优选提取工艺,并进行预测分析。 结果: 最佳提取工艺为甲醇浓度76%、提取时间45 min、料液比为2 ml∶43 ml;此条件下尿苷和腺苷含量理论值分别为0.309 0,0.833 0 mg·g-1。 结论: 模型预测值与实验观察值接近,表明采用Box-Behnken响应面法优化后得到的提取工艺参数可用于益安宁丸中尿苷与腺苷的提取。     

添子胶囊的质量标准的建立

摘 要 目的：建立添子胶囊的质量标准。方法: 采用薄层色谱法定性鉴别山茱萸、女贞子及何首乌;采用高效液相色谱法定量测定制剂中二苯乙烯苷的含量。色谱柱：Diamonsil Plus C18色谱柱(250 mm×4.6 mm,5 μm);流动相：乙腈 水（25 ∶〖KG-*2〗75）;检测波长为254 nm;流速：1.0 ml·min-1;进样量：10 μl,柱温：30℃。结果: 山茱萸、女贞子及何首乌与对照品及对照药材在相同位置显同样斑点,阴性对照品在相应位置不显斑点。二苯乙烯苷的线性范围21.12~105.60 μg·ml-1,r=0.999 8,平均回收率为97.95%,RSD=0.61%（n=6）。结论: 本方法简便可靠,可作为添子胶囊质量控制标准。     

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.