愈伤灵胶囊中药材的鉴别及羟基红花黄色素A的测定

目的 提高愈伤灵胶囊的质量标准.方法 采用TLC法鉴别愈伤灵胶囊中的三七、当归;采用HPLC测定其中的羟基红花黄色素A.结果 TLC鉴别愈伤灵胶囊中三七、当归的色谱清晰;羟基红花黄色素A进样量0.2784～1.3920μg与峰面积有良好的线性关系(r =0.9999),平均回收率为98.9%,RSD=0.7%(n=6).结论 所建方法简单、准确、灵敏、重复性好,能有效控制愈伤灵胶囊的质量.     

七味红花殊胜丸质量标准研究

目的：建立七味红花殊胜丸质量标准。方法：采用薄层色谱法（TLC）对处方中红花进行定性鉴别;用高效液相色谱法（HPLC）测定羟基红花黄色素A含量。结果：TLC定性鉴别分离效果好,斑点显色清晰。羟基红花黄色素A的进样浓度在13.18~79.10μg·ml-1范围内与峰面积积分值呈良好线性关系（r=0.9998）;平均回收率为98.2%,RSD=1.27%（n=6）;每丸含红花以羟基红花黄色素A计应不少于1.0mg。结论：标准可用于该制剂的质量控制。     

辽源七厘散质量标准研究

目的:建立辽源七厘散的质量标准.方法:建立血竭、冰片、儿茶、骨碎补的薄层色谱鉴别,用HPLC法测定红花中羟基红花黄色素A的含量.结果:在TLC色谱中能检出血竭、冰片、几茶、骨碎补,阴性空白无干扰.HPLC法能准确的测定羟基红花黄色素A的含量,线性范围为0.113 7～1.478 1 μg(r=0.999 9),平均回收率为104%,RSD(n=6)为1.3%.结论:方法操作简单,准确可靠,重现性好,可作为辽源七厘散的质量控制方法.     

HOLC法测定肤痒颗粒中羟基红花黄色素A的含量

目的:建立肤痒颗粒的鉴别和含量测定的方法.方法:采用HPLC法测定羟基红花黄色素A的含量.结果:羟基红花黄色素A含量在0.02046～0.2046μg范围内有良好的线性关系r=0.9998,平均回收率为99.85%,RSD=0.10%n=5.结论:方法专属性强、重复性好,简便易行,可用于该制荆的质量控制.     

蝎龙接骨散质量标准研究

目的:建立蝎龙接骨散新的质量标准。方法:采用薄层色谱法(TLC)定性鉴别处方中的血竭、红花和当归;采用高效液相色谱法对羟基红花黄色素A和阿魏酸进行含量测定。用InertsilC8-3柱,乙腈-0.2%磷酸-四氢呋喃(23:75:2)为流动相,流速为1.0mL/min,检测波长为340nm。结果:TLC特征斑点明显、专属性强。羟基红花黄色素A和阿魏酸的线性范围分别为11.13～111.35μg/mL和3.42～34.2μg/mL;平均加样回收率分别为100.35%和99.43%(n=6)。结论:所建的新标准可用于蝎龙接骨散的质量控制。     

妇科灌肠液质量标准的建立

摘要：目的:建立妇科灌肠液的质量标准。方法:采用TLC法对妇科灌肠液中大血藤、紫花地丁、三棱进行定性鉴别;采用HPLC法对妇科灌肠液中羟基红花黄色素A、蒙花苷进行含量测定,色谱柱:Wondasil C18（250 mm×4.6 mm,5μm）;流动相:甲醇-乙腈-0.5%磷酸水溶液,梯度洗脱;流速:1.0 ml·min-1;检测波长:403 nm、330 nm;柱温:30℃;进样量:10μl。结果:TLC斑点清晰,分离度好,阴性对照无干扰;羟基红花黄色素A、蒙花苷分别在进样浓度40.80～204.00μg·ml-1（r=0.999 9）、60.00～300.00μg·ml-1（r=0.999 9）范围内与峰面积呈良好线性关系,平均加样回收率分别为99.56%、98.68%,RSD分别为2.25%、1.94%（n=6）。结论:该方法快速、准确、专属性强,可作为妇科灌肠液质量控制的方法。     

七味红花殊胜丸中药材的鉴定及羟基红花黄色素A的测定

建立七味红花殊胜丸的鉴别及含量测定的方法,提高质量标准.方法采用TLC法鉴别方中麻黄素、诃子和红花;采用HPLC法测定红花中的羟基红花黄色素A.采用C18柱,流动相为甲醇-乙腈- 0.7％磷酸溶液(26:2:27),检测波长403 nm.结果盐酸麻黄碱、诃子、红花的薄层色谱斑点清晰,专属性强.羟基红花黄色素A进样量0....     

通脉化瘀胶囊制备工艺及质量标准研究

目的 优选通脉化瘀胶囊制备工艺,确定质量标准。方法 单因素考察确定最优制备工艺,显微鉴别、薄层鉴别、HPLC方法含量测定以及检查项目确定质量标准。结果 以药材总量的0.56～0.60倍水为粘合剂湿法制粒后填充胶囊,通过显微鉴别可清晰看到全蝎刚毛、降香纤维、土鳖虫体壁碎片、红花花粉粒、肉桂纤维及大黄草酸钙簇晶;三七及降香药材TLC鉴别斑点清晰,专属性强,无干扰;HPLC方法测定羟基红花黄色素A含量应不低于1.0 mg/g。结论 优化的制备工艺稳定可行;全蝎、降香、土鳖虫、红花、肉桂、大黄显微鉴别特征明显易观察,三七及降香药材TLC鉴别可作为通脉化瘀胶囊定性鉴别的有效方法;HPLC方法测定羟基红花黄色素A含量可作为质量控制检测指标。     

HPLC法测定肤痒颗粒中羟基红花黄色素A的含量

目的:建立肤痒颗粒的鉴别和含量测定的方法。方法:采用HPLC法测定羟基红花黄色素A的含量。结果:羟基红花黄色素A含量在0.02046～0.2046μm范围内有良好的线性关系r=0.9998,平均回收率为99.85%,RSD= 0.10%n=5。结论:方法专属性强,重复性好,简便易行,可用于该制剂的质量控制。     

七味马钱子丸的质量标准提高研究

目的:提高七味马钱子丸的质量标准。方法:采用薄层色谱法(TLC)对制剂中诃子、木香进行定性鉴别。采用高效液相色谱法测定制剂中羟基红花黄色素A、马钱子碱和士的宁的含量,色谱柱为Phenomenex Prodigy C_(18),流动相为甲醇-乙腈-0.7%磷酸溶液(26∶2∶72,V/V/V,羟基红花黄色素A)、乙腈-0.01 mol/L庚烷磺酸钠和0.02 mol/L磷酸二氢钾等量混合溶液(以10%磷酸溶液调pH至2.8)(21∶79,V/V,马钱子碱和士的宁),流速为1.0 mL/min,检测波长为403 nm(羟基红花黄色素A)、260 nm(马钱子碱、士的宁),柱温为25℃,进样量为10μL。结果:诃子、木香的TLC图斑点清晰,分离度好,阴性对照无干扰。羟基红花黄色素A、马钱子碱和士的宁检测质量浓度线性范围分别为6.29~62.94μg/mL(r=0.999 3)、1.83~18.30μg/mL(r=0.999 4)、2.11~21.11μg/mL(r=0.999 6);精密度、稳定性、重复性试验的RSD<2.0%(n=6);加样回收率分别为101.66%~104.91%(RSD=1.14%,n=6)、99.58%~104.55%(RSD=1.75%,n=6)、101.22%~104.04%(RSD=0.99%,n=6)。结论:提高的标准可更好地用于七味马钱子丸的质量控制。     

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.     

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.     

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.