尿石通颗粒质量标准的研究

目的 :建立尿石通颗粒的质量控制方法。方法 :用薄层色谱法对尿石通颗粒中的连钱草进行定性鉴别 ;以芦丁为对照品 ,采用分光光度法法测定颗粒中总黄酮 (以芦丁计 )含量。结果 :薄层色谱中斑点清晰 ,易于识别 ;分光光度法重复性好 ,总黄酮在 8.7～ 6 9.6 μg·ml-1浓度范围内呈线性关系 ,r =0 .9999,平均加样回收率 97.5 % (n =5 ) ,RSD =2 .8%。结论 :本法可有效地控制尿石通颗粒的质量。     

UV法测定排石颗粒含量的不确定度评定

目的:建立紫外分光光度法测定排石颗粒中总黄酮含量的不确定度评定方法,找出影响不确定度的因素.方法:采用紫外分光光度法测定总黄酮的含量,并依据《测量不确定度评定与表示》(JJF 1059-1999)中有关规定评估其不确定度.结果:扩展不确定度为7.99％,含量测定结果可表示为(9.94±0.79)mg·g-1.结论:紫外测定总黄酮含量的不确定度主要由标准曲线的拟合、对照品与样品的配制和稀释引入.     

肾石通颗粒质量标准研究

目的制定肾石通颗粒质量控制方法。方法采用TLC法对方中的扁艹蓄、牛膝进行定性鉴别;采用比色法对方中金钱草的总黄酮进行含量测定。结果本品定性鉴别薄层色谱特征明显,专属性强;总黄酮在0.008~0.048g·L-1,范围内具有良好的线性关系(r=0.9996),平均回收率为101.31%。结论该方法可以准确地进行定性、定量检测,有效地控制肾石通颗粒的质量。     

银冬颗粒中总黄酮含量的测定

目的:建立紫外分光光度法测定银冬颗粒中总黄酮含量的方法.方法:紫外分光光度法测定总黄酮的含量,检测波长为510 nm.结果:总黄酮的检测浓度在6.45～51.6μg· mL-1范围内与吸光度呈良好线性关系(r=0.9997);平均回收率为99.85％,RSD=2.35％ (n=5).结论:该方法的精密度,重复性,稳定性,加样回收率良好,能用于银冬颗粒的质量控制.     

基于信息熵理论优选尿石颗粒的提取工艺研究

目的应用信息熵理论优选尿石颗粒的提取工艺。方法以总黄酮含量、栀子苷含量和浸膏得率为综合评分指标,运用信息熵理论确定各指标的权重系数,通过正交试验考察影响因素提取次数、提取时间和加水量,优化提取工艺。结果最佳提取工艺条件为加10倍量水提取3次,每次1 h。结论该方法稳定可行,可用于尿石颗粒提取工艺的优选。     

石淋通颗粒质量标准的研究

目的制定石淋通颗粒的质量标准。方法对处方中的广金钱草进行了薄层鉴别。用紫外分光光度法测定了制剂中总黄酮的含量。检测波长为274nm。结果薄层鉴别方法专属性强,含量测定通过方法学考察,总黄酮以芦丁计在0.050125mg~0.30075mg范围内,呈良好的线性关系。芦丁的平均回收率为99.40%(n=9),RSD为0.93%。结论方法简便、准确、重现性好。可用于控制石淋通颗粒质量。     

通脉颗粒中葛根素和总黄酮含量的测定

目的：建立通脉颗粒中葛根素及总黄酮含量的测定方法。方法：采用高效液相色谱法和紫外分光光度法对三个批号的通脉颗粒中葛根素及总黄酮的含量进行测定。结果：葛根素的含量分别为7．36±0．70％,9．68±0．27％,8．45±0．56％,总黄酮的含量分别为15．41±1．14％,20．23±0．94％,18．75±0．72％。结论：通脉颗粒中葛根素和总黄酮含量的测定方法操作简便快捷,可作为该制剂的质量控制方法。     

HPLC测定肾石通颗粒中延胡索乙素含量

目的建立HPLC法对肾石通颗粒中延胡索乙素含量测定。方法采用Shim-packODS柱(250mm×5.0mm,5μm),流动相为甲醇-0.1%磷酸溶液(三乙胺调pH值至6.0)(55∶45V/V)为流动相,流速0.8mL/min;紫外检测波长:280nm,柱温40℃。结果延胡索乙素在0.02325~0.16275μg范围内线性关系良好(r=0.9995,n=7),最低检测质量浓度0.02325μg,肾石通颗粒中延胡索乙素含量为39.0~40.6μg/g。结论该方法具有操作简便、方法可靠、稳定性好的特点,可用于肾石通颗粒中延胡索乙素含量测定及质量控制。     

分光光度法测定醒脾养儿颗粒中总黄酮的含量

目的：测定醒脾养儿颗粒中总黄酮的含量。方法：紫外一可见分光光度法测定，以芦丁为时照品，以510nm为测定波长。结果：芦丁在5～45mg·L^-1范围内线性良好，r=0．9996。回收率为98．5％，RSD为1．5％。结论：本方法快速简便、准确可靠、灵敏度高，适用于醒脾养儿颗粒中总黄酮的含量测定。     

HPLC测定肾石通颗粒中丹参素的含量

目的:建立高效液相色谱法测定肾石通颗粒中丹参素含量的方法。方法:采用Kromasil C18色谱柱,流动相为乙腈-0.1%磷酸溶液(5∶95),检测波长280nm,流速1ml/min。结果:丹参素钠在0.2936~2.936μg质量与峰面积积分值呈良好线性关系,平均回收率98.4%,RSD0.9%。结论:该法灵敏、准确,可做为肾石通颗粒的质量控制方法。     

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.

     

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.     

2-(Acetoxyphenyl)-(Z)-styryl sulfides as cyclooxygenase inhibitors

2-(Acetoxyphenyl)-(Z)-styryl sulfides are described as selective cyclooxygenase-2 (COX-2) inhibitors, useful for treating inflammation and COX-2-mediated disorders including neoplasia. 2-(Acetoxyphenyl)-(Z)-styryl sulfide is claimed to be the most potent COX inhibitor in the series with a COX-2 selectivity ratio of 33. This compound is also claimed to be superior to celecoxib (Celebrex^®, Pfizer) in inhibiting cell growth of colorectal carcinoma cells. In this evaluation, the COX inhibitory activity of this compound is compared to that previously disclosed for diarylheterocycles and 2-(acetoxyphenyl)alkyl sulfides. The validity of the DLD-1 cell line in the growth inhibition studies is questioned based on recent literature reports indicating the lack of COX-2 expression in this cell line.     

Sleep-disordered breathing with chronic opioid use

Chronic opioid use for pain relief or as substitution therapy for illicit drug abuse is prevalent in our societies. In the US, retail distribution of methadone and oxycodone has increased by 824 and 660%, respectively, between 1997 and 2003. μ-Opioids depress respiration and deaths related to illicit and non illicit chronic opioid use are not uncommon. Since 2001 there has been an emerging literature that suggests that chronic opioid use is related to central sleep apnoea of both periodic and non-periodic breathing types, and occurs in ～ 30% of these subjects. The clinical significance of these sleep-related abnormalities are unknown. This review addresses the present knowledge of control of ventilation mechanisms during wakefulness and sleep, the effects of opioids on ventilatory control mechanisms, the sleep-disordered breathing found with chronic opioid use and a discussion regarding the future research directions in this area.     

Drug targets for cognitive enhancement in neuropsychiatric disorders

The investigation of novel drug targets for treating cognitive impairments associated with neurological and psychiatric disorders remains a primary focus of study in central nervous system (CNS) research. Many promising new therapies are progressing through preclinical and clinical development, and offer the potential of improved treatment options for neurodegenerative diseases such as Alzheimer's disease (AD) as well as other disorders that have not been particularly well treated to date like the cognitive impairments associated with schizophrenia (CIAS). Among targets under investigation, cholinergic receptors have received much attention with several nicotinic agonists (α7 and α4β2) actively in clinical trials for the treatment of AD, CIAS and attention deficit hyperactivity disorder (ADHD). Both glutamatergic and serotonergic (5-HT) agonists and antagonists have profound effects on neurotransmission and improve cognitive function in preclinical experiments with animals; some of these compounds are now in proof-of-concept studies in humans. Several histamine H3 receptor antagonists are in clinical development not only for cognitive enhancement, but also for the treatment of narcolepsy and cognitive deficits due to sleep deprivation because of their expression in brain sleep centers. Compounds that dampen inhibitory tone (e.g., GABA_A α5 inverse agonists) or elevate excitatory tone (e.g., glycine transporter inhibitors) offer novel approaches for treating diseases such as schizophrenia, AD and Down syndrome. In addition to cell surface receptors, intracellular drug targets such as the phosphodiesterases (PDEs) are known to impact signaling pathways that affect long-term memory formation and working memory. Overall, there is a genuine need to treat cognitive deficits associated with many neuropsychiatric conditions as well as an increasingly aging population.