丹七片质量标准的研究

目的建立丹七片的质量标准。方法采用薄层色谱法鉴别丹参和三七,采用高效液相色谱法同时测定三七中的人参皂苷Rg1、人参皂苷Rb1、三七皂苷R1的含量。结果薄层色谱法可检出丹参和三七;人参皂苷Rg1、人参皂苷Rb1、三七皂苷R1分别在0.964~9.64、0.995~9.95、0.245~2.45μg的范围内线性关系良好,相关系数r均为0.999;人参皂苷Rg1、人参皂苷Rb1、三七皂苷R1的平均加样回收率分别为101.3%(RSD=1.12%),97.8%(RSD=1.80%),97.5%(RSD=0.68%)。结论本方法操作简单,重现性好,结果稳定,可有效地控制丹七片的质量。     

HPLC法测定跌打片中人参皂苷Rg1和人参皂苷Rb1的含量

目的:建立高效液相色谱法测定跌打片中人参皂苷Rg1和人参皂苷Rb1的含量测定方法.方法:采用Luna C18色谱柱(250 mm×4.6 mm,5μm);柱温:35℃;流动相为乙腈-水,梯度洗脱;流速1.0 ml ·min-1;检测波长203 nm.结果:人参皂苷Rg1线性范围为0.340～5.094 μg(r=1.000 0),人参皂苷Rb1线性范围为0.303 ～0.454 μg(r=1.000 0);平均加样回收率:人参皂苷Rg1为97.17％,RSD=1.09％ (n =6),人参皂苷Rb1为102.63％,RSD=1.18％ (n =6).结论:该方法简便可靠,可用于跌打片的质量控制.     

益脑胶囊中远志及人参的质量控制方法

目的：建立益脑胶囊中远志及人参的质量控制方法。方法：采用薄层色谱法鉴别方中远志，采用高效液相色谱法测定成品中人参皂苷Rg1的含量。结果：鉴别方法专属性强，定量方法简便准确，人参皂苷含量在0．174～17．360μg范围内线性关系良好，r=0．9999，平均回收率为98．25％，RSD为2．10％。结论：本方法可有效地控制益脑胶囊中远志与人参的质量。     

消渴降糖片定性定量研究

目的 建立消渴降糖片定性定量研究方法.方法 采用薄层色谱法鉴别黄精、甜菊叶、桑椹、山药;高效液相色谱法测定人参皂苷Rb1、Ro的含量.结果 薄层斑点清晰,阴性样品无干扰;人参皂苷Rb1在19.40～97.00 μg·mL-1与峰面积线性关系良好(r=0.999 6),平均加样回收率为101.5％(n=6),RSD =2.3％、人参皂苷Ro在5.98～35.88μg·mL-1与峰面积线性关系良好(r=0.999 9),平均加样回收率为103.6％ (n=6),RSD=1.7％.结论 本方法快速、简便、准确、专属性强、重现性好,可作为消渴降糖片质量控制的方法.     

丹莪妇康颗粒中人参皂苷Rg1、Rb1含量测定

目的：测定丹莪妇康颗粒中人参皂苷Rg1、Rb1的含量，为丹莪妇康颗粒的质量评价提供依据。方法：应用高效液相色谱法，采用Liehrospher C18柱，以流动相A：乙腈，流动相B：0．05％磷酸水溶液，按梯度洗脱；流速为1ml·min^-1；检测波长为203nm。柱温：室温。结果：人参皂苷Rg1、Rb1分别在5．22—104．40μg·ml^-1，5．10～102．00μg·ml^-1范围内呈良好线性关系．平均回收率分别为96．92％（RSD=0．90％），99．19％（RSD=1．26％）。结论：本法可用于该制剂的质量控制。     

高效液相色谱法测定珍黄片的含量

目的：建立高效液相色谱法测定珍黄片的含量。方法：采用高效液相色谱法对制剂中人参皂苷Rg1、人参皂苷Rb1和三七皂苷R1的含量进行测定。结果：人参皂苷Rg1、人参皂苷Rb1和三七皂苷R1的线性范围分别为1．144～11．440μg（r=0．9999）、0．948～9．480μg（r=0．9999）和0．434-4．340μg（r=0．9998）,平均回收率分别为96．46％（RSD=1．01％）、98．17％（RSD=1．02％）和96．27％（RSD=1．16％）。结论：该方法简便、灵敏、准确,适用于珍黄片的含量测定。     

七宁胶囊主药鉴定检测方法研究

目的：控制七宁胶囊制剂质量，建立三七叶、地不容、三分三的质控标准。方法：用薄层色谱法对七宁胶囊中主要药材三七叶、地不容进行定性鉴别，对毒性药材三分三中硫酸阿托品的量进行限量检查，用高效液相色谱法测定七宁胶囊中人参皂苷Rb1的含量。结果：人参皂苷Rb1含量测定的线性范围为1－30μg/mL，平均回收率为98．10％，RSD为1．31％。结论：方法简便、实用，测定结果重现性好，可作为七宁胶囊的质量控制方法。     

浮小麦质量控制探讨

目的：修订完善舒胸胶囊原标准中鉴别及含量测定方法。方法：采用薄层色谱法鉴别三七、红花及高效液相色谱法测定三七中人参皂苷Rg1,Rb1和三七皂苷R。的总量。结果：三七、红花薄层斑点清晰;人参皂苷Rg1,Rb1,三七皂苷R1分别在0．442～11．050μg（r=0．9998）、0．344-8．600μg（r=0．9999）、0．208-5．200μg（r=0．9994）范围内线性关系良好,平均回收率分别为98．97％（RSD为1．4％）、99．57％（RSD为1．8％）、98．58％（RSD为2．2％）。结论：所建方法简便、准确,可用于舒胸胶囊的质量控制。     

六味参苓颗粒的质量标准研究

目的:建立六味参苓颗粒的质量控制方法。方法:采用薄层色谱(TLC)法对处方中西洋参、黄芪、麦冬、茯苓、枳壳进行定性鉴别;采用高效液相色谱法测定西洋参中人参皂苷Rb1的含量。结果:TLC专属性强,阴性对照无干扰;人参皂苷Rb1的浓度在26.4～792.0μg·mL-1范围内与峰面积积分值呈良好的线性关系(r=0.9997),方法平均回收率为98.35%,RSD=2.09%(n=6)。结论:所建方法简便、可行,可用于六味参苓颗粒的质量控制。     

HPLC法测定田七痛经散中三七皂苷R1、人参皂苷Rg1、Rb1的含量

目的：建立液相色谱法测定田七痛经散中三七皂苷R1及人参皂苷Rg1、Rb1含量。方法：采用Watres Sunfire C18（250mm×4．6mm,5μm）色谱柱,乙腈-水为流动相,梯度洗脱,流速1．0ml·min^-1,检测波长203nm,柱温30℃。结果：三七皂苷R1线性范围为0．21—2．1μg（r=0．9999）,平均加样回收率为98．8％,RSD为1．51％（n=6）;人参皂苷Rg1线性范围为0．78—7．18μg（r=0．9999）,平均加样回收率为99．9％,RSD为1．92％（n=6）;人参皂苷Rb1线性范围为0．81—8．10μg（r=0．9998）,平均加样回收率为98．8％,RSD为1．63％（n=6）。结论：方法灵敏、准确,重复性好,可用于制剂的含量测定及质量控制。     

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.

     

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.