薄层扫描法测定利脑心胶囊中芍药甙的含量

应用ＴＬＣＳ法测定利脑心胶囊中芍药甙含量．样品用甲醇提取、大孔吸附树脂分离芍药甙，以硅胶Ｇ为薄层吸附剂，苯－甲醇－醋酸乙酯－氨水（１０：４：２：０．５）为展开剂，茴香醛－冰醋酸－硫酸（０．１：１０：０．２）溶液为显色剂，用ＣＳ－９３０薄层扫描仪，在λｓ＝５５５ｎｍ，λＲ＝６７０ｎｍ波长处测定含量。本法平均加样回收率为１００．５％，ＲＳＤ为３．７６％（ｎ＝５）。     

薄层扫描法测定黄芪生脉颗粒中黄芪甲甙含量

目的：制订黄芪生脉颗粒中黄芪甲甙含量测定方法。方法：双波长薄层扫描法，经乙酰洗涤、正丁醇提取和Ｄ１０１大乳吸附树脂柱层析法制备样品，以氯仿－甲醇－水（１３：７：２）下层液为展开剂，检测波长为５１０ｎｍ，参比波长为７００ｎｍ。结果：加标回收率平均为９８．７％（ＲＳＤ＝２．０％，ｎ＝６），标准曲线ｒ＝０．９９６６，重复性ＲＳＤ＝１．４％（ｎ＝５），精密度ＲＳＤ＝２．０％（ｎ＝６）。结论：方法稳定、可靠     

薄层扫描法测定元胡止痛片中延胡索乙素的含量

目的：制定元胡止痛片中延胡索乙素含量测定方法。方法：双波长薄层扫描法,以苯－石油醚（９０～１２０℃）－甲醇－三氯甲烷（３：３：０．５：１０）为展开剂,检测波长３４０ｎｍ,参比波长３６５ｎｍ。结果：回收率平均为９７．６％（ＲＳＤ＝１．７９％,ｎ＝５）。标准曲线ｒ＝０．９９９８,线性范围０．２～１．２ｕｇｊ。结论：本方法简便,准确,可作为元胡止痛片的质量标准。     

薄层扫描法测定蒙成药地格达——4汤中栀子甙的含量

用薄层扫描法对蒙成药地格达－４汤中栀子甙的含量进行了测定，λＳ＝２４０ｎｍ，λＲ＝３１０ｎｍ。方法简单，结果准确，精密。平均回收率为９８．６％，ＲＳＤ为１．２０％（ｎ＝６）。     

双波长薄层扫描法测定异麻匹林片中咖啡因和盐酸伪麻黄碱含量

目的 测定异麻匹林片中咖啡因和盐酸伪麻黄碱的含量。方法 双波长薄层扫描,咖啡因的测定波长λｓ＝２７０ｎｍ,λＲ＝３５０ｎｍ,盐酸伪麻黄碱的λｓ＝５１０ｎｍ,λＲ＝６１０ｎｍ,展开剂为氯仿－醋酸乙酯－甲醇－氨水（１５：４：３：０．３）。结果咖啡因和盐酸伪麻黄碱的平均回经分别为９９．０％和９９．８％,ＲＳＤ分别为１．９％和０．８％。结论 该法简单、快速、结果准确,适合于该制剂的质量控制。     

薄层扫描法测定蒙成药地格达-4汤中栀子甙的含量

用薄层扫描法对蒙成药地格达－４汤中栀子甙的含量进行了测定，λｓ＝２４０ｎｍ，λＲ＝３１０ｎｍ。方法简单，结果准确、精密。平均口收率为９８．６％，ＲＳＤ为１．２０％（ｎ＝６）。     

薄层扫描法测定复方大黄洗液中大黄素含量

通过对大黄素的定性和定量的检测投篮和方大黄洗液的质量。方法：采用薄层扫描法,以大黄素为指标,测定复方大黄洗液中大黄素的含量。使用０．５％ＣＭＣ－Ｎａ硅胶Ｇ板,展开剂为正己烷－甲酸乙酯－乙酸－乙酸乙酯－氯仿－冰醋酸（１６：３：３：１：０．２）,薄层抛描条件是λｓ＝４４０ｎｍ,λｒ＝５６０ｎｍ,平均架样回收率９６．２２％,ＲＳＤ＝６．４２％（ｎ＝３）。结论用本法测定复方大黄洗液中大黄素的含量,操作简便     

高效液相色谱法梯度法脱测定三七中三七皂苷R1含量

目的：以ＨＰＬＣ梯度法脱测定三七中三七皂苷Ｒ１含量。采用Ｓｐｈｅｒｉｃｏｒｂ ＮＨ２柱,流动相为ＣＨ３ＣＮ－ＣＨ３ＯＨ－Ｈ２Ｏ,梯度洗脱浓度５５：３０：１５→７０：２０：１０,波长２１０ｎｍ,外标一点法测定。结果：以峰面积计算,三七皂苷Ｒ１在５～４０μｇ．ｍｌ＾－１呈线性相关,γ＝０．９９４,最低检测限为０．６μｇ．ｍｌ＾－１（Ｓ／Ｎ）＝３。平均回收率１０２．６％,ＲＳＤ为１．４３％,日内误差ＲＳＤ＝１．７％（ｎ＝５）,日间误差ＲＳ＝３．０％（ｎ＝４）。结论：本法专属性强,结果准确,操作简便。     

强身灵口服液中黄芪甲苷的含量测定及稳定性考察

目的：测定强身灵口服液中黄芪甲苷的含量以控制产品质量,并考察制剂的稳定性。方法：供试品以正丁醇提取,氨试液纯化,以氯仿－甲醇－水（６５∶３５∶１０）为展开剂,进行双波长薄层扫描,检测波长５３０ｎｍ,参比波长７００ｎｍ。结果：线性范围２．２～１１．０μｇ,ｒ＝０．９９９０,平均回收率９８．１１％,ＲＳＤ为１．０５％（ｎ＝５）。结论：方法简便、灵敏、专属性及重现性好,可用于产品质量控制。     

反相HPLC法测定罂粟壳中吗啡,可待因的含量

采用Ｃ１８柱,以０．０５ｍｏｌ／Ｌ醋酸钠缓冲液（ｐＨ３．６）－乙腈－乙醇（２２：２：１）为流动相,检测波长为２５４ｎｍ。吗啡、可待因与各杂质成分分离度良好。含量测定的平均回收率分别为９４．７％（ＲＳＤ＝１．４３％,ｎ＝５）;９４．６％（ＲＳＤ＝１．７３％,ｎ＝５）。     

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.