高效液相色谱法测定复方金银花颗粒中绿原酸和黄芩苷含量

目的：采用高效液相色谱法测定复方金银花颗粒中绿原酸和黄芩苷的含量。方法：色谱柱为Zorbax SB—C18（250mm×4．6mm，5μm），流动相为含1％乙酸的水-甲醇梯度洗脱，检测波长为280nm；柱温为25℃。结果：绿原酸在0．0465～0、2324μg范围内线性关系良好（r=0．9998），平均加样回收率为100．6％，RSD为0．6％；黄芩苷在0．2505～1．2525μg范围内线性关系良好（r=0．9995），平均加样回收率为100．1％，RSD为1．1％。结论：该方法简便、准确、重现性好，可作为复方金银花颗粒含量控制方法。     

复方羊角颗粒质量标准研究

目的建立复方羊角颗粒的质量标准。方法用薄层色谱法对复方羊角颗粒中的白芷和川芎进行定性鉴别；用高效液相色谱法对制荆中的欧前胡素进行含量测定。色谱柱为Kromasil C18柱（250mm×4．6mm，5μm），流动相为甲醇-水（70：30），检测波长为300nm，流速为1．00mL／min。结果薄层色谱斑点清晰，易于识别；欧前胡素进样量在0，0988-1．976μg范围内与峰面积线性关系良好，r=0．9999；平均加样回收率为98．8％，RSD为0．44％，结论该方法简便快速、准确，重现性好，可有效控制复方羊角颗粒的质量。     

高效液相色谱法同时测定复方防己颗粒中粉防己碱和防己诺林碱的含量

目的：研究一种能同时准确测定复方防己颗粒中的粉防己碱和防己诺林碱的方法。方法：采用高效液相色谱法测定粉防己碱和防己诺林碱的含量；色谱柱ZorbaxsbCl。柱；流动相为甲醇-乙腈-0．002moL·L^-1。“磷酸二氢钾-乙二胺（55：25：20：0．06），流速1．0mL·min，柱温为室温，检测波长为230nm，进样量为20μL,结果：本法可以准确测定复方防己颗粒中的粉防己碱和防己诺林碱，精密度、回收率、稳定性均符合要求。结论：该方法能同时测定复方防己颗粒中的粉防己碱和防己诺林碱的含量，方法简单、快速、灵敏度高，可用于复方防己颗粒的质量控制。     

妇灵颗粒质量标准的研究

目的建立妇灵颗粒的质量标准。方法采用薄层色谱法对妇灵颗粒中木香、白术、黄柏、苦参进行定性鉴别；并应用高效液相色谱法测定芍药苷的含量。色谱柱：Kromasil（4．6mm×250mn，5μm）；流动相为甲醇-0．05mol／L磷酸二氢钾溶液（40：60）；检测波长为230nm；流速：0．8ml／min；柱温：35℃。结果芍药苷在1．06-10．60μg范围内呈良好的线性关系，r=0．9999，平均回收率为98．67％，RSD=1．42％（n=6）。结论该方法简便、准确、可靠，可作为妇灵颗粒的的质量控制方法。     

高效液相色谱法测定复方羊角颗粒中欧前胡素的含量

目的建立复方羊角颗粒中欧前胡素的含量测定方法。方法采用高效液相色谱法。色谱柱为Diamonsil C18柱（200mm×4．6mm,5μm）;流动相为甲醇-水（65：35）;检测波长为248mm;流速为1．00mL·min^-1。结果欧前胡素进样量在0．0106～0．0954μg与其峰面积值呈良好的线性关系（r=0．9998）,平均加样回收率为99．1％。RSD为0．8％。结论该方法操作简便,结果准确可靠,可用于复方羊角颗粒的质量控制。     

HPLC法测定丹芩颗粒中黄芩苷和丹酚酸B的含量

目的：建立高效液相色谱法测定丹芩颗粒中黄芩苷和丹酚酸B的含量。方法：采用Dionex高效液相色谱仪，色谱柱为Diomand C18柱（200mm×4．6mm，5μm）；测定黄芩苷的流动相为甲醇-水-磷酸（43：57：0．2），检测波长为280nm；测定丹酚酸B的流动相为甲醇-乙腈-水-甲酸（27：8：63：2），检测波长为286nm；流速为1．0mL·min^-1；柱温30℃。结果：在测定条件下，黄芩苷和丹酚酸B的浓度分别在15．0—90．2μg·mL^-1（r=0．9998）和48．7～207μg·mL^-1（r=0．9999）范围内线性关系良好；方法回收率（n=6）分别为98．3％（RSD=1．4％）和97．1％（RSD=1．2％）。结论：本方法操作简便，准确度高，专属性强，适用于丹芩颗粒的质量控制。     

复方柳菊片的质量标准研究

目的建立复方柳菊片的质量标准。方法用薄层色谱（TLC）法对旱柳叶进行定性鉴别；用高效液相色谱（HPLc）法测定复方柳菊片的绿原酸含量，选用Agilent Hypersil C18色谱柱，流动相为乙腈-0．1％磷酸（12：88），检测波长327nm。结果TLC检出了旱柳叶的特征斑点；绿原酸进样量在0．077～1．93μg范围内与峰面积线性关系良好（r=0．9999），平均加样回收率为99．63％．RSD=1．60％（n=6）。结论所用方法简便、稳定、可靠，可作为复方柳菊片的质量控制方法。     

HPLC法测定小儿康颗粒中芍药苷的含量

建立HPLC法测定小儿康颗粒中芍药苷的含量。采用Phenomenex Luna C18色谱柱，以乙腈-0．1％磷酸（13：87）为流动相，流速：lmL·min^-1检测波长：230nm。芍药苷在21．48-107．4μg·mL。范围内线性关系良好，r=0．9996；加样回收率为100．0％。RSD=1．3％（n=6）。方法简便可行、准确，能有效控制小儿康颗粒质量。     

气相色谱法测定复方冰片搽剂中冰片、薄荷脑和樟脑的含量

目的：建立复方冰片搽剂中冰片、薄荷脑和樟脑的含量测定方法。方法：采用气相色谱法，色谱柱：10％PEG-30M石英毛细管色谱柱；柱温：150℃；进样口温度250℃；程序升温；FID检测器。结果：冰片、樟脑和薄荷脑平均回收率分别为：99．6％（RSD为0．8％）、99．8％（RSD为0．9％）、98．5％（RSD为1．0％）。结论：本法简便准确灵敏，可用于本品的质量控制。     

高效液相色谱法测定复方清肝胶囊中栀子苷含量

目的用高效液相色谱（HPLC）法测定复方清肝胶囊的栀子苷含量方法。方法采用C18色谱柱，流动相为乙腈-水（15：85），流速为1．0mL／min，检测波长238nm。结果进样量与峰面积的线性范围为0．18-0．42μg,r=0．9999；平均回收率为97．95％，RSD=0．9％（n=9）。结论HPLC法能有效控制复方清肝胶囊的质量，操作简单、结果准确、灵敏度高。     

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.

---

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.