HPLC法测定丹枣口服液中丹参素及原儿茶醛的含量

采用HPLC法同时测定丹枣口服液中的丹参素及原儿茶醛。方法：选用Kromasil ODS C18色谱柱（200mm×4．6mm,5μm）,流动相甲醇-1％冰醋酸（12：88）,检测波长280nm,流速1．0ml·min^-1。结果：丹参素钠、原儿茶醛分别在进样量0．28～2．82μg（r=0．999 5）,0．05～0．55μg（r=0．999 9）范围内呈良好线性关系。丹参素钠、原儿茶醛平均回收率分别为100．9％（RSD=2．5％）,99．3％（RSD=2．2％,n=9）。结论：方法简便、准确,重复性好,可用于该制剂的质量控制。     

高效液相色谱法测定心可舒片中原儿茶醛的含量

目的：采用高效波相色谱法(HPLC)测定心可舒片中原儿茶醛的合量，以控制该制剂的质量。方法：以C18化学键合硅胶柱分离原儿茶醛，以甲醇—水—醋酸(10：90：1)为流动相，UV检测波长280nm测定。结果：原儿茶醛峰与其它组分峰的分离度为8．9；理论塔板数以原儿茶醛峰计算为42030；方法的平均加样回收率为98．3％(n＝5)；5次独立测定的相对偏差RSD为1．09％；原儿茶醛在0．25—2．5μg范围内浓度与吸收面积值呈良好的线性关系。结论：本法测定心可舒片中原儿茶醛的含量，结果准确，重复性好。     

HPLC测定肝得治胶囊中原儿茶醛、丹参素含量

目的 高效液相色谱法测定肝得治胶囊中原儿茶醛、丹参素的含量。方法 采用ODSC，柱（5μm，4．6mm×250mm），流动相为甲醇-1％冰醋酸（18：82），检测波长为280mm，流速1．0ml／min，柱温：室温。结果 原儿茶醛在2．9～58μg／ml之间线性良好，γ=0．9999；丹参素在7．1～142μs／ml之间线性良好，γ=0．9999；原儿茶醛平均回收率100．3％，RSD=3．4％（n=6），丹参素平均回收率99．5％。RSD=1．9％（n=6）。结论 该方法能准确可靠地同时测定肝得治胶囊中原儿茶醛、丹参素含量，能够有效地控制该制剂的质量。     

HPLC法测定清脂通络胶囊中原儿茶醛的含量

目的测定清脂通络胶囊中原儿茶醛的含量。方法采用高效液相色谱法，使用C18柱，甲醇-水-冰醋酸(5：110：1)为流动相，检测波长为280nm。结果加样回收率为95.49％，RSD=1．2％，三批样品中原儿茶醛含量的平均值为0．005％。结论方法简便、准确、分离度较好，结果稳定。可用于本品的质量控制。     

高效液相色谱法测定耳聪颗粒中原儿茶醛的含量

目的：建立耳聪颗粒中原儿茶醛的含量测定方法。方法：采用高效液相色谱法测定耳聪颗粒中原儿茶醛的含量。采用SilC18色谱柱，以甲醇-1％醋酸（13：87）为流动相，流速为1mL·min^-1，检测波长280nm。结果：原儿茶醛在0．0762-0．4572μg范围内线性关系良好，r=0．9999，平均回收率为100．9％，RSD为0．78％（n=6）。结论：该方法简便、灵敏、准确，可作为耳聪颗粒的质量控制方法。     

安神口服液的质量控制研究

目的 建立安神口服液的鉴别方法和原儿茶醛的含量测定方法。方法 采用薄层色谱(TLC)法对该制剂中的酸枣仁、地黄、丹参进行定性鉴别；薄层扫描法测定该制剂中原儿茶醛的含量。结果 TLC色谱中斑点清晰，易于识别：原儿茶醛的平均回收率为102．32％，RSD为0．99％。结论 本方法简便、准确、可靠，制剂质量可控。     

高效液相色谱法测定复方丹参片与滴丸中7种活性成分含量

目的：建立高效液相色谱( HPLC)法同时测定复方丹参片和复方丹参滴丸中7种活性成分含量的方法。方法采用Zorbax C18色谱柱,以乙腈-0.1％磷酸溶液为流动相,梯度洗脱,流速1 mL·min-1,检测波长为203,270和281 nm。结果7种成分峰面积与浓度的线性关系良好;加样回收率在95.1％~100.4％;滴丸样品中丹参酮ⅡA未能检出。结论建立了两类复方丹参制剂中同时测定丹参素、原儿茶醛、三七皂苷R1、人参皂苷Rg1、丹酚酸B、人参皂苷Rb1和丹参酮ⅡA含量的方法,精密度高,重复性好,可用于两类复方丹参制剂的质量控制;复方丹参片中丹参酮ⅡA含量明显高于滴丸。     

RP-HPLC法测定心可舒胶囊中原儿茶醛的含量

目的：建立心可舒胶囊中原儿茶醛的HPLC测定含量方法。方法：色谱柱：phenomenesC18柱（200mm×4．6mm,51Am）,流动相：甲醇-水-冰醋酸水溶液（10：90：0．5）,流速：1．0ml·min^-1,检测波长：280hm。结果：原儿茶醛在0．80～4．0μg范围内有良好的线性关系（r=0．9997）,平均加样回收率为99．87％（RSD：1．0％）。结论：本法简便、灵敏度高,分离效果好,适用于该制剂的质量控制。     

RP-HPLC同时测定香丹注射液中丹参素钠、原儿茶醛和丹酚酸B的含量

目的测定香丹注射液中丹参素钠、原儿茶醛和丹酚酸B的含量。方法采用反相高效液相色谱法分析．色谱柱为Diamnsil C18（250mm x 4．6ram,5vm）,流动相为0．1％冰醋酸-乙腈（90：10）,流速为1．0mL·min-1,检测波长为280nm。结果丹参素钠、原儿茶醛和丹酚酸B分别在S．06～101．10vg·mL-1、5．60～111．90ug·mL-1。和5．43～108．50utg·mL-1。的求度范围内有较好的线性关系．加样回收率分别为102．4796、98．36％和99．71％。结论该方法简便、准确、重复性好,并为该制荆的质量控制提供了依据。     

HPLC法测定前列安通胶囊中原儿茶醛含量

目的：采用HPLC法测定前列安通胶囊中原儿茶醛含量,以控制该制剂的质量。方法：用十八烷基键合硅胶柱分离原儿荼醛。流动相为甲醇-水-甲酸（9．5：90：0．5）;检测波长281nm。结果：主峰峰形较好,保留时间适当：线性回归方程为：y=9×10^6x＋5436．8r=0．9999,原儿茶醛在0．0408μg-0．4080μg范围内呈良好的线性关系;回收率为96．4,RSD为1．65（n=6）;结论：该方法测定前列安通胶囊中原儿茶醛含量方便,准确,快速。     

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.