反相高效液相色谱法测定非洛地平缓释片的含量

采用ＲＰ－ＨＰＬＣ法测定非洛地平缓释片的含量。以ＮＯＶＡ－ＰＡＫＣ１８柱为分析柱,甲醇－水（８０：２０）为流动相,检测波长为２３８ｎｍ。该法线性良好（ｒ＝０．９９９９）,精密度ＲＳＤ＝２．２％,平均加样回收率９９．１％,ＲＳＤ＝０．７％（ｎ＝５）。     

HPLC测定风寒咳喘口服液中柚皮甙含量

用ＨＰＬＣ法测定风寒咳喘口服液中柚皮甙的含量。ＨＩＴＡＣＨＩＧＥＬ３０５０色谱柱，以甲醇－醋酸－水（４５：５：５０）为流动相，检测波长２８３ｎｍ。回收率为９８．５１％，ＲＳＤ为０．４１％。     

HPLC法测定精制冠心口服液中丹参素的含量

建立了反相ＨＰＬＣ测定精制冠心口服液中的丹参素的含量测定方法。采用Ｃ１８柱,水－甲醇－二甲基甲酰胺－冰醋酸（９０：４：４：２）为流动相,检测波长２８１ｎｍ,线性范围为０．０２７２￣０．２２４８ｍｇ／ｍｌ（ｒ＝０．９９９９,ｎ＝５）,回收率为９８．４％,ＲＳＤ＝０．８％。     

离子对色谱法测定颠茄及莨菪制剂中的3种有效成分

本文以安宫黄体酮为内标，采用离子对色谱法测定莨菪烷类的３种有效成分（东莨菪碱、山莨菪碱、阿托品）的含量。仪器：ＬＣ－４Ａ，层析柱：ＯＤＳ４．６ｍｍ×１５ｃｍ；柱温：３５℃；流动相：乙腈─甲醇─冰乙酸─二乙胺─水（水含０．００５ｍｏｌ／Ｌ十二烷基磺酸钠，５０：２５：０．０７５：０．１２５：２５）。在２０７ｎｍ波长处检测，样品回收率：东莨菪碱，１００．３％，ｎ＝５，ＲＳＤ＝１．３％；山莨菪碱，９８．８％，ｎ＝５，ＲＳＤ＝１．２％；阿托品，９９．１％，ｎ＝５，ＲＳＤ＝０．９３％。     

RP—HPLC测定天乐口服液中橙皮苷的含量

采用ＲＰ－ＨＰＣＡ测定天乐口服液中橙皮苷的含量,以μ－ＢｏｎｄａｐａｋＣ１８柱（１０μｍ,４．６ｍｍ×２５０ｍｍ）为固定相,２％甲醇的乙腈溶液－０．１％磷酸和０．１％三乙胺的水溶液（２０：８０）为流动相进行测定,紫外检测波长２８４ｎｍ,平均回收率为９９．９５％,ＲＳＤ＝０．９３％。     

高效液相色谱法用于注射用穿琥宁及穿戛宁注射液含量测定的 …

目的：测定注射用穿琥宁及穿琥宁注射液含量。方法：采用高效液相色谱法。色谱柱为Ｓｈｉｍｐａｃｋ ＣＬＣ Ｃ１８柱,流动相为０．０２ｍｏｌ．Ｌ＾－１磷酸二氢钾（ｐＨ３．０）－乙腈－甲醇（４０：１０：５０）,流速１．２ｍＬ．ｍｉｎ＾－１,检测波长为２５１ｎｍ。应用二级管阵列检测器对色谱峰纯度进行检验,以排除有关物质的干扰。结果：平均回收率为９９．８８％,ＲＳＤ为０．１３％（ｎ＝３）。方法日内ＲＳＤ为０．     

复方喜树碱贴膏中喜树碱的高效液相测定法

建立了反相高效液相色谱治测定复方喜树碱贴膏中喜树碱含量的方法。ＨＰＬＣ条件为：岛律Ｓｈｉｍ－ｐａｃｋＣＬＣ—ＯＤＳ（１５０Ｘ６．０ｍｍ）柱，流动相为甲醇－０．０１ｍｏｌ／Ｌ磷酸二氢钾缓冲液＝５０：５０（ｐＨ＝６．５），内标为对羟基苯甲酸甲酯；紫外检测波长２５４ｎｍ。实验结果表明浓度线性范围５．２１～２６．０２ｕｇ／ｍｌ（ｒ＝０．９９９９），平均口收率（ｎ＝５）为９９．６２％，ＲＳＤ＝０．５％。     

高效液相色谱法测定壮骨关节丸中补骨脂素和异补骨脂素的含量

目的： 测定壮骨关节丸中补骨脂素、异补骨脂素的含量。方法： 高效液相色谱法, ＡｌｌｔｉｍａＣ１８ 分析柱（２５０ ｍ ｍ ×４－６ ｍ ｍ , ５ μｍ） , 流动相： 甲醇－ 水（５０∶５０） , 检测波长： ２４５ ｎｍ , 流速：１－０ ｍＬ·ｍｉｎ － １ , 柱温： ４０ ℃。结果： 补骨脂素在０－０７４ ８ ～０－５９８ ４ μｇ （ｒ ＝ ０－９９９ ９） 、异补骨脂素在０－０７５ ４ ～０－６０３ ２ μｇ （ｒ ＝ ０－９９９ ９） 范围内呈线性; 补骨脂素和异补骨脂素平均回收率分别为９８－２８ ％ （ ＲＳＤ＝ １－６ ％ ） 和９８－７２ ％ （ ＲＳＤ＝ ２－０ ％ ） 。结论： 本方法简便、快速, 准确。     

高效液相色谱法测定注射用穿琥宁的含量

采用高效液相色谱法「检测波长为２１５ｎｍ,ＣＬＣ－ＯＤＳ柱,乙醇－水－醋酸（５０：５０：０．１）为流动相」测定注射用穿琥宁的含量,方法准确,简便。在浓度为每ｍｌ１．１－５．５μｇ范围内线性关系良好,平均回收率为９９．６％,ＲＳＤ＝０．８５％。     

高效液相色谱法测定兔血浆中羟基喜树碱的含量

采用高效液相色支测定兔血浆中羟基喜树碱的含量。色谱柱为Ｓｈｉｍｐａｃｋ ＣＬＣ－ＯＤＳ,流动相为甲醇－１０ｍｍｏｌ／Ｌ磷酸盐缓冲液（６０：４０,ｐＨ４．０）,检测波长３８２ｎｍ。血药浓度在５２￣１０４００ｎｇ／ｍｌ范围内呈线性关系Ｙ＝－２２９４＋５０．６０Ｘ,ｒ＝０．９９９４,最低检出浓度为２０ｎｇ／ｍｌ,方法回收率为１０３．０％,ＲＳＤ为２．９６％（ｎ＝３）,萃取回收率为６３．２％,ＲＳＤ为２．     

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.