RP-HPLC法同时测定复方氟康唑霜中氟康唑、甲硝唑、氯霉素3种组分含量

目的： 建立同时测定复方氟康唑霜中氟康唑、甲硝唑、氯霉素３ 组分含量的简便方法。方法： 反相高效液相色谱法, 采用外标法, Ｕｌｔｒａｓｐｈｅｒｅ－ ＯＤＳ柱, 流动相为甲醇－ 水（５０∶５０） , 检测波长２６１ ｎｍ 。结果： 线性范围分别是： 氟康唑４０－１ ～２００－６ μｇ·ｍＬ－１ , ｒ＝０－９９９ ４; 甲硝唑２０－０ ～１００－０ μｇ·ｍＬ－１ , ｒ＝０－９９９ ８; 氯霉素３９－９～１９９－６ μｇ·ｍＬ－ １ , ｒ＝ ０－９９９ ８。平均回收率： 氟康唑９８－３１ ％ ; 甲硝唑１００－４ ％ , 氯霉素９８－１７ ％ 。结论：本法分离度好, 快速, 简便。适用于该制剂中３ 种成分的同时测定。     

络合萃取-分光光度法测定复方解热凝胶中马来酸氯苯那敏含量

创立了测定复方解热凝胶中马来酸氯苯那敏含量的络合萃取 分光光度法．实验表明,马来酸氯苯那敏在８ ～１８ μｇ／ｍＬ范围内呈现良好的线性关系．Ａ＝ ０－０４３ ８ Ｃ－ ０－０１６ ６ ,ｒ＝ ０－９９９ ７（ ｎ ＝ ５）,ＲＳＤ 为０－７４ ％ ,回收率９９－９ ％ ．     

HPLC测定定晕宁颗粒中葛根素的含量

采用ＨＰＬＣ法,选用Ｓｙｍｍｅｔｒｙ－Ｃ１８柱和甲醇：水（２５：７５）,乙酸调ｐＨ４．２。测定定晕宁颗粒中葛根素含量,结果回归方程为Ｙ＝１．７７ｘ－０．２８１３,ｒ＝０．９９９（ｎ＝５）,线性范围为０．６１４￣６．１４μｇ,平均回收率为９９．０３％,ＲＳＤ为３．９８％。     

尼麦角林及片剂的HPLC测定

用ＨＰＬＣ法测定尼麦角林原材料及其片剂的含量。方法：以ＬＵＮＡ Ｃ８为色谱柱，磷酸盐溶液－乙腈为流动相，检测波长为２８０ｎｍ结果：线性关系ｒ＝０．９９９ ９９，平均回收率为１００．０％，ＲＳＤ＝０．７５％。结论方法简便，准确，适合于该产品的质量检验分析。     

氯地滴眼液的含量测定

目的：采用ＨＰＬＣ法测定氯地滴眼液中氯霉素和地塞米松磷酸钠的含量。方法：色谱分析条件：ＯＤＳ柱作分析柱,流动相为甲醇／水体系,０￣８ｍｉｎ使用４０％甲醇,８￣１６ｍｉｎ使用６０％甲醇,流速１ｍｌ／ｍｉｎ,０￣９ｍｉｎ２４０ｎｍ紫外检测,：二组分分离良好。各组各组性关系良好,平均回收率氯霉素９９．８％（ＲＳＤ＝１．２％,ｎ＝５）,地塞米松磷酸钠９９．４％（ＲＳＤ＝０．７％,ｎ＝５）,结论：该法用于氯     

复方赖氨酸颗粒中盐酸赖氨酸的HPLC测定

目的： 采用反相ＨＰＬＣ 法, 分离测定复方赖氨酸颗粒中的盐酸赖氨酸。方法： 用２ , ４ － 二硝基氟苯为衍生化试剂, 将盐酸赖氨酸进行衍生化。以十八烷基硅烷键合硅胶为填充剂, 甲醇－０－０５ ｍｏｌ·Ｌ－ １ 醋酸钠和醋酸溶液（６５∶３５） 为流动相, 检测波长为３６０ ｎｍ 。结果： 盐酸赖氨酸浓度在２－７ ～２７ μｇ·ｍ Ｌ－ １ 范围内线性关系良好, ｒ ＝ ０－９９９ ９ , 回归方程 Ｃ＝ ２－５９１ ×１０ － ５ Ａ－ ０－３１６ ６ 。平均回收率为１００－２ ％ , ＲＳＤ 为０－６６ ％ （ ｎ ＝ ６） 。结论： 本法可用于测定复方赖氨酸颗粒中盐酸赖氨酸含量。     

一阶导数光谱法测定醋柳碘酊中水杨酸的含量

本文应用一阶导数光谱法测定醋柳碘酊中水杨酸的含量，可以排除其它组分形成的背景干扰。采用峰－谷法，以Ｄ值（｜△Ａ１｜＋｜△Ａ２｜）计算样品的含量。Ｄ值与浓度的关系为Ｄ＝８．６２３×１０＾－２Ｃ＋７．２×１０＾－３（ｘ＝０．９９９９）。方法简便、实用、重现性好。平均回收率为９９．９８％（ｃｖ＝０．３０％，ｎ＝９）。     

高效液相色谱法测定氯霉素氢化可的松滴耳液的含量

目的：采用ＨＰＬＣ法测定氯霉素氢化可的松滴耳液中氢霉素和氢化可的松的含量。方法：采用Ｃ１８色谱柱,流动相为甲醇－水（６０：４０ｖ／ｖ）,检测波长为２４０ｎｍ。结果：氯霉素在２５０～７５０ｕｇ．ｍｌ＾－１浓度范围内,ｒ＝０．９９９９,回收率９９．０％,ＲＳＤ＝０．５％;氢化可的松在４９．９６～１４９．８８ｕｇ．ｍｌ＾－１浓度范围内,ｒ＝０．９９９９,回收率９７．７％,ＲＳＤ＝０．８％。结论：该方法可     

联立方程新解法测定氯霉素氢化可的松滴耳液的含量

目的：测定氯霉素氢化可的松滴耳剂中二组份的含量。方法：采用新Ｖｉｅｒｏｒｄｔ法不经分离直接测定氯霉素氢化可的松滴耳剂中氯霉素、氢化可的松的含量。结果：２７８，２４８ｎｍ分别为测定波长，以稀醇为空白，氯霉素和氢化可的松的平均回收率及ＲＳＤ分别为１００．７９％、０．４２％；９９．８２％、１．４２％。结论：氯霉素氢化可的松滴耳剂以稀醇为稀释剂，不经分离，直接在２４８，２７８ｎｍ处测其吸收值，α与β乘积小于０．５；Ａａ＋ｂ２７８与βＡａ＋ｂ２４８、Ａａ＋ｂ２４８与αＡａ＋ｂ２７８的比值均大于１．２，符合新Ｖｉｅｒｏｒｄｔ法的要求，本法操作简便快速，重现性好，可消除二组份相互干扰，结果满意     

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。     

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.