紫外分光光度法测定盐酸罂粟碱氯化钠注射液中盐酸罂粟碱的含量

目的 　建立盐酸罂粟碱氯化钠注射液中盐酸罂粟碱合量测定方法。方法 　采用紫外分光光度法在 2 5 0 nm处测定盐酸罂粟碱的含量。结果 　盐酸罂粟碱在 0 .64 5～ 5 .80 9μg· m L- 1 范围内 ,线性关系良好 ( r=0 .9999) ;平均加样回收率为 99.66%,RSD为 0 .5 %( n=9)。结论 　本方法结果准确 ,重现性较好。     

高效液相色谱法测定注射用盐酸罂粟碱的含量

目的建立注射用盐酸罂粟碱中盐酸罂粟碱的含量测定方法。方法采用高效液相色谱法。以甲醇-0．005N庚烷磺酸钠（冰乙酸调pH值至3．0）（55：45）为流动相,用外标法按峰面积计算回收率。结果盐酸罂粟碱在1．490—11．920μg／ml范围内,线性关系良好（r=0．9999）;平均回收率为99．5,RSD为0．31（n=9）。结论高效液相色谱法操作简便快捷,测定结果准确,可用于注射用盐酸罂粟碱的含量测定和质量控制。     

高效液相色谱法测定注射用盐酸罂粟碱的含量

目的建立注射用盐酸罂粟碱中盐酸罂粟碱的含量测定方法。方法采用高效液相色谱法。以甲醇-0．005N庚烷磺酸钠(冰乙酸调pH值至3．0)(55：45)为流动相，用外标法按峰面积计算回收率。结果盐酸罂粟碱在1．490～11．920μg／ml范围内，线性关系良好(r=0．9999)；平均回收率为99．5，RSD为0．31(n=9)。结论高效液相色谱法操作简便快捷，测定结果准确，可用于注射用盐酸罂粟碱的含量测定和质量控制。     

高效液相色谱法测定鼻炎康片中麻黄碱和伪麻黄碱的含量

目的建立高效液相色谱法测定鼻炎康片中盐酸麻黄碱和盐酸伪麻黄碱的含量。方法采用高效液相色谱法,色谱柱：Phenomenex C18（250mm×4．6mm,5μm）;流动相：甲醇-0．07mol·L^-1磷酸钠溶液（用磷酸调pH=6．0,含17．5mmol十二烷基硫酸钠）（50：50）;检测波长：210nm。结果盐酸麻黄碱进样量在0．01029～1．029μg呈现良好的线性关系,r=0．9999;盐酸伪麻黄碱进样量在0．02023～0．5058μg呈现良好的线性关系,r=0．9997。盐酸麻黄碱平均加样回收率为95．6％（n=6）,RSD为1．6％;盐酸伪麻黄碱平均加样回收率为97．9％（n=6）,RSD为1．6％。结论本法准确、重复性好,可有效控制制剂中盐酸麻黄碱、盐酸伪麻黄碱的含量。     

HPLC法测定注射用盐酸罂粟碱的含量

目的:建立注射用盐酸罂粟碱中盐酸罂粟碱的HPLC含量测定方法。方法:Dikma C18柱(250 mm×4．6 mm,5μm),以甲醇-0．005 mol·L-1庚烷磺酸钠(冰乙酸调pH至3．0)(55:45)为流动相,流速1．0 ml·min-1,检测波长是254 nm。结果:盐酸罂粟碱在1．49-11．92μg·ml-1范围内,(r=0．999 9)线性关系良好;平均回收率为99．7％,RSD为0．9％(n=9)。结论:本法操作简便快捷,测定结果准确,可用于注射用盐酸罂粟碱的质量控制。     

紫外分光光度法测定盐酸美西律片的含量

目的：建立紫外分光光度法测定盐酸关西律片的含量。方法：紫外分光光度法,以261nm为测定波长。结果：平均加样回收率为100．10％（n=9）,RSD为0．23％。结论：该法可靠,操作简便,可用于盐酸美西律片剂质量控制。     

高效液相色谱法测定盐酸罂粟碱卵磷脂微乳含量

目的 建立测定盐酸罂粟碱 卵磷脂微乳含量的高效液相色谱法。方法 采用C18柱（250 mm×4.6 mm，5 μm）；以甲醇 水 三乙胺（60：40：0.001）（V：V：V）为流动相，流速1.0 mL·min 1，检测波长为248 nm。结果 盐酸罂粟碱在0.181 2～0.604 0 mg·mL 1浓度范围进样量与峰面积呈良好的线性关系（r=0.999 9）；微乳平均回收率为99.46%，RSD为0.4%（n＝5），药物保留时间为9～10 min。结论 该方法结果准确，重现性较好。可用于盐酸罂粟碱 卵磷脂微乳的含量测定和质量控制。     

HPLC法测定泌尿宁片中盐酸小檗碱的含量

目的：采用HPLC法测定泌尿宁片中盐酸小檗碱的含量。方法：色谱柱为Hypersil C18（200mm×4．6mm，10μm）；流动相为乙腈．磷酸二氢钾-十二烷基硫酸钠（50：25：25）；流速：1ml·min^-1；检测波长345nm。结果：盐酸小檗碱进样量在0．0195—0．1950μg之间。与峰面积呈良好的线性关系（r=0．9999），平均加样回收率为99．42％，RSD=0．72％（n=5）。结论：本方法操作简单、快速，可用于测定泌尿宁片中盐酸小檗碱的含量。     

高效液相色谱法测定香连片中盐酸小檗碱含量

目的建立香连片的盐酸小檗碱含量的测定方法。方法采用高效液相色谱法对方中的盐酸小檗碱进行含量测定,采用ODS色谱柱（250mm×4．6mm,5μm）,柱温为室温,流动相为每100ml加十二烷基磺酸钠0．1g的乙腈旬．1％磷酸溶液（49：51）,检测波长为265nm,流速：1ml／min。结果盐酸小檗碱进样量在1．95～13．0μg范围内线性良好,r=0．9995,平均回收率为98．84％（n=5）,RSD=1．47％。结论试验结果表明本法简便快速,重现性好,结果准确可靠,可以作为香连片中盐酸小檗碱含量测定的方法。     

高效液相色谱法测定柏洁洗剂中盐酸小檗碱含量

目的建立测定柏洁洗剂中盐酸小檗碱含量的高效液相色谱（HPLC）法。方法以十八烷基硅烷键合硅胶为填充剂，乙腈-0．033mol／L磷酸二氢钾溶液（25：75）为流动相，检测波长为265nm，进样量10μL，流速1．0mL／min，以外标法按峰面积计算含量。结果盐酸小檗碱进样量在0．0984～0．4920μg范围内与峰面积积分值线性关系良好，回归方程Y=4．16780 X-10．26217，r=0．9999（n=5），平均加样回收率为99．74％，RSD=1．10％（n=6）。结论HPLC法简便、快捷，结果准确，重现性好，可用于柏洁洗剂中盐酸小檗碱的含量测定和质量控制。     

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.