RP—HPLC法测定扑感敏片中三种有效成分的含量

目的：探讨扑敏片中三种有效成分的含量测定新方法。方法：利用HPLC内标法,用C18色谱柱,以甲醇－水（45：55）为流动相,检测波长：285nm,灵敏度：0．2AuFS。结果：扑热息痛在30－150ug/ml,氨基比体在20－100ug/ml,咖啡因在6－30ug/ml浓度范围内均呈良好的线性关系,结论：该方法分析速度快,操作简便,准确,灵敏度高,专属性强,可用作该制剂含量的测定。     

系数倍率法测定妇康泡腾片两组分的含量

目的：建立妇康泡腾片中甲硝唑和硝酸咪康唑的测定方法。方法：以95％的乙醇为溶剂,采用系数倍率法,甲硝唑的测定波长为321．0nm,硝酸咪康唑的测定波长为228．0nm,结果：甲硝唑和硝酸咪康唑浓度与吸收率呈线性关系的浓度范围分别为6．40－13．60ug/ml和5．6－10．00ug/ml,平均回收率分别为100．04％（RSD．0．33％）和100．52（RSD＝0．09％）,结论：方法简便可靠,可用于妇康泡腾片的含量测定。     

薄层色谱比色法测定胆乐胶囊中猪去氧胆酸的含量

目的：制定胆乐胶囊中主要有效成分猪去氧胆酸的含量控制标准。方法：采用薄层色谱－比色法测定胆乐胶囊中猪去氧胆酸的含量。以环已烷－乙酸乙酯－醋酸－甲醇（2;16：1：1）为展开剂,测定波长为544nm。结果：点样量在12－72ug/ml范围内线性关系良好,平均回收率为93．8％（n=3,RSD=3.0%),R=0.998。结论：仪器设备简单,结果准确、可靠。     

灌装温度对中药代煎包材中塑化剂迁移率的影响规律

目的研究中药代煎包材中邻苯二甲酸酯类塑化剂的迁移量随灌装温度的变化规律,为规范中药代煎流程提供一定的参考。方法检测中药代煎包材中17种常见邻苯二甲酸酯类塑化剂的含量;将蒸馏水煮沸后,在梯度温度下灌装到中药代煎包材中,采用气质联用色谱技术,定性定量各邻苯二甲酸酯类塑化剂的迁移率。结果GC-MS符合检测邻苯二甲酸酯类塑化剂的要求,标准曲线和相关系数显示,在0.05~5.00 mg/L呈良好线性关系,相关系数>0.998,检出限为0.002 mg/L。中药代煎包材检出的邻苯二甲酸酯类塑化剂及其含量为DEHP(0.122 mg/kg)、DBP(0.273 mg/kg)、DIBP(0.073 mg/kg)、DEP(0.024 mg/kg)和DMP(0.037 mg/kg),其他12种PAEs未检出。30~100℃的梯度温度灌装后,蒸馏水中检出的塑化剂及其迁移率分别为DEHP(0.14%~10.58%)、DBP(6.29%~20.76%)、DEP(ND^1.09%),其余未检出。结论GC-MS能够准确、快捷地检测中药代煎包材中邻苯二甲酸酯类塑化剂的含量;样品包材中PAEs及其迁移量符合GB96852016中相关要求;灌装温度与中药代煎包材中DEHP、DBP的迁移率呈正相关,灌装温度越高,DEHP、DBP的迁移率也越高;灌装温度对中药代煎包材中DIBP、DMP和DEP的迁移率没有显著影响。从减少塑化剂的迁移量和保证中药代煎效率的角度出发,中药代煎的灌装温度控制在60℃以下能显著降低DEHP、DBP的迁移量。     

HPLC法测定萘丁美酮干混悬剂的含量

目的：报道HPLC法测定萘丁美酮干混悬剂的含量。方法：采用Kromasil C18色谱法,以甲醇－0．05mol/L醋酸钠（盐）缓冲液（80：20,pH3.5)为流动相,检测波长261nm,结果：在199．68－1198．08ug/ml范围内,线性关系良好（r=0.9999);平均回收率100．5％（RSD＝0．86％）。结论：该方法简便,快速。结果准确可靠,可作为萘丁美酮干混悬剂含量测定的方法。     

黄芪多种成分抗人疱疹病毒的初步实验研究

目的：为了开发利用黄芪的抗病毒性质，我们进行了此项研究。方法：我们以阿普洛韦（ACV)为阳性对照，采用对病毒所致细胞病变的抑制及空斑减数实验，观察了黄芪总皂苷、总多糖、总黄酮抗HSV药效。结果：在Hep-2细胞系统中，ACV对HSV－1 HS－1株直接杀灭、感染阻断、增殖抑制的ED50为30．83ug/ml,16.04ug/ml,20.04ug/ml；对HSV－2333株的相应ED50为16.45ug/ml,18.62ug/ml,10.85ug/ml,黄芪总皂苷对HSV－1 HS－1株相应ED50为1．68ug/ml，1．72ug/ml，1．95ug/ml；对HSV－2333株相应ED50为1．73ug/ml，2．70ug/ml，2．74ug/ml，黄芪总多糖对HSV－1 HS－1株的相应ED50为4．03ug/ml，5．33ug/ml，4．90ug/ml；对HSV－2333株相应ED50为6．04ug/ml，5．43ug/ml，7．50ug/ml，黄芪总黄酮对HSV－1 HS－1株的相应ED50为4．95ug/ml，2．75ug/ml，3．49ug/ml；对HSV－2333株的相应ED50为3．56ug/ml，3．93ug/ml，6．27ug/ml。结论：黄芪对HSV－1的治疗指数为ACV的10．3，4．1，5．5倍；对HSV－2的治疗指数为ACV的3．7，2．7，1．0，1．6倍。总多糖对HSV－1的治疗指数为ACV的10．3，4．1，5．5倍；对HSV－2的治疗指数为ACV的3．7，2．7，3．3倍。总黄酮的治疗指数为ACV相近，值得开发利用。     

高效液相色谱法测定醋氯芬酸缓释片的含量

目的：建立了高效液相色谱法测定醋氯芬酸缓释片的含量。方法：采用Zorbax SB-C18色谱柱,以乙腈－四氢呋喃－冰醋酸（25：25：50,用1．0mol/L的NaOH高pH3.5）为流动相,流速为1.0ml/min,以对羟基联苯为内标物,检测波长为275nm,结果：醋 芬酸在10．2－50．1ug/ml范围内呈良好线性（r=0.9993),平均回收率为100．3％,RSD为0．45％,结论：本法可用于该片剂的测定,操作简便,结果准确。     

四乙酰核糖HPLC法测定

为了建立高效液相色谱法分离测定四乙酰核糖纯度及相关杂质的方法,以YWG－18为分析柱,以35％乙腈为流动相,流速为1ml/min,检测波长为210nm,对四乙酰核糖进行了HPLC法测定在50ug/ml-10000ug/ml浓度范围内呈线性关系（r=0.99997),且测定方法性较好（RSD＜1％）,精密度＜1％,证明本方法简单准确,重现性好,可用于分离测定四乙酰核糖纯度及相关质。     

双波长比值光谱法测定银黄口服液中绿原酸和黄芩苷含量

目的：应用双波长比值光谱法对银黄口服液中绿原酸和黄芩苷含量测定进行研究。方法：依据绿原酸和黄芩苷的比值光谱特征,选择266和342nm作为测定波长。结果：绿原酸线性范围2－20ug/ml,回收率98。9,RSD为1．58％;黄芩苷线性范围2－16ug/ml,回收率100．4％,RSD为1．32％,结论：本法为一种灵敏,准确和简便的分析方法,可在其他中药制剂中推广应用。     

LC-MS/MS测定注射用聚氯乙烯袋中注射液的邻苯二甲酸二异辛酯

目的 建立测定注射用聚氯乙烯(PVC)袋中注射液的邻苯二甲酸二异辛酯(DEHP)含量的方法.方法 以邻苯二甲酸二乙酯(DEP)为内标,采用LC-MS法测定.结果 DEHP和DEP的tR分别为2.86、1.05 min,在19.6～588.0 ng·ml-1有较好线形关系,RSD=3.5%,平均回收率为99.2%,最低检测限为5.88 ng·ml-1.结论 所建方法专属性强,适用于对注射用PVC袋中注射液的DEHP的含量测定.     

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.