HPLC法测定天麻胶囊中非法掺入的吲哚美辛

目的：建立HPLC法测定中成药天麻胶囊中非法掺入的西药吲哚美辛。方法：采用kromasil C8（250mm×4.6mm．10μm）．流动相：0．1mol·L^-1冰醋酸溶液-乙腈（52．5：47．5），检测波长：228nm，流速：1．0ml·min^-1，柱温：25℃。结果：测得吲哚美辛线性范围为10．3-92．7μg·ml^-1（r=0．9999），平均回收率为102．0％，RSD为0．7％。结论：本法操作简便，结果可靠。可用于检测天麻胶囊中非法添加的西药吲哚关辛。     

薄层色谱法测定天麻胶囊中掺入的吲哚美辛

目的:检定某厂家天麻胶囊中掺入的西药成分吲哚美辛.方法:采用薄层色谱法.结果与结论:方法简便,灵敏,专属性强,建立的方法可供药监打假中检测天麻胶囊中掺入吲哚美辛用.     

液相色谱-离子阱质谱联用法检测抗风湿类中药制剂中非法掺入的萘普生、吲哚美辛

目的：建立检测抗风湿类中成药中非法掺入萘普生、吲哚美辛的专属性方法。方法：采用液相色谱-电喷雾质谱联用法。液相色谱：色谱柱为Agilent C18柱（150mm×4．6mm，5μm），流动相为0．02moL·L^-1。醋酸铵-1％醋酸溶液-甲醇（32：3：65），流速0．4mL·min^-1；柱温30℃。质谱：电喷雾电离源（ESI）负离子检测；质荷比范围m／z 100～400，干燥气温度350℃；干燥气流速10L·min^-1；干燥气压力276kPa；源电压为5kV。通过相对分子质量，一级及二级质谱碎片信息、液相色谱保留时间和紫外光谱四方面的信息，对抗风湿类中成药的提取液中非法掺入的萘普生、吲哚美辛进行定性鉴别。结果：6批抗风湿类中药，3批检出掺有萘普生，其中2批检出同时掺有吲哚美辛。结论：该方法选择性强，灵敏度高，可作为分析检测抗风湿类中成药中萘普生、吲哚美辛的有效方法，可用于分析鉴定中成药非法添加西药成分的打假工作．     

热熔挤出技术制备吲哚美辛速释胶囊

目的以热熔挤出技术制备吲哚美辛速释胶囊。方法选用不同的亲水性载体，如聚乙二醇（PEG-6000，PEG-10000）、聚乙烯吡咯烷酮（PVP—k30）、泊洛沙姆188（F-68），应用热熔挤出技术制备吲哚美辛速释胶囊，比较其与物理混合物胶囊及原料药胶囊的药物溶出速率。结果与相应的物理混合物胶囊及原料药胶囊相比，用热熔挤出技术制备的速释胶囊吲哚美辛的溶出速率快，且以PEG-10000／PVP—k30／F-68／吲哚美辛质量比：1：1：1：1系统的药物溶出速率最快。结论用热熔挤出技术制备的吲哚美辛速释胶囊可提高药物的溶出度。     

“天麻胶囊”质量标准中补充检验吲哚美辛的方法

目的:建立天麻胶囊中非法添加吲哚美辛的检测方法.方法:采用TLC快速筛选、HPLC-PDA法进行定量检验以及UPLC-MS法进行结构确认.结果:建立的方法能鉴别并确认添加的吲哚美辛,灵敏度高,专属性好.结论:该方法简便、快速,结果准确,可用于检测天麻胶囊中非法加入的吲哚美辛成分.     

氨糖美辛肠溶胶囊中吲哚美辛的含量测定

目的采用高效液相色谱（HPLC）法测定氨糖美辛肠溶胶囊中吲哚关辛含量。方法采用phenomsil BDS-C18色谱柱（250mm×4．6mm，5μm），以0．1mol／L冰醋酸溶液-乙腈（45：55）为流动相，检测波长为228nm。结果吲哚关辛质量浓度的线性范围为19．96～73．16μg／mL，（r=0．9999），平均回收率为100．1％，RSD=0．3％（n=6）。结论HPLC法可准确检测出氨糖关辛肠溶胶囊中吲哚美辛含量。     

吲哚美辛锌胶囊的溶出度研究

［摘要］目的：探讨吲哚美辛锌胶囊的溶出度，控制药品质量。方法：用紫外分光光度法测定吲哚美辛锌的含量，用转篮法测定溶出度。结果：随着pH值增加，吲哚美辛锌的溶解度增大，溶出度符合Weibull方程，t50为26.8 min。结论：吲哚美辛锌胶囊45 min溶出度＞75%，符合《中华人民共和国药典》规定。     

检查天麻胶囊中添加吲哚美辛的方法研究

建立薄层色谱法、高效液相色谱法对添加吲哚美辛的天麻胶囊进行分离分析，并用高效液相色谱-二极管阵列检测进行定性鉴定。测定了7个厂家的11批产品，发现其中2批添加了吲哚美辛。本方法可作为监督检查天麻胶囊中添加化学药的参考方法。     

吲哚美辛缓释胶囊单剂量与多剂量达稳态时的相对生物利用度

采用反相高效液相色谱法测定１１名健康志愿受试者单剂量口服７５ｍｇ和多剂量口服吲哚美辛缓释胶囊和吲哚美辛片后，吲哚美辛血药浓度变化情况。测得单剂量口服７５ｍｇ吲哚美辛缓释胶囊与吲哚美辛片的达峰时间分别是４．０ｈ与１．５ｈ，峰浓度分别是１．０２μｇ·ｍｌ－１与３．７μｇ·ｍｌ－１，吲哚美辛缓释胶囊的相对生物利用度为１０２％。测得多剂量口服吲哚美辛缓释胶囊与吲哚美辛片达稳态后的Ｃｍｉｎ分别是０．２０８μｇ·ｍｌ－１与０．２６３μｇ·ｍｌ－１，Ｃｍａｘ分别是１．２６μｇ·ｍｌ－１与１．２２６μｇ·ｍｌ－１，Ｔｍａｘ分别为２．７７ｈ与１．８２ｈ，ＦＩ分别是１４０．８１％与１２８．２１％。以ＡＵＣ为指标，经统计分析，吲哚美辛缓释胶囊与吲哚美辛片在单剂量和多剂量达稳态时是生物等效制剂。     

HPLC法测定吲哚美辛肠溶片含量

目的：采用HPLC法测定吲哚美辛肠溶片含量。方法：色谱柱：C18柱（岛津VP—ODS，150mm×4．6mm，5μm）；流动相：0．1mol·L^-1冰醋酸溶液-乙腈（50：50）；流速1ml·min^-1；检测波长228nm。结果：吲哚美辛在5-500μg·ml^-1浓度范围内呈良好的线性关系（r=0．9999），平均回收率为99．7％，RSD为0．1％（n=6）。结论：本方法简便快速，重现性好，结果准确可靠。     

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.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

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.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.     

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.