HPLC法同时测定复方可待因口服溶液中磷酸可待因、盐酸麻黄碱、盐酸曲普利啶的含量

目的 建立同时测定复方可待因口服溶液中磷酸可待因、盐酸麻黄碱、盐酸曲普利啶3组分含量的高效液相色谱法。方法 采用Hypersil-BDSCN柱，流动相为乙腈-0．4％乙酸铵溶液-三乙胺(30：70: 0．2)，流速为1．0ml／min，检测波长257nm，外标法计算。结果 线性范围分别是磷酸可待因125～l000μg／ml，r=0．9999，盐酸麻黄碱75～600μg／ml，r=0．9996；盐酸曲普利啶18～140μg／ml，r=0．9997。回收率分别为磷酸可待因99．9％、盐酸麻黄碱99．7％、盐酸曲普利啶100．3％。结论 本方法分离效果好，辅料无干扰，快速，简便，适合于该制剂3组分的同时测定。     

HPLC法测定茶碱麻黄碱片中茶碱和麻黄碱的含量

目的：建立HPLC法测定茶碱麻黄碱片中茶碱与盐酸麻黄碱的含量。方法：采用Diamonsil C18色谱柱，以甲醇-0．005mol·L^-1磷酸二氢钾溶液（含0．3％三乙胺，用磷酸调节pH值至3．0）（20：80）为流动相，流速为1．3mL·min^-1，检测波长210nm。结果：所选流动相适用范围较广，耐用性好，样品中两种成分分离度大。盐酸麻黄碱与茶碱分别在进样量在0．30—0．90μg（r=0．9997）和1．42～4．24μg（r=0．9993）范围线性关系良好，回收率分别为99．8％和100．0％（RSD分别为1．0％和0．8％）。结论：本法简便、准确、精密度高，可有效地控制茶碱麻黄碱片中双组分的含量。     

HPLC法测定抗感口服液中麻黄碱含量

目的：建立抗感口服液中盐酸麻黄碱的含量测定方法。方法：采用高效液相色谱法，以C18为固定相，流动相为磷酸二氢钠0．25mol／L(用磷酸调节PH=3．5)水溶液-甲醇(70：30)，检测波长为214nm。结果：盐酸麻黄碱进样量在0～0．576mg／ml范围内与峰面积有良好的线性关系，r=0．9990，平均回收率RSD=0．31％。结论：本法专属性强、重现性好。     

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法测定小儿肺热咳喘口服液中盐酸麻黄碱及盐酸伪麻黄碱的含量

目的：建立小儿肺热咳喘口服液中盐酸麻黄碱及盐酸伪麻黄碱含量的HPLC测定法。采用Agilent XDB-C18柱,流动相为乙腈-0．2％磷酸（3：97）,检测波长：210nm。结果：盐酸麻黄碱在0．03068～1．534μg（r=1．0000）范围内成线性关系,平均回收率（n=6）为98．6％,RSD=2．6％。盐酸伪麻黄碱在0．03110～1．555μg（r=1．0000）范围内成线性关系,平均回收率（n=6）为97．8％,RSD=2．4％。结论：本法简便、可靠、准确,可用于该制剂的质量控制。     

紫外分光光度法测定氯麻滴鼻液的含量

目的：建立氯麻滴鼻液中氯霉素和盐酸麻黄碱的含量测定方法。方法：采用双波长分光光度法同时测定氯麻滴鼻液中氯霉素和盐酸麻黄碱的含量。结果：氯霉素的平均回收率为99．8％，RSD为0．3％(n=6)；盐酸麻黄碱的平均回收率为100．3％，RSD为0．6％(n=6)。结论：本法简便、准确，符合医院制剂快速检验的要求。     

离子对反相高效液相色谱法测定镇咳宁糖浆中盐酸麻黄碱的含量

目的：建立镇咳宁糖浆中盐酸麻黄碱的含量测定方法。方法：采用高效液相色谱法,以C18为固定相,流动相为乙腈—水—磷酸(48：52：0．1)(每1000ml加4g十二烷基硫酸钠)。检测波长210nm,结果：盐酸麻黄碱进样量在0．4304～1．291μg范围内与峰面积有良好的线性关系(r=0．9996),平均回收率为100．2％,RSD为1．7％(n=6)。结论：所用方法简单快速,专属性强,重现性好,能够控制产品的质量。     

高效液相色谱法测定消炎止咳片中盐酸麻黄碱含量

目的 用高效液相色谱（HPLC）法测定消炎止咳片的盐酸麻黄碱含量。方法 色谱柱为Alltech C18柱（150mm×4．6mm，5μm），流动相为乙腈-0．1％磷酸溶液（5：95），检测波长207nm，流速为1．0mL／min。结果 盐酸麻黄碱质量浓度线性范围为4．34～26．04μg／mL（r=0．9999），平均回收率为99．58％，RSD为1．36％。结论 HPLC法精密度好，结果准确，可作为消炎止咳片的盐酸麻黄碱含量测定方法。     

HPLC测定复方鼻炎喷雾剂中盐酸麻黄碱的含量

目的：建立用高效液相色谱法测定复方鼻炎喷雾剂中盐酸麻黄碱的含量。方法：采用Hypersil ODS2（250mm×4．6mm,5μm）大连依利特分析仪器有限公司色谱柱;流动相为乙腈-0．1％磷酸（10：90）;流速为1．0ml／min;检测波长为207nm。结果：盐酸麻黄碱的进样量在7．1～142．0ng范围内与峰面积呈良好的线性关系（r=0．9996）：平均回收率为101．9％（RSD=2．0％,n=6）。结论：该方法操作简单、准确、重复性好,可用于复方鼻炎喷雾剂中盐酸麻黄碱的含量测定。     

高效液相色谱法测定鼻嗅通喷雾剂中盐酸麻黄碱的含量

目的：建立高效液相色谱法测定鼻溴通喷雾剂中盐酸麻黄碱的含量。方法：以DiamonsilC17（4．6mm×15mm，5μm）为分析柱，甲醇-0．01mol·L^-1磷酸二氢钾（用磷酸调pH2．5）（4：96，V／V）为流动相，流速为1．0mL·min^-1，检测波长为210nm，采用外标法定量测定。结果：盐酸麻黄碱进样量在0．148～0．740μg范围内与峰面积呈良好的线性关系（r=1．0000）。平均回收率为99．39％；RSD为0．92％，（n=9）。结论：本方法操作简便，结果准确可靠，适用于鼻嗅通喷雾剂中盐酸麻黄碱含量的测定。     

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.

     

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.     

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.     

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.