高效液相色谱法测定氯麻滴鼻液中氯霉素和盐酸麻黄碱的含量

目的 :建立测定氯麻滴鼻液中氯霉素和盐酸麻黄碱含量的高效液相色谱法。方法 :采用反相 μ Bondpak色谱柱 ,甲醇- 0 .0 2mol·L-1磷酸二氢钾 (5 5∶45 ,磷酸调 pH值3.5 )为流动相 ,检测波长 2 5 4nm。结果 :氯霉素和盐酸麻黄碱的线性范围分别为 2 0～ 12 0 μg·ml-1(r =0 .9998) ,80～ 480 μg·ml-1(r =0 .9998) ;加样回收率分别为 10 1.4% ,RSD =0 .5 %及 10 0 .8% ,RSD =0 .9% (n =5 ) ,日内RSD分别为 0 .9%和 0 .4% (n =5 ) ,日间RSD分别为 1.0 %和 0 .8% (n =4)。结论 :HPLC法可用于本制剂的含量测定和质量控制 ,方法简便、灵敏、结果准确     

氯霉素滴眼液及其相关物质二醇物的毛细管电泳分析法

目的　建立适合氯霉素滴眼液含量测定及其杂质二醇物检测的高效毛细管电泳定量检测方法。 方法 　采用毛细电泳法 ,以水杨酸为内标 ,运行电压 2 5 KV,运行缓冲液为 2 5 mmol· L- 1 磷酸盐缓冲液 (p H=6.0 ) ,检测波长 2 14 nm。结果 　氯霉素滴眼液及二醇物线性范围分别为 5 0～ 2 5 0 μg·ml- 1 (r=0 .9992 )和 4.0～ 2 0 .0 μg· ml- 1 (r=0 .9988)。平均回收率分别为 99.8%和 10 1.5 % ,RSD分别为 0 .8%和 2 .0 % (n=5 )。结论 　本方法能同时进行含量测定和杂质检测 ,对控制氯霉素滴眼液的质量有一定的价值     

高效液相色谱法测定血中氯胺酮浓度的改进

目的 :建立人血中氯胺酮HPLC测定法。方法 :以ODXC18(15 0mm× 4.6mm)为色谱柱 ,流动相为 2 90ml甲醇 16 0ml水 (含 0 .5ml正丁胺、0 .5ml冰醋酸 )。检测波长 2 30nm ,布比卡因为内标。结果 :本法在 0 .5～ 2 0 μg·ml-1范围内线性关系良好 (r=0 .9918) ,3种浓度的回收率分别为 93.18% ,97.2 5 % ,95 .88% ,日内日间RSD都在 (1.0～ 2 .0 ) %之间 ,血浆中最低检测限为 0 .2 5 μg·ml-1。结论 :本方法灵敏、准确 ,结果满意     

用HPLC法测定复方对乙酰氨基酚胶囊4组分的含量

目的 :采用HPLC法同时测定复方对乙酰氨基酚胶囊中对乙酰氨基酚、盐酸伪麻黄碱、咖啡因、和马来酸氯苯那敏的含量。方法 :色谱柱为ODSC18,15 0mm× 4 .6mm ;流动相 :甲醇 - 0 .0 5mol/L磷酸二氢钾 三乙胺 (15∶85∶0 .0 2 ) ,用磷酸调pH至 3.4 ,检测波长 2 15nm。结果 :线性范围分别为 :对乙酰氨基酚 5 0～ 35 0 μg·mL-1(r =0 .9997)、盐酸伪麻黄碱 6 .0～ 4 2μg·mL-1(r=0 .9938)、咖啡因 6 .0～ 4 2 μg·mL-1(r =0 .9998)、马来酸氯苯那敏 0 .6～ 4 .2 μg·mL-1(r =0 .9999)。平均回收率分别为 :对乙酰氨基酚 10 2 .3%、盐酸伪麻黄碱 10 0 .9%、咖啡因 10 1.8%、马来酸氯苯那敏 10 1.5 %。结论 :本法分离度好 ,快速 ,简便 ,可同时测定该胶囊中的四组分。     

高效液相色谱法测定对乙酰氨基酚口服溶液的含量

目的 　建立高效液相色谱法测定对乙酰氨基酚口服溶液中对乙酰氨基酚的含量 ,方法 　 Alltech-C1 8柱为固定相 ,甲醇 -水 (2 0∶ 80 )为流动相 ,检测波长 :2 44 mm,用外标法定量。 结果 　线性范围 :对乙酰氨基酚在 12 μg· m L- 1～ 12 0 μg· m L- 1浓度范围呈良好线性关系。 A=-13 5 0 2 .760 8+ 783 0 4.5 789C,r=0 .999。测得 3批的回收率分别为 98.7%、98.5 %、97.8% ,RSD分别为 0 .5 9%、0 .64 %、0 .42 %。结论 　本法简便快捷、结果准确 ,适用于对乙酰氨基酚口服溶液的含量测定。     

RP-HPLC法测定甲硝唑氯霉素凝胶中2种成分的含量

目的　建立高效液相色谱法测定甲硝唑氯霉素凝胶制剂中甲硝唑、氯霉素含量的方法。方法　用ODS C18柱 ;流动相为甲醇 水 (5 0∶5 0 ) ;检测波长 2 77nm。结果　甲硝唑的线性范围 :19 94～ 179 5 μg·ml 1(r=0 9998) ,平均回收率 10 0 8% ,RSD为 1 6 7% ;氯霉素的线性范围 :2 0 30～ 182 7μg·ml 1(r=0 9998) ,平均回收率 98 2 % ,RSD为 1 5 0 %。结论　本方法分离度好 ,快速 ,简便     

HPLC法同时测定复方诺氟沙星滴鼻液中的诺氟沙星和盐酸麻黄碱

目的　建立一种快速、准确的高效液相色谱法同时测定诺氟沙星 ( NOR)和盐酸麻黄碱 ( EPH)的含量。 方法　使用 C1 8色谱柱 ,流动相为乙腈— 0 .1%磷酸 ( 15 :85 V/V) ,检测波长为 2 5 6nm。结果 　样品测定在 9min内完成。诺氟沙星在 10～ 60μg· ml- 1 浓度范围内 ,r=0 .9999,RSD= 0 .46% ,平均回收率为 99.91% ;盐酸麻黄碱在 2 5～ 12 5 μg· ml- 1浓度范围内 ,r=0 .9992 ,RSD=0 .5 1% ,平均回收率为 10 0 .0 3%。 结论 　方法可快速准确地检测复方诺氟沙星滴鼻液中的诺氟沙星和盐酸麻黄碱含量     

抗癫痫药拉莫三嗪的血药浓度测定及动物的药代动力学研究

目的 :测定血清中拉莫三嗪的浓度及动物的药代动力学研究。方法 :采用HPLC ,以苯乙酮为内标 ,甲醇 KH2 PO4 ( 0 .0 5mol·L 1,pH 3.8)为流动相 ,经YWGODS柱 ( 2 0 0mm× 3.6mm)分离 ,30 5nm波长的二极管阵列检测器检测。取家兔以 2 5mg·kg 1经胃给药 ,设定时间抽血 ,测定动物药代动力学参数。结果 :浓度在 0 .2 5～ 5 0 μg·ml 1范围内线性良好 (r=0 .9998) ,平均回收率为 93 78%± 2 6 6 % ,日内RSD和日间RSD分别为 2 4% (n =9)和 5 3% (n =5 )。动物血药浓度 时间曲线经 3p87药代动力学程序包拟合 ,结果Cmax=9.34 μg·ml 1,t1/ 2 (ke) =8.78h ,CL/f(s)为0 .6 9L·h 1。结论 :抗癫痫药拉莫三嗪在动物实验中属一级动力学二房室模型     

高效液相色谱法同时测定滴鼻剂中盐酸麻黄素和氢化可的松的含量

目的 :用HPLC法同时测定滴鼻剂中盐酸麻黄素氢化可的松的含量。方法 :采用C18色谱柱 ,流动相为甲醇 0 .0 5mol·L-1KH2 PO4 三乙胺 (5 0∶5 0∶0 .2 ) ,用磷酸调 pH3.7,检测波长 2 5 7nm。结果 :盐酸麻黄素在 36 0～ 6 0 0 μg·ml-1浓度范围内线性关系良好 (r =0 .9999) ,回收率 10 1.3% ,RSD为 1.0 %。氢化可的松在 36～ 6 0 μg·ml-1浓度范围内线性关系良好 (r =0 .9998) ,回收率 10 1.5 % ,RSD为 1.0 %。结论 :该方法可同时测定滴鼻剂中盐酸麻黄素氢化可的松含量。     

RP-HPLC法测定复方甲硝唑片中甲硝唑和维生素B_6的含量

目的 :建立RP HPLC法测定复方甲硝唑片中甲硝唑和维生素B6的含量。方法 :采用Shim packCLC ODS柱 (4 .6mm× 2 0 0mm ,5 μm) ,甲醇 水 (30∶70 )为流动相 ,2 90nm为检测波长 ,外标法测定含量。 结果 :甲硝唑和维生素B6的线性范围分别为 5 0～ 5 0 0 μg·ml-1(r=0 .9996 ) ,5～ 5 0 μg·ml-1(r =0 .9998) ,平均回收率分别为 10 0 .2 % (RSD =0 .93% ) ,99.5 %(RSD =0 .4 2 % ) ,n =6。结论 :RP HPLC法测定复方甲硝唑片中甲硝唑和维生素B6的含量 ,方法准确 ,操作简便 ,结果可靠。     

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.

     

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.     

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.     

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.     

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.