HPLC法测定苍鹅鼻炎胶囊中马来酸氯苯那敏的含量

目的建立高效液相色谱法测定苍鹅鼻炎胶囊中马来酸氯苯那敏的含量的方法。方法采用DiamonsilC18(250mm×4.6mm,5μm)柱:乙腈-0.2%十二烷基硫酸钠溶液-磷酸(50∶50∶0.1)为流动相;流速:1.0ml/min;检测波长为225nm。结果马来酸氯苯那敏线性范围为0.1238～0.2890μg(r=0.9999),平均回收率为99.3%,RSD=0.4%(n=6)。结论该方法简便,准确,可控制苍鹅鼻炎胶囊中马来酸氯苯那敏的含量。     

HPLC法同时测定顺气化痰片及顺气化痰颗粒中氨茶碱和马来酸氯苯那敏的含量

目的:为控制顺气化痰片及顺气化痰颗粒质量,建立高效液相色谱法同时测定顺气化痰片及其颗粒剂中氨茶碱和马来酸氯苯那敏的含量。方法:采用C18(150 mm×4.6 mm,5μm)色谱柱,流动相为甲醇-0.05 mol.L-1磷酸二氢钠(40∶60,用磷酸调节pH 3.5),流速1.0 mL.min-1,检测波长275 nm(茶碱)、264 nm(马来酸氯苯那敏)。结果:茶碱的线性范围为2.03～101.4μg.mL-1(r=0.9998);马来酸氯苯那敏的线性范围为1～50μg.mL-1(r=0.9998)。片剂中茶碱的平均回收率为99.4%,RSD=2.0%;马来酸氯苯那敏的平均回收率为99.8%,RSD=0.84%;颗粒剂中茶碱的平均回收率为101.5%,RSD=1.6%;马来酸氯苯那敏的平均回收率为99.9%,RSD=0.89%。结论:该方法简便、灵敏、准确,适用于顺气化痰片剂及颗粒剂中氨茶碱和马来酸氯苯那敏的同时测定及该品种的质量控制。     

RP-HPLC法测定咳特灵胶囊中马来酸氯苯那敏的含量

目的建立反相高效液相色谱法测定咳特灵胶囊中马来酸氯苯那敏的含量。方法采用C18柱(250 mm×4.6 mm,5μm)为色谱柱;流动相:甲醇-0.025 mol·L-1磷酸二氢钾溶液(含10 mL·L-1三乙胺,用磷酸调pH3.0)(50∶50);流速为1.0 mL·min-1;检测波长为262 nm。结果马来酸氯苯那敏质量浓度在4.60~115.00 mg·L-1范围内呈线性关系,其回归方程为Y=20.404X+22.29,r=1.000 3,平均回收率为99.7%,RSD为1.6%(n=6)。结论方法简便准确,重复性好,灵敏度高,可用于咳特灵胶囊中马来酸氯苯那敏的含量测定。     

HPLC法测定小儿氨酚黄那敏颗粒中二组分的含量及马来酸氯苯那敏含量均匀度考察

目的:应用HPLC测定小儿氨酚黄那敏颗粒中对乙酰氨基酚与马来酸氯苯那敏的含量,并对马来酸氯苯那敏的含量均匀度进行考察。方法:采用ODS柱(大连依利特250mm×4.5mm,5μm),以甲醇-0.5mol·ml-1磷酸二氢钠-三乙胺(150∶850∶0.25),用磷酸调节pH为2.3为流动相,检测波长215nm。结果:平均回收率(n=3)对乙酰氨基酚为99.5%(RSD=0.3%),马来酸氯苯那敏96.8%(RSD=0.4%)。结论:该方法快速准确,能更好地控制产品质量。     

氨咖黄敏胶囊中马来酸氯苯那敏的质量控制情况评价

目的建立氨咖黄敏胶囊胶囊中马来酸氯苯那敏的含量测定及含量均匀度检查方法,对9个厂家生产的氨咖黄敏胶囊中马来酸氯苯那敏的质量控制情况进行比较。方法高效液相色谱法,菲罗门Gemin-i C18(250mm×4.6mm,5μm),流动相:以磷酸盐缓冲液(磷酸二氢铵11.5g,加水溶解,加H3PO41mL,加水至1000mL)-乙腈(82∶18)为流动相,检测波长为262nm。结果马来酸氯苯那敏的线性范围为8.12～162.47mg·mL-1,r为0.9999。平均回收率为98.9%(RSD=0.8%)。结论经过质量比较说明,有必要对咖黄敏胶囊中马来酸氯苯那敏进行控制。     

HPLC法测定复方抗感片中对乙酰氨基酚和马来酸氯苯那敏的含量

目的测定复方抗感片中对乙酰氨基酚和马来酸氯苯那敏含量。方法HPLC,以乙腈-水-三乙胺(150∶850∶15)(用磷酸调节pH值至2.8±0.1)为流动相;采用C18柱,检测波长为265nm。结果对乙酰氨基酚及马来酸氯苯那敏分别在160.2~720.9μg.mL-1及2.8~14.0μg.mL-1范围内线性关系良好,相关系数分别r=0.9998,r=0.9999(n=8);对乙酰氨基酚及马来酸氯苯那敏的平均回收率分别为101.00%、RSD=0.96%,100.39%、RSD=1.45%。结论建立HPLC法可作为本品的定量分析方法。     

HPLC法测定氨咖黄敏胶囊中马来酸氯苯那敏的含量

目的 建立测定氨咖黄敏胶囊中马来酸氯苯那敏含量的方法.方法 色谱柱为VP-ODS柱,流动相为甲醇-0.05 moL? L1磷酸二氢钾溶液(含三乙胺0.03％,用磷酸调pH至3.0)(43∶57),检测波长为215 nm,柱温为40℃,流速为1.0 mL?min-1.结果 马来酸氯苯那敏在20.24～48.57μg?mL-1浓度范围内线性关系良好,r=0.9998;平均回收率为99.78％,RSD=0.67％.结论 该方法专属性好,简捷、快速、准确,适用于氨咖黄敏胶囊中马来酸氯苯那敏含量的测定.     

HPLC法测定金感胶囊中马来酸氯苯那敏的含量

目的 应用HPLC法测定金感胶囊中马来酸氯苯那敏的含量.方法 采用HPLC法.色谱柱为C18柱;流动相为乙腈-磷酸盐缓冲液;检测波长为262nm;流速为1.0mL·min-1;柱温为30℃.结果 马来酸氯苯那敏在规定范围内线性关系良好,平均加样回收率符合要求,RSD符合要求.结论 该法简便快速,重复性好,灵敏度高,结果准确,可用于金感胶囊中马来酸氯苯那敏的含量的测定.     

高效液相色谱法测定小儿氨酚黄那敏颗粒中马来酸氯苯那敏含量及均匀度

目的 建立小儿氨酚黄那敏颗粒中马来酸氯苯那敏含量及均匀度的检测方法。方法 采用高效液相色谱法对小儿氨酚黄那敏颗粒中的马来酸氯苯那敏含量及均匀度进行测定。以shimpack VP-ODS(150 mm×4.6 mm,5 μm)色谱柱为固定相;甲醇-0.01 mol·L-1辛烷磺酸钠溶液(三乙胺调节pH值至3.0,63∶37)为流动相;流速为1 mL·min-1;检测波长为261 nm;进样量为10 μL。结果 马来酸氯苯那敏在7.928~31.712 mg·L-1的范围与峰面积呈良好线性关系,r=0.999 92。样品中马来酸氯苯那敏的平均回收率为99.8%(n=9,RSD=0.83%)。用该文建立的方法对5个批次小儿氨酚黄那敏颗粒中的马来酸氯苯那敏含量及均匀度进行了测定,其含量均为标示量的90.0%～110.0%,均匀度符合规定。结论 该方法准确可靠,可作为小儿氨酚黄那敏颗粒中马来酸氯苯那敏含量及均匀度的测定方法。     

HPLC法测定咳特灵胶囊中马来酸氯苯那敏的含量

采用高效液相色谱法测定咳特灵胶囊中马来酸氯苯那敏的含量。用Diamonsil C18为色谱柱,流动相:乙腈-1%三乙胺与1%磷酸溶液(16∶84),流速:1.0 mL.min-1,检测波长:270 nm。马来酸氯苯那敏的线性范围为0.418~4.18μg(r=0.9999),平均回收率为101.44%(n=9),RSD为1.7%。本法快速、简单、准确,专属性强,分离效果好。     

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.     

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.