HPLC法测定咳喘平合剂中盐酸麻黄碱、伪麻黄碱的含量

目的建立复方制剂咳喘平合剂中麻黄碱、伪麻黄碱的含量测定方法.方法色谱柱:Diamond C18柱(4.6mm×250mm,5μm).流动相:乙腈-0.1%磷酸溶液(6∶94).流速:1.0mL?min-1,检测波长:207nm,柱温25℃,进样量10μL.结果 盐酸麻黄碱在0.1008～0.5040μg范围内呈良好线性关系,平均回收率为100.3%;盐酸伪麻黄碱在0.1015～0.5075μg范围内呈良好线性关系,平均回收率为101.1%.结论 本测定方法简便可行、重复性好,可用于咳喘平合剂中有效成分盐酸麻黄碱、伪麻黄碱的含量测定.     

RP-HPLC法测定盐酸麻黄碱糖浆的含量

以反相高效液相色谱法测定盐酸麻黄碱糖浆的含量.色谱柱为Shimpack CLC-ODS柱(Ф6.0m m×150mm,5μm),流动相为甲醇-1%醋酸铵溶液(40∶60),检测波长为256nm.结果盐酸麻黄碱在0.4～4.0/mg/ml范围内线性关系良好(r=0.9998,n=12);平均回收率为100.5%,RSD 为0.72%(n=15).方法简单,精密度高.     

RP-HPLC法测定盐酸麻黄碱糖浆的含量

以反相高效液相色谱法测定盐酸麻黄碱糖浆的含量.色谱柱为Shimpack CLC-ODS柱(Ф6.0m m×150mm,5μm),流动相为甲醇-1%醋酸铵溶液(40∶60),检测波长为256nm.结果盐酸麻黄碱在0.4～4.0/mg/ml范围内线性关系良好(r=0.9998,n=12);平均回收率为100.5%,RSD 为0.72%(n=15).方法简单,精密度高.     

HPLC法测定1％盐酸麻黄碱滴鼻剂中盐酸麻黄碱的含量

目的:建立HPLC法测定1%盐酸麻黄碱滴鼻剂中盐酸麻黄碱的含量测定方法.方法:采用C<,18>色谱柱(4.6mm×150 mm,5μm);流动相为甲醇-0.01 mol/L磷酸二氢钠(60:40);流速:1 ml/min;柱温:室温;检测波长为257 nm.结果:盐酸麻黄碱在40～400 μg/ml浓度范围内呈良好线性关系(r=0.999 9),含量测定平均回收率为101.12%,RSD为1.02%(n=9).结论:该方法分析操作简便、快速,选择性高并具有一定的灵敏度,适用于医院制剂的质量控制.     

氯卡麻滴鼻剂中氯霉素、盐酸麻黄碱和硫酸卡那霉素的含量测定

目的建立氯卡麻滴鼻剂中主药成分氯霉素、盐酸麻黄碱和硫酸卡那霉素的含量测定法,以便更好的控制其质量。方法高效液相色谱法,测氯霉素和盐酸麻黄碱,L-column C18色谱柱(250mm×4.6mm,5μm),流动相为0.02mol/L磷酸二氢钾溶液-甲醇(60:40)为流动相;检测波长254nm。流速1.0ml/min,柱温35℃,进样量为10μl;紫外分光光度法,测硫酸卡那霉素含量,测定波长530nm。结果氯霉素其检测质量浓度在25μg/ml～100μg/ml范围内与峰面积积分值的线性关系良好(r=0.9999),平均回收率为100.46%,RSD=1.2%(n=9);盐酸麻黄碱其检测质量浓度在100μg/ml～400μg/ml范围内与峰面积积分值的线性关系良好(r=0.9992),平均回收率为99.50%,RSD=0.49%(n=9);硫酸卡那霉素其检测质量浓度在0.1mg/ml～0.3mg/ml范围内与紫外吸收度的线性关系良好(r=0.9999),平均回收率为99.50%,RSD=0.97%(n=9)。结论本法简便、准确、重现性好,可用于氯卡麻滴鼻剂中各主成分含量测定。     

RP-HPLC法同时测定合剂中麻黄碱、苯海拉明的含量

目的: 用RP-HPLC法同时测定小儿麻黄碱苯海拉明合剂中盐酸麻黄碱、盐酸苯海拉明的含量.方法: 采用C18色谱柱,流动相为乙腈-0.02 mol·L-1十二烷基硫酸钠溶液-三乙胺(52∶48∶0.1),用磷酸调pH3.5,检测波长254 nm.结果: 盐酸麻黄碱、盐酸苯海拉明的线性范围分别为(0.500 8～5.008μg和0.503 2～5.032)μg,平均回收率分别为99.6%(RSD=0.8%)和100.2%(RSD=1.0%)(n=6).结论: 该法可同时测定合剂中盐酸麻黄碱、盐酸苯海拉明的含量.     

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-BDS CN柱,流动相为乙腈-0.4%乙酸铵溶液-三乙胺(30:70:0.2),流速为1.0 ml/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125～1 000μg/ml,r=0.9999,盐酸麻黄碱75～600μg/ml,r=0.9996;盐酸曲普利啶18～140 μg/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同时测定复方泼尼松龙滴鼻液中盐酸麻黄碱和醋酸泼尼松龙的含量

目的 建立HPLC测定复方泼尼松龙滴鼻液中盐酸麻黄碱和醋酸泼尼松龙两组分含量.方法 色谱柱:Hypersil ODS2(4.6 mm×250 mm,5 μm),流动相:甲醇-1%乙酸铵(用磷酸调节pH值至6.0)(52:48),检测波长:257 nm,流速:1.0ml/min,进样量:20μl.结果 盐酸麻黄碱和醋酸泼尼松龙的线性关系良好,分别为0.3972-4.9648 mg/ml和0.04022～0.5028 mg/ml,r分别为0.99997与0.99998(n=6);平均回收率分别为98.1%(RSD=0.94%,n=9)和99.7%(RSD=1.21%,n=9);制剂中其它成分无干扰.结论 二组分分离度好、辅料无干扰,本法简便、准确、重复性好,能同时测定复方泼尼松龙滴鼻液中两组分的含量.     

反相-高效液相色谱法测定黄龙止咳颗粒中盐酸麻黄碱和盐酸伪麻黄碱的含量

目的：建立反相-高效液相色谱法（RP-HPLC）测定黄龙止咳颗粒中盐酸麻黄碱和盐酸伪麻黄碱含量的方法.方法：色谱柱：AgilentZORBAXSB-C18色谱柱（4.6mm×250mm,5μm）;流动相：乙腈-磷酸二氢钾溶液（4∶96）（取磷酸二氢钾6.8g,加水1000ml溶解后,加三乙胺1ml,用磷酸调节pH值至3.0）;检测波长：210nm;柱温：35℃.结果：盐酸麻黄碱、盐酸伪麻黄碱进样量分别在0.0040～0.0480μg（r=0.9996）、0.0237～0.2844μg（r=0.9999）范围内线性关系良好;平均回收率分别为96.2％、97.5％,RSD分别为1.97％、1.81％.结论：本方法简便、准确,适用于黄龙止咳颗粒中盐酸麻黄碱和盐酸伪麻黄碱的含量测定.     

HPLC法测定复方川贝片中盐酸麻黄碱的含量

目的:采用HPLC法测定复方川贝片中盐酸麻黄碱的含量.方法:使用kromasilC18柱(200mm×4.6mm,5μm),流动相为甲醇-水(1∶1),流速为1.0ml·min-1,检测波长254nm.结果:采用反相高效液相色谱法测定复方川贝片中盐酸麻黄碱的含量,盐酸麻黄碱的线性范围为0.498～7.47μg·ml-1,r=0.9996,回收率为98.08%(RSD=2.16%).结论:本方法快速、准确,可作为该复方制剂的质量控制标准.     

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.