反相高效液相色谱法测定复方庆大霉素膜中盐酸丁卡因的含量

目的建立高效液相色谱法测定复方庆大霉素膜中盐酸丁卡因含量的方法。方法色谱柱：phenomenex Gemini C18110A（250×4.60mm）,5μ;流动相：乙腈-0.1mol·L^-1醋酸钠缓冲液（用冰醋酸调pH为7.50）（75∶25）;流速：1.0mL·min^-1;检测波长：306nm。结果盐酸丁卡因浓度在4.87～29.23μg·mL^-1范围内与峰面积呈良好的线性关系,回归方程为：y=103612x＋1830.4,R^2=1;平均回收率为99.57%,RSD=0.57%（n=9）。结果该方法简便、快速、准确、灵敏度高,适用于复方庆大霉素膜中盐酸丁卡因的含量测定。     

HPLC法测定复方庆大霉素膜中盐酸丁卡因和醋酸地塞米松的含量及含量均匀度

目的:建立高效液相色谱法同时测定复方庆大霉素膜中盐酸丁卡因和醋酸地塞米松的含量及含量均匀度。方法:色谱柱为Waters Sunfire C18(4.6 mm×150 mm,5μm),流动相为1%三乙胺溶液(冰醋酸调节pH至7.0)-甲醇(35∶65),检测波长为240 nm,柱温25℃,流量1.0 mL.min-1。结果:盐酸丁卡因在80.54～1006.80μg.mL-1范围内线性关系良好(r=1),平均模拟处方回收率为101.0%,RSD为0.42%;醋酸地塞米松在2.36～29.51μg.mL-1范围内线性关系良好(r=1),平均模拟处方回收率为100.6%,RSD为0.38%。结论:方法快速简便,准确可靠,重复性好,可用于复方庆大霉素膜的质量控制。     

HPLC法测定复方地塞米松丁卡因乳膏中醋酸地塞米松和盐酸丁卡因的含量

建立复方地塞米松丁卡因乳膏中醋酸地塞米松、盐酸丁卡因含量的HPLC测定方法。色谱柱为SUNTEK Kromasil C18;流动相为甲醇-水-三乙胺(75∶25∶0.04),流速为1.0mL.min-1,检测波长为240 nm,线性范围:醋酸地塞米松2.5~20μg.mL-1,盐酸丁卡因100~800μg.mL-1,r=0.9999。平均回收率:醋酸地塞米松为100.12%,RSD为0.89%;盐酸丁卡因为98.63%,RSD为0.97%。方法准确可靠,简单易行,可用于复方地塞米松丁卡因乳膏中醋酸地塞米松、盐酸丁卡因的含量测定。     

HPLC同时测定复方硫酸新霉素药膜中盐酸丁卡因和克霉唑的含量

目的建立同时测定复方硫酸新霉素药膜中盐酸丁卡因和克霉唑含量的方法。方法采用HPLC,以Agilent HC-C18为色谱柱,流动相为甲醇-0.1%三乙胺溶液(用磷酸调pH至3.0)(85∶15),盐酸丁卡因和克霉唑的检测波长分别为311 nm和227 nm,流速0.8 mL.min 1,柱温20℃,进样20μL。结果盐酸丁卡因在2.5～50.0 mg.L 1内,峰面积与浓度呈良好的线性关系(r=0.999 5),平均回收率为99.3%,RSD=0.99%(n=9);克霉唑在5.33～106.5 mg.L 1内峰面积与浓度呈良好的线性关系(r=0.999 5),平均回收率为99.8%,RSD=1.28%(n=9)。结论本法简便、准确、重复性好,可用于复方硫酸新霉素药膜中盐酸丁卡因和克霉唑的含量测定。     

RP-HPLC法测定复方庆大霉素普鲁卡因颗粒中盐酸普鲁卡因的含量

目的建立反相高效液相色谱法测定复方庆大霉素普鲁卡因颗粒中盐酸普鲁卡因含量的方法.方法采用C18色谱柱(4.6mm×150mm,5μm),水-乙腈-三乙胺(85∶15∶0.02)(冰醋酸调pH至3.9)为流动相,流速:1.0mL·min-1,检测波长为292nm.结果盐酸普鲁卡因在20.45~204.52μg·mL-1范围内有良好的线性关系,回归方程为:A=3.6539×104C+3.1613×104(r=0.9998),平均回收率为99.60%,RSD为1.44%(n=6).结论本法快速,简便准确,可用于复方庆大霉素普鲁卡因颗粒中盐酸普鲁卡因的含量测定.     

HPLC同时测定复方盐酸丁卡因凝胶中盐酸丁卡因和乳酸依沙吖啶的含量

目的 建立高效液相色谱法同时测定复方盐酸丁卡因凝胶中有效成分盐酸丁卡因、乳酸依沙吖啶含量的方法。方法 采用Thermo Hypersil BDS C₁₈色谱柱(4.6 mm×150 mm,5 μm),以乙腈-水-三乙胺(30∶70∶0.5)为流动相,双通道检测波长为270 nm和310 nm,流速为1 mL·min^-1,进样量为10 μL。结果 盐酸丁卡因在40.0~160.0 mg·L^-1内峰面积与浓度呈良好的线性关系(r=0.999 9),平均回收率为100.2%,RSD为2.08%;乳酸依沙吖啶在38.1~152.4 mg·L^-1内峰面积与浓度呈良好的线性关系(r=0.999 8),平均回收率为99.7%,RSD为1.71%。结论 本法简便、准确、重复性好,可用于复方盐酸丁卡因凝胶中盐酸丁卡因和乳酸依沙吖啶的含量测定。     

HPLC法测定口腔溃疡液中氯霉素及盐酸丁卡因的含量

目的建立测定口腔溃疡液中氯霉素和盐酸丁卡因含量的HPLC方法.方法以十八烷基硅烷键合硅胶为填充剂;0.8%磷酸∶甲醇∶三乙胺(55∶45∶0.2)为流动相,流速1.0 ml·min-1,检测波长278 nm.结果氯霉素线性关系为Y=11091.8 13173.8X,相关系数r=0.9999(n=5),线性范围在10.16～91.44 g·L-1,平均回收率100.10%(RSD=1.22,n=6);盐酸丁卡因线性关系为Y=4186.65 10132.3X,相关系数r=0.9999(n=5),线性范围在5.98～53.82 g·L-1,平均回收率100.14%(RSD= 1.05% ,n=6).结论该法操作简便、准确,可作为口腔溃疡液中氯霉素和盐酸丁卡因含量的质量控制方法.     

紫外分光光度法测定盐酸丁卡因含量

目的建立紫外分光光度法测定复方盐酸丁卡因含漱液中的盐酸丁卡因含量,有效控制药品质量。方法利用盐酸丁卡因最大吸收波长,在311nm处紫外分光光度法测定含量。结果盐酸丁卡因含量测定方法的线性范围为1～9μg·mL-1,其回归方程为y=0.076x 0.0045(n=5,r=1.0000),平均回收率为101.3%,RSD为0.78%(n=9)。在测定波长处空白溶液对盐酸丁卡因测定无干扰,样品溶液在7h内稳定。结论本法快速,简便,重现性好,可用于复方盐酸丁卡因含漱液的质量控制。     

高效液相色谱法同时测定复方甲硝唑散中甲硝唑、盐酸丁卡因及醋酸地塞米松的含量

目的:建立以高效液相色谱法同时测定复方甲硝唑散中甲硝唑、盐酸丁卡因及醋酸地塞米松含量的方法。方法:色谱柱为C18,流动相为甲醇-水-三乙胺(65∶35∶0.36),检测波长甲硝唑、盐酸丁卡因为310nm,醋酸地塞米松为240nm,流速为1ml/min,柱温为25℃。结果:甲硝唑、盐酸丁卡因、醋酸地塞米松进样量分别在0.412μg~2.06μg(r=0.9999)、0.191μg~0.956μg(r=0.9999)、0.121μg~0.604μg(r=0.9998)范围内线性关系良好;平均回收率分别为100.69%(RSD=1.28%)、101.37%(RSD=0.23%)、102.40%(RSD=0.89%)。结论:本方法简便、准确,重现性好,可用于复方甲硝唑散的质量控制。     

反相高效液相色谱法同时测定盐酸丁卡因胶浆中2组分的含量

目的:建立以反相高效液相色谱法同时测定盐酸丁卡因胶浆中盐酸丁卡因和羟苯乙酯含量的方法。方法:色谱柱为C8,流动相为甲醇-无水乙醇-水-三乙胺(70∶15∶15∶0.05) ,检测波长为280nm。结果:盐酸丁卡因与羟苯乙酯的检测浓度线性范围分别为10～50μg/ml(r=0. 9997)、2～10μg/ml(r=0 .9999) ;平均回收率分别为100.82 %、100.16 %。结论:本方法简便、快速、准确,适用于盐酸丁卡因胶浆的质量控制。     

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.