复方环丙沙星喷鼻剂的制备

本文采用紫外分光光度法测定复方环丙沙星喷鼻剂中环丙沙星的含量和旋光法测定盐酸麻黄碱的含量,环丙沙星平均回收率为100.36%,RSD为1.68%;盐酸麻黄碱平均回收率为100.52%,RSD为0.55%.     

复方环丙沙星喷鼻剂的制备

目的;介绍复方环丙沙星喷鼻剂的制备和质量控制。方法：采用紫外分光光度法测定环丙沙星的含量,旋光法测定盐酸麻黄碱的含量。结果：该方法操作方便,结果准确,平均回收率为100.1％,RSD为0.9%.     

复方环丙沙星喷鼻剂的制备

本采用紫外分光光度法测定复方环丙沙星喷鼻剂中环丙沙星的含量和旋光法测定盐酸麻黄碱的含量,环丙沙星平均回收率为100.36%,RSD为1.68％;盐酸麻黄碱平均回收率为100.52%,RSD为0．55％。     

复方加麻喷鼻剂的制备与临床应用

目的研制复方加麻喷鼻剂并观察其治疗过敏性鼻炎、急慢性鼻炎、慢性鼻窦炎的临床疗效。方法以壳聚糖为辅料，加替沙星、盐酸麻黄碱为主药，制备复方加麻喷鼻剂，采用紫外分光光度法和旋光度法分别测定加替沙星和盐酸麻黄碱的含量，并对157例门诊患者进行临床疗效观察。结果加替沙星和盐酸麻黄碱的平均回收率分别为100.89%(RSD＝1.10%)和99.90%(RSD＝0.70%)。临床应用总有效率96.5%。结论该复方加麻喷鼻剂配方合理，制备简单，临床疗效显著。     

复方环丙沙星喷鼻剂含量测定方法研究

目的测定复方环丙沙星喷鼻剂中乳酸环丙沙星、盐酸麻黄碱的含量。方法用紫外分光光度法测定乳酸环丙沙星含量,溶剂为0．05mol／L氢氧化钠溶液,测定波长为334nm;用旋光法测定盐酸麻黄碱。结果乳酸环丙沙星质量浓度在6～18μg／mL范围内与吸收度呈良好的线性关系。乳酸环丙沙星、盐酸麻黄碱平均回收率分别为99．64％和100．27％,RSD分别为0．42％和0．58％（n=6）。结论方法简便、准确、灵敏度高、重现性好,可用于该制剂的质量控制。     

HPLC法同时测定复方苯海拉明麻黄碱糖浆三组分的含量

目的建立HPLC法同时测定复方苯海拉明麻黄碱糖浆中盐酸苯海拉明、盐酸麻黄碱和枸橼酸喷托维林的含量。方法采用HPLC法,色谱柱为AgilentC18柱,以乙腈和0.5%三乙胺（用磷酸调节pH=3.0）为流动相,流速1.0mL·min^-1,梯度洗脱;检测波长210nm;外标法定量。结果盐酸苯海拉明在20.50～205.00μg·mL^-1围内呈良好线性关系（r=0.99999）,回收率为100.21%,RSD=0.57%;盐酸麻黄碱在19.95～199.50μg·mL^-1围内呈良好线性关系（r=0.9999）,回收率为100.14%,RSD=0.94%;枸橼酸喷托维林在15.75～157.50μg·mL^-1围内呈良好线性关系（r=0.9999）,回收率为99.83%,RSD=0.64%。结论本方法灵敏可靠,结果准确,可用于复方苯海拉明麻黄碱糖浆的质量控制。     

复方氨茶碱口服溶液中盐酸麻黄碱含量测定

目的建立测定复方氨茶碱口服溶液中盐酸麻黄碱含量的高效液相色谱法。方法采用Waters C18柱（250 mm×4.6 mm,5μm）,流动相为乙腈-0.2%磷酸溶液（5∶95）,流速为1.0 mL/min,检测波长为210 nm,柱温为35℃。结果盐酸麻黄碱质量浓度在6.11～305.60μg/mL内与峰面积线性关系良好（r=1.000 0）,平均回收率为99.92%,RSD为0.58%（n=6）。结论该方法准确、简便,可用于测定复方氨茶碱口服溶液中盐酸麻黄碱的含量。     

HPLC法测定三拗片中盐酸麻黄碱和盐酸伪麻黄碱的含量

目的建立HPLC法测定三拗片中盐酸麻黄碱与盐酸伪麻黄碱总含量的方法。方法选用极性乙醚连接苯基键合硅胶为填充剂的phemomenex synergi Polar-RP色谱柱(250 mm×4.6 mm,4μm);以甲醇-0.9 g.L-1磷酸溶液(含体积分数0.04%三乙胺和体积分数0.02%二正丁胺)(1.5∶98.5)为流动相;流速:0.8 mL·min-1;检测波长:210 nm;进样量:5μL;柱温:30℃。结果盐酸麻黄碱在4.97~99.44μg.mL-1范围内线性关系良好,平均回收率为100.7%,RSD为0.5%(n=6);盐酸伪麻黄碱在2.01~60.30μg.mL-1范围内线性关系良好,平均回收率为101.9%,RSD为0.8%(n=6)。结论该方法简便、准确、重复性好,可作为三拗片的质量控制方法。     

HPLC法测定复方软甲膏中水杨酸和盐酸丁卡因的含量

目的:建立测定复方软甲膏中水杨酸和盐酸丁卡因含量的HPLC法.方法:色谱柱为Agilent-C18(4.6 mm×150 mm,5μm);流动相为甲醇-水-磷酸(50:50:0.04),流速1.0 mL/min,检测波长313 nm.结果:水杨酸溶液在82.00～410.00μg/mL时与其吸收值呈良好线性关系(r=0.999 9),平均加样回收率99.80%,RSD=1.68%;盐酸丁卡因溶液在5.00～25.00μg/mL时与其吸收值呈良好线性关系(r=0.999 9),平均加样回收率99.75%,RSD=1.36%.结论:本方法操作简便、快捷,结果准确、可靠,适用于复方软甲膏的质量控制.     

高效液相色谱法测定复方呋喃西林滴鼻液中主药的含量

目的:建立高效液相色谱法(HPLC)测定复方呋喃西林滴鼻液中呋喃西林和盐酸麻黄碱的含量.方法:采用HPLC,Agilent Eclipse×OB-C8色谱柱,乙腈:0.05 mol·L-1磷酸二氢钾溶液(22:78)为流动相,检测波长为255 nm.结果:呋喃西林在8～32μg·ml-1浓度范围内,盐酸麻黄碱在400～1600μg·ml-1浓度范围内,峰面积与浓度呈良好的线性关系,其相关系数分别为r=0.999 8和r=0.999 9,呋喃西林的平均回收率为99.66%(RSD为0.68%),日内RSD为0.38%;日间RSD为1.25%;盐酸麻黄碱的平均回收率为99.90%(RSD为0.44%),日内RSD为0.29%,日间RSD为1.12%.结论:本法简便、快速、结果准确,可用于测定复方呋喃西林滴鼻液的含量.     

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.