氢溴酸加兰他敏分散片的研究

目的　研究氢溴酸加兰他敏分散片的处方组成及制备工艺。方法　制备氢溴酸加兰他敏分散片 ,制定质量控制标准 ,采用高效液相色谱法测定其含量、溶出度 ,并考察其稳定性。结果　氢溴酸加兰他敏分散片稳定性较好 ,质量控制方法可行 ,高效液相色谱法测定该片含量的平均回收率为 10 0 2 % (RSD为 1 4 5 % )。结论　本品处方合理 ,工艺成熟 ,质量稳定 ;为临床治疗老年性痴呆症提供了一种易于服用且奏效较快的新制剂。     

紫外分光光度法测定溴吡斯的明片中溴吡斯的明的含量

目的:建立测定溴吡斯的明片中溴吡斯的明含量的方法。方法:采用紫外分光光度法,以去离子水为空白,在269nm波长处测定溴吡斯的明的含量。结果:溴吡斯的明检测浓度在16.56～41.40μg·mL-(1r=0.9999)范围内与吸光度呈良好的线性关系;平均回收率为99.87%,RSD=0.19%(n=9)。结论:该法操作简便、精密度好、结果可靠,适用于溴吡斯的明片中溴吡斯的明含量的快速测定。     

复方头孢克洛片制备及稳定性考察

目的 研究复方头孢克洛片的处方和制备工艺.方法 配制复方头孢克洛片,并制定质量标准,采用高效液相色谱法测定含量及进行稳定性考察.结果 以该处方工艺制成的片剂,质量可控,稳定性较好.结论 本品处方工艺成熟,质量可控,稳定性较好.     

注射用丁溴东莨菪碱的制备及稳定性考察

目的:探讨注射用丁溴东莨菪碱的处方组成、制备工艺、测定方法及稳定性。方法:以甘露醇为填充剂,制备注射用丁溴东莨菪碱;采用高效液相色谱法测定其含量和有关物质。结果:最佳处方为主药20mg,甘露醇20mg;高温、强光对本品均有不利影响;密闭,在凉暗干燥处保存2年无明显变化。结论:经中试放大制备的注射用丁溴东莨菪碱性质稳定、质量可控。     

注射用丁溴东茛菪碱的制备及稳定性考察

目的:探讨注射用丁溴东莨菪碱的处方组成、制备工艺、测定方法及稳定性.方法:以甘露醇为填充剂,制备注射用丁溴东莨菪碱;采用高效液相色谱法测定其含量和有关物质.结果:最佳处方为主药20 mg,甘露醇20mg;高温、强光对本品均有不利影响;密闭,在凉暗干燥处保存2年无明显变化.结论:经中试放大制备的注射用丁溴东莨菪碱性质稳定、质量可控.     

氢溴酸加兰他敏分散片的研究

目的 研究氢溴酸加兰他敏分散片的处方组成及制备工艺。方法 制备氢溴酸加兰他敏分散片，制定质量控制标准，采用高效液相色谱法测定其含量、溶出度，并考察其稳定性。结果 氢溴酸加兰他敏分散片稳定性较好，质量控制方法可行，高效液相色谱法测定该片含量的平均回收率为100．2％(RSD为1．45％)。结论 本品处方合理，工艺成熟，质量稳定；为临床治疗老年性痴呆症提供了一种易于服用且奏效较快的新制剂。     

替莫唑胺分散片的制备及其稳定性研究

目的：研究替莫唑胺分散片的处方和制备工艺。方法：对配制的替莫唑胺分散片采用高效液相色谱法测定含量，并进行稳定性考察。结果：以该处方、工艺制成的片剂，质量可控，稳定性较好。结论：本品处方工艺成熟，质量稳定。     

溴吡斯的明缓释片的含量测定

目的:建立以紫外分光光度法测定溴吡斯的明缓释片中溴吡斯的明的含量。方法:以去离子水为空白,269nm为检测波长,测定溴吡斯的明的含量。结果:溴吡斯的明在16.56～41.40mg.L-1范围内浓度与吸光度呈良好的线性关系(r=0.999 9),平均回收率为99.91%。结论:本方法操作简便、准确、重现型好,可为完善该制剂的质量标准提供依据。     

微流控芯片非接触电导检测法测定溴吡斯的明片中溴吡斯的明的含量

目的:建立测定溴吡斯的明片中溴吡斯的明含量的方法。方法:采用微流控芯片非接触电导检测法。在高电场强度条件下利用微流控芯片上特殊的微通道实现组分快速、高效的分离,以非接触电导检测器进行检测;分析缓冲液种类和浓度、添加剂种类和浓度、分离电压和进样时间等因素对分离检测的影响。结果:优化选择1 mmol.L-1 HAc+1 mmol.L-1 NaAc(pH 4.5)缓冲溶液、不加添加剂、分离电压1.80 kV、进样时间10 s时,2 min内可实现溴吡斯的明片中溴吡斯的明含量快速检测。在优化条件下,溴吡斯的明的检测浓度线性范围为10～100μg.mL-1(r=0.999 7),检出限为0.6μg.mL-(1S/N=3),RSD=1.9%,加样回收率为96.6%～100.3%。结论:本方法简便快速,重复性好,可用于溴吡斯的明片的快速检测和药品生产质量控制。     

注射用氟康唑的制备工艺及稳定性研究

目的:筛选注射用氟康唑的制备工艺,建立其含量测定方法。方法:以pH值及助溶剂种类等为考察因素筛选处方;采用高效液相色谱法测定其含量。结果:溶液pH在6.5～8.5时制剂稳定性较好,且丙二醇可增加制剂澄明度;氟康唑检测浓度在40～200μg/ml范围内线性关系良好,平均回收率为100.37%,RSD=1.37%(n=3)。结论:按照筛选出的处方、工艺制备的注射用氟康唑质量稳定,含量测定方法准确、可行。     

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.