正交试验优选松针滴丸制备工艺

目的:优选松针滴丸的制备工艺。方法:以药物与基质配比、基质种类、滴制温度、冷却剂温度为考察因素,以丸重变异系数、溶散时限、外观质量的综合评分为评价指标,采用正交试验优选滴丸的处方和成型工艺。结果:滴丸制备的最佳条件为药物与基质的配比1∶4,基质为PEG4000与PEG6000(1∶1),滴制温度为80℃,冷却剂温度为10℃。结论:该工艺制得的滴丸丸重差异小、溶散时间短、综合质量好。     

盐酸小檗碱滴丸成型工艺的研究

目的研究影响盐酸小檗碱滴丸成型的各种因素,确立最佳成型工艺。方法以滴丸的溶散时限、外观质量及丸重差异等作为综合评定指标,优选出滴丸的处方和成型工艺。结果盐酸小檗碱滴丸制备过程的最佳工艺条件为:以PEG1000+PEG4000(1∶1)为基质,药物-基质以1∶4配比,料温95℃,二甲基硅油为冷却剂,冷却液温度为5℃,滴制口径3mm,滴速为50滴.min-1,滴距6cm为最佳条件。结论该成型工艺成品率高,符合滴丸的质量要求,可用于盐酸小檗碱滴丸制备。     

盐酸川芎嗪滴丸制备工艺研究

目的研究影响滴丸成型的各种因素,确立最佳成型工艺。方法以滴丸的溶散时限、外观质量及丸重差异等作为综合评定指标,优选出滴丸的处方和成型工艺。结果盐酸川芎嗪滴丸最佳滴制工艺条件为,以PEG4000+PEG6000(1∶1)为基质,基质与药物配比为5∶1,滴制温度90℃,二甲基硅油为冷却剂,滴速为40滴/min,滴距8 cm为最佳条件。结论该工艺简便、可行,评价指标可靠、合理,符合2010年版《中国药典》对滴丸制剂的要求。     

山楂叶总黄酮滴丸的制备工艺优化

目的:确立山楂叶总黄酮滴丸的最佳成型工艺.方法:采用正交试验法,以滴丸的外观质量、溶散时间以及滴丸的重量差异系数为评价指标,优选药物与基质的配比、混合基质配比、药液的温度以及冷却剂温度,确定最佳滴制条件.结果:最佳条件为山楂叶总黄酮与基质比为1∶5,混合基质配比PEG 4000∶PEG 6000=1∶2,药液温度为85℃,冷却剂温度为10℃.结论:本方法确定的山楂总黄酮滴丸制备工艺稳定可行.     

复方灵芝滴丸制备工艺研究

目的:研究复方灵芝滴丸的制备工艺。方法:采用滴制法制备复方灵芝滴丸,以聚乙二醇(PEG)6000与PEG4000比例、中间品与基质比例、液体石蜡与二甲硅油比例为考察因素,以滴丸的丸重变异系数、外观质量及溶散时限的综合评分作为评价指标,采用正交试验优选滴丸的处方;采用单因素方法,以滴制、成型情况优劣考察滴丸的滴制工艺。结果:最佳滴丸处方为PEG6000与PEG4000比例1∶1,液体石蜡与二甲硅油比例1∶3,中间品与基质的比例1∶2.5;滴制温度为80℃,滴距为6cm,滴速为26滴·min-1,冷却距离为60cm,冷却温度为2～3℃。结论:选取的处方及滴制工艺合理、简便,适用于本制剂的制备。     

苯巴比妥滴丸的制备工艺研究

目的　以水溶性高分子材料PEG - 6 0 0 0和PEG - 4 0 0 0为基质 ,研究苯巴比妥滴丸的最佳制备工艺。方法　通过对苯巴比妥滴丸制备过程的实验 ,以滴丸的成型、圆整度、重量差异为筛选指标 ,以药液的保温温度、滴制速度、药物与基质的最佳配比为主要考察因素 ,对苯巴比妥滴丸的制备工艺进行优选 ,并讨论了影响滴丸成型、圆整度及丸重差异的其他因素。结果　药物与基质的最佳配比为 1∶5、药液保温温度为 90～ 95℃、滴制速度为 5 0drops·min-1,为最佳制备工艺条件。按照此优化条件制备的苯巴比妥滴丸成型率最高。结论　此制备工艺设备简单 ,操作方便 ,不仅适合于苯巴比妥滴丸的制备 ,也同样适合于其他滴丸产品的实验室制备及工业化生产     

山红调脂滴丸的制备工艺研究

目的：研究影响山红调脂滴丸制备工艺的各种因素,确立最佳制备工艺。方法：采用正交设计试验方法,以溶散时限、圆整度为指标确定滴丸的处方工艺,以丸重合格率为指标筛选滴丸滴制条件。结果：最佳工艺为滴制温度为85℃,PEG4000与PEG6000比例为1：1,药物与基质的比例为1：5,冷却温度10℃,滴距10cm,滴速20～30滴／min。结论：制得的滴丸溶散时限、圆整度及丸重均符合质量要求,该工艺合理、简便。     

盐酸青藤碱滴丸的制备工艺及质量研究

目的优选盐酸青藤碱滴丸的最佳制备工艺并控制其质量。方法以滴丸的溶散时限、硬度、成型情况作为综合评定指标,对药液温度、基质配比(PEG4000∶PEG6000)、药物与基质的比例、及滴制过程中滴速进行正交实验设计,优选滴丸最佳制备工艺。采用高效液相色谱法测定盐酸青藤碱滴丸中盐酸青藤碱的含量。结果最佳制备工艺为药液温度为75℃,PEG4000∶PEG6000为1∶4,药物基质比为1∶3,滴速为60滴.min 1,冷凝液为二甲基硅油。盐酸青藤碱在0.2~1.0μg.mL 1内呈良好的线性关系,r=0.999 5,平均回收率为99.3%,RSD为1.2%。结论本试验制得的滴丸溶散时限、外观及丸重均符合质量要求,制备方法简便可行。含量测定方法操作简便、专属性强、重复性好、结果准确可靠,可用于盐酸青藤碱滴丸的质量控制。     

黄芩苷滴丸成型工艺考察

目的:研究黄芩苷滴丸的制备工艺。方法:以滴丸的圆整度、滴制时的拖尾情况、溶散时限、硬度等为指标,对基质、药物与基质的配比、熔融的温度、滴制温度、冷却剂、冷却温度及冷凝柱的长度进行考察。结果:滴丸最佳制备工艺为最佳基质PEG 6000,药(黄芩苷-PVPK30固体分散体)-基质(质量比)(1∶5),熔融温度为80～90℃,滴制温度为85～90℃,冷凝剂为液体石蜡和植物油1∶1的混合物,冷凝液的温度在10℃左右,冷凝柱长为40 cm。结论:优选得到的黄芩苷滴丸成型工艺稳定可行。     

复方咽扁滴丸制备工艺研究

目的:研究影响复方滴丸成型的各种因素,确立最佳制备工艺.方法:以滴丸的溶散时限、丸重差异等作为综合评定指标,采用正交设计实验的方法,优选出滴丸的处方和成型工艺.结果:复方咽扁滴丸最佳滴制工艺条件为:以PEG6000为基质,基质与药物配比为4:1,滴制温度85℃,二甲基硅油为冷却剂,滴速50滴/min,滴管温度60℃为最佳制备工艺.结论:该工艺简便、易行,评价指标可靠、合理.符合2010年版<中国药典>对滴丸制剂的要求.     

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.