紫草凝胶剂的制备与质量控制

目的制备紫草凝胶剂,建立其质量控制方法。方法用正交实验法以卡波姆-940,甘油配比和凝胶pH值为因素,每因素三水平,以凝胶在55 ℃水浴中的颜色变化时间及外观性状的综合评价为指标,用L₉(3⁴)正交表进行实验,筛选出最优处方,制备紫草凝胶剂,采用紫外-可见分光光度法测定左旋紫草素的含量,用薄层色谱法进行鉴别。结果最优处方为卡波姆-940为0.7%,甘油15%,pH为6.0,凝胶制备工艺可行,其主要成分能采用薄层色谱法鉴别,其pH为5.5～6.0稳定性好,左旋紫草素的线性范围为8.2～41.0 μg·mL-1,平均回收率为99.84﹪,RSD为3.18﹪(n=9)。结论该凝胶剂制备工艺简单,质量可控,方法可靠,稳定性好。     

柏竹凝胶剂的制备

目的:制备用于防治婴幼儿尿布皮炎的柏竹凝胶剂.方法:以卡波姆-940为凝胶基质制备柏竹凝胶,建立质量标准,考察其稳定性.结果:凝胶制备工艺可行,其组成药物可采用薄层色谱法鉴别;其pH为6.0～7.0,稳定性好.结论:柏竹凝胶制备工艺简便,质量可控,稳定性好,值得推广应用.     

紫草膜剂的制备及左旋紫草素的含量测定

目的:确定并优化紫草膜剂的处方工艺,建立稳定可靠的左旋紫草素含量测定方法,对紫草膜剂进行质量控制。方法:以紫草提取物为原料药,采用聚乙烯醇为成膜材料,加入甘油、羧甲基纤维素钠制备紫草膜剂。通过单因素实验与正交试验,以膜的机械性能为评价指标,筛选优化处方工艺。采用高效液相色谱法对膜剂中主要活性成分左旋紫草素的含量进行测定。结果:PVA的种类与用量,增塑剂甘油的用量及载药量均会明显影响膜剂的成型与机械性能。优化处方中成膜材料聚乙烯醇205S与540S的用量比为1∶3,甘油的用量为7.6%,聚乙烯醇:紫草提取物为9∶1。含量测定的HPLC方法日内、日间精密度分别为0.77%与0.74%,加样回收率为99.67%(n=9),重复性好。结论:所制备的紫草膜剂含量均匀,机械性能良好,符合膜剂质量要求。     

伤疡愈凝胶的制备及质量标准研究

目的:制备伤疡愈凝胶并建立其质量标准。方法:以卡波姆940为凝胶基质制备伤疡愈凝胶。采用分光光度法在516nm波长处测定其含量;其它成分用薄层色谱法进行鉴别。结果:左旋紫草素浓度在8.048～40.24μg.mL-1范围内线性关系良好(r=0.9998),平均回收率为99.45%(RSD=1.13%)。结论:本制剂制备工艺简便,所建标准可用于质量控制。     

橘红总黄酮凝胶剂的制备工艺研究

目的：研究橘红总黄酮凝胶剂最优制备工艺。方法：以凝胶剂的涂展性和光泽度等为指标,通过正交实验法考察卡波姆940、氮酮、丙二醇、甘油的用量,优选橘红总黄酮凝胶剂的制备工艺。结果：橘红总黄酮凝胶剂的最优工艺处方为：橘红总黄酮/卡波姆940/氮酮/丙二醇/甘油=1.3%/0.8%/2%/15%/10%。结论：经过试验研究得出的制备工艺简单、稳定、可行,为橘红总黄酮凝胶剂的实际生产提供参考。     

盐酸恩丹西酮鼻用凝胶剂的制备与质量控制

目的设计盐酸恩丹西酮鼻用凝胶剂处方,并建立其质量控制方法.方法以卡波姆-940和甘油作为凝胶基质和主要辅料,用三乙醇胺调节pH值,制备盐酸恩丹西酮鼻用凝胶剂,采用紫外分光光度法对凝胶剂中盐酸恩丹西酮的含量进行测定.结果所得凝胶剂质量稳定,含量准确,盐酸恩丹西酮平均回收率为100.15%.结论该制剂制备工艺简便、稳定性好,质量控制方法简便、快速、准确.     

正交试验优选复方环丙沙星凝胶基质组成及制备工艺

目的:优选复方环丙沙星凝胶基质组成及制备工艺。方法:选取盐酸环丙沙星、卡波姆-940、甘油、三乙醇胺处方用量4种因素为可变因素,以成品稳定性为考察指标,选用L9(34)表进行正交试验。结果:最优的基质组成及工艺为盐酸环丙沙星0.3%、卡波姆-9401%、甘油7.5%、三乙醇胺2%。结论:按优选工艺制备的凝胶符合《中国药典》2000年版规定。     

紫花地丁复方止痒凝剂的处方和制备工艺优选

目的:考察紫花地丁复方止痒凝胶剂的处方和制备工艺。方法:采用L9(34)正交实验设计,考察凝胶基质种类、甘油用量、氢氧化钠用量3个因素对凝胶剂质量的影响,以凝胶剂的成型性、酸碱度为指标进行综合评价;采用HPLC法对复方止痒凝胶制剂的君药紫花地丁的主要成分秦皮乙素含量进行测定。结果:紫花地丁复方止痒凝胶的最佳处方包括:中药复方止痒浓缩液53.9g、卡波姆940 1.80g、蒸馏水35.9g、无水乙醇5.00g、氮酮1.50g、甘油5.40g、氢氧化钠0.432g,复方止痒凝胶中秦皮乙素平均含量为457.2μg·mL-1。结论:经验证试验,证明所优选的复方止痒凝胶剂制备工艺简单、重复性好、质量可控。     

消疹口服液质量标准研究

目的建立消疹口服液的质量标准。方法用薄层色谱法对紫草进行定性鉴别,用高效液相色谱法测定消疹口服液的左旋紫草素含量。结果紫草的薄层色谱特征明显,专属性强;左旋紫草素质量浓度在0．02—1．0mg／mL范围内与峰面积线性关系良好,平均回收率为99．6％,RSD=1．07％（n=9）。结论建立的方法操作简便,结果准确,重现性好。     

盐酸利多卡因凝胶-口服液的研制及质量控制

目的筛选盐酸利多卡因凝胶-口服液处方,制备适合电子胃镜检查的辅助制剂。方法以卡波姆-940为基质、二甲基硅油为消泡剂制备盐酸利多卡因凝胶-口服液,详细考察其性状均匀性、消泡能力、含量、pH,确定最优处方,并通过高温、低温及离心试验考察样品的初步稳定性。结果2%盐酸利多卡因凝胶-口服液主要成分的最优处方为卡波姆-9400.3%,甘油15%,三乙醇胺0.8%,二甲基硅油2%。除高温下会使样品主药含量略有下降外,其他性质均稳定。结论2%盐酸利多卡因凝胶-口服液的制备工艺简便,质地细腻均匀,室温下稳定性好,消泡能力强,符合临床应用要求。     

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.     

Pharmacological treatment of COVID-19: an opinion paper

The precocity and efficacy of the vaccines developed so far against COVID-19 has been the most significant and saving advance against the pandemic. The development of vaccines has not prevented, during the whole period of the pandemic, the constant search for therapeutic medicines, both among existing drugs with different indications and in the development of new drugs. The Scientific Committee of the COVID-19 of the Illustrious College of Physicians of Madrid wanted to offer an early, simplified and critical approach to these new drugs, to new developments in immunotherapy and to what has been learned from the immune response modulators already known and which have proven effective against the virus, in order to help understand the current situation.     

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.