单硝酸异山梨酯HPMC骨架片的研制及释放度的考察

目的讨论亲水骨架材料羟丙基甲基纤维素(HPMC)在单硝酸异山梨酯口服缓释片剂中的应用。方法以湿法制粒压片法制备单硝酸异山梨酯亲水凝胶骨架片,对有影响体外释放的HPMC用量进行了考察。结果与结论单硝酸异山梨酯释药速度随HPMC用量增加、压片颗粒粒径的减小,释药速度减慢。     

复方单硝酸异山梨酯缓释片的制备

目的:制备复方单硝酸异山梨酯缓释片并考察其工艺条件.方法:以乙基纤维素为骨架材料,分别制备单硝酸异山梨酯和阿司匹林(ASA)骨架缓释颗粒,进行薄膜包衣控制两种药物同步释放;将两种缓释骨架颗粒与速释单硝酸异山梨酯、辅料混合压片,制备复方单硝酸异山梨酯缓释片.结果:片剂中两种药物达到良好的缓释效果,有效缓释时限＞10 h.体外药物释放过程符合Higuchi方程,r值均在0.9995以上.结论:本品制备工艺合理,缓释效果好,质量容易保证.     

通心络与单硝酸异山梨酯合用治疗老年冠心病心绞痛60例疗效观察

目的探讨通心络与单硝酸异山梨酯合用治疗冠心病心绞痛的临床疗效。方法以临床症状、体表心电图、血脂分析等方法观察通心络与单硝酸异山梨酯合用治疗老年冠心病心绞痛的疗效,并与单用单硝酸异山梨酯组作对照。结果通心络与单硝酸异山梨酯合用临床症状有效率96.67%、心电图改善76.67%、显效率均高于单用单硝酸异山梨酯组(P<0.05);血清胆固醇和低密度脂蛋白治疗后下降明显(P<0.05),而单用单硝酸异山梨酯组治疗前后血脂无明显变化(P>0.05)。结论通心络与单硝酸异山梨酯合用能够很好地改善老年冠心病心绞痛的临床症状及心电图的缺血变化,并对血液黏稠度和血脂有很好的改善作用,同时能减少单硝酸异山梨酯的用量及副作用。     

通心络与单硝酸异山梨酯合用治疗老年冠心病心绞痛疗效观察

目的 :探讨通心络与单硝酸异山梨酯合用治疗冠心病心绞痛的临床疗效。方法 :以临床症状、体表心电图、血脂分析等方法观察通心络与单硝酸异山梨酯合用治疗老年冠心病心绞痛的疗效 ,并与单用单硝酸异山梨酯组作对照。结果 :通心络与单硝酸异山梨酯合用临床症状有效率 96 .6 7%、心电图改善 76 .6 7%、显效率均高于单用单硝酸异山梨酯组 (P <0 .0 5 ) ;血清胆固醇和低密度脂蛋白治疗后下降明显 (P <0 .0 5 ) ,而单用单硝酸异山梨酯组治疗前后血脂无明显变化 (P >0 .0 5 )。结论 :通心络与单硝酸异山梨酯合用能够很好地改善老年冠心病心绞痛的临床症状及心电图的缺血变化 ,并对血液黏稠度和血脂有很好的改善作用 ,同时能减少单硝酸异山梨酯的用量及副作用     

盐酸伊伐布雷定对单硝酸异山梨酯在比格犬体内的药动学影响

目的 研究盐酸伊伐布雷定对单硝酸异山梨酯在比格犬体内的药动学影响.方法 采用HPLC法测定单硝酸异山梨酯单独给药或联合盐酸伊伐布雷定给药后不同时间比格犬体内的血药浓度,采用非房室模型计算单硝酸异山梨酯药动学参数.结果 单硝酸异山梨酯单独给药及与盐酸伊伐布雷定联合使用后,在比格犬体内单硝酸异山梨酯的主要药动学参数差异无统计学意义(P<0.05).单硝酸异山梨酯联合盐酸伊伐布雷定给药相对单硝酸异山梨酯单独给药的生物利用度为100%.结论 盐酸伊伐布雷定与单硝酸异山梨酯联合用药后对单硝酸异山梨酯在比格犬体内的药动学过程无影响.     

单硝酸异山梨酯的药理实验研究

目的： 研究单硝酸异山梨酯的抗心肌缺血及耐缺氧作用, 并与进口单硝酸异山梨酯及国产消心痛进行比较。方法： 采用药物诱发心肌缺血法及冠状动脉结扎法。结果： 国产单硝酸异山梨酯对垂体后叶素诱发的心肌缺血, 对家兔冠状动脉结扎所致的心肌缺血均有明显的保护作用, 可明显延长常压缺氧、异丙肾上腺素诱发缺氧小鼠的生存时间。结论： 国产单硝酸异山梨酯的抗心肌缺血作用与进口单硝酸异山梨酯及国产消心痛作用相近。     

单硝酸异山梨酯的药理实验研究

目的：研究单硝酸异山梨酯的抗心肌缺血及耐缺氧作用,并与进品单硝酸异山梨酯及国产消心痛进行比较。方法：采用药理诱发心肌缺血法及冠状动脉结扎法。结果：国产单硝酸异山梨酯对垂体后叶素诱发的心肌缺血,对家兔冠状动脉结扎所致的心肌缺血均有明显的保护作用,可明显延长常压缺氧、异丙肾上腺素诱发缺氧小鼠的生存时间。结论：国产单硝酸异山梨酯的抗心肌缺血作用与进口单硝酸异山梨酯及国产消心痛作用相近。     

单硝酸异山梨酯治疗30例缺血性心肌病的观察

目的 观察单硝酸异山梨酯治疗缺血性心肌病患者的疗效及价值.方法 将60例缺血型心肌病患者分为单硝酸异山酯组与对照组给予常规抗心力衰竭治疗,单硝酸异山梨组是在常规治疗组的基础上加服单硝酸异山梨酯,治疗后监测心脏彩超、临床心功能.结果 单硝酸异山梨酯组患者治疗后LVDD(左室舒张末内径)、LVEF(左室射血分数)、FS(左室缩短率)治疗前后比较差异有统计学意义,且LVEF、FS与对照组比较差异有统计学意义,单硝酸异山梨酯组有效率高于对照组.结论 单硝酸异山无酯对缺血型心肌病有确切疗效.     

单硝酸异山梨酯滴丸的研究

目的 研究剥备单硝酸异山梨酯滴丸剂．建立质量控制方法。方法 采用滴丸制备法制成单硝酸异山梨酯滴丸,并用高效液相色谱法测定其含量。结果 成功制备单硝酸异山梨酯滴丸剂。结论 工艺简单,质量稳定可靠。     

高效液相色谱法测定单硝酸异山梨酯胶囊的含量及含量均匀度

高效液相色谱法测定单硝酸异山梨酯胶囊的含量及含量均匀度河北省药品检验所０５００１１韩学静郭毅郑德海刘庆京杜增辉单硝酸异山梨酯（５－ＩＳＭＮ）为新一代抗心绞痛的硝酸酯类药物，是硝酸异山梨酯在体内的主要活性代谢产物。具有半衰期长，生物利用度高等特点，１９...     

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.