恩拉霉素质量标准的建立

目的 建立恩拉霉素质量标准。方法 采用HPLC-PDA法建立鉴别及恩拉霉素组分检查方法，采用效价法建立恩拉霉素含量测定方法，并根据药品质量标准分析方法验证指导原则的要求，进行相应方法验证。结果 鉴别恩拉霉素组分检查方法专属性良好，在100~350u/mL范围内浓度与组分A与B峰面积之和具有良好的线性关系(r=0.9999)；效价含量测定方法专属性良好，在10~48u/mL范围内浓度与抑菌圈直径具有良好的线性关系(r=0.9995)，方法准确度回收率96.3%，RSD为2.9%。 结论 该质量标准考察项目全面，方法简单准确，可作为恩拉霉素质量控制的方法。     

克拉霉素缓释片中克拉霉素的反相高效液相色谱法含量测定的方法学考察

目的:建立用反相高效液相色谱法测定克拉霉素缓释片中克拉霉素的含量测定方法,并考察其方法学的实用性。方法:采用Hypersil BDS C18色谱柱(200 mm×4.6 mm,5μm)为固定相,流动相为乙腈-0.067 mol/L磷酸二氢钾溶液(40∶60),流速为1.0 mL/min,检测波长为210 nm,柱温为25℃;采用反相高效液相色谱法检测克拉霉素缓释片中克拉霉素的含量。结果:克拉霉素浓度在0.17~0.65 mg/mL范围内呈良好的线性关系(r=0.9998),平均RSD为0.89%,回收率为99.50%;4批克拉霉素缓释片中的平均含量为96.87%。结论:在克拉霉素缓释片质量控制检测中,用反相高效液相色谱法测定克拉霉素的含量,其操作快速、简便,可适用于克拉霉素缓释片的含量测定。     

肝宁片质量标准测定方法的研究

目的：制定肝宁片的质量标准。方法：采用TIC法对肝宁片中洋委陵菜、球果紫堇、水飞蓟果进行了鉴别，用薄层扫描法测定水飞蓟宾的含量。结果：定性鉴别专属性强，含量测定回收率为97．8％。r=0．9997。结论：建立的定性、定量方法，可作为本品的质量控制的标准。     

壮药猫豆质量标准研究

目的制定猫豆药材的质量标准。方法根据2010年版《中国药典》方法,鉴别猫豆的性状、显微特征,检查其水分、总灰分、酸不溶灰分、浸出物;采用薄层色谱(TLC)法进行定性鉴别;采用高效液相色谱法(HPLC)测定左旋多巴的含量。结果初步建立了猫豆药材薄层色谱鉴别方法及左旋多巴HPLC测定方法;确定了水分、灰分、浸出物及左旋多巴的含量限度。结论所建立的定性、定量方法及理化指标可作为猫豆药材的质量控制标准。     

醒脑治瘫胶囊成分提取工艺及质量标准的研究

目的：建立醒脑治瘫胶囊质量标准。方法：采用薄层色谱法对黄芪、人工牛黄进行定性鉴别；高效液相色谱法对芍药苷进行含量测定。结果：芍药苷的平均回收率为99．6%，RSD为1．06％。结论：本法操作简便，结果准确，可以作为醒脑治瘫胶囊质量控制的方法。     

硫酸氨基葡萄糖凝胶质量控制标准的初步研究

目的建立硫酸氨基葡萄糖凝胶的质量控制标准。方法建立了酸碱度、卫生学、定性鉴别、含量测定等质量控制方法。结果硫酸氨基葡萄糖凝胶的pH为6.3～6.5,卫生学检查符合规定,定性鉴别方法简便易行,含量测定平均回收率为100.3%,RSD=2.32%(n=5)。结论制订的质量标准可以控制硫酸氨基葡萄糖凝胶的质量。     

柏子养心片质量标准研究

目的 建立柏子养心片的质量标准。方法 采用显微对党参，肉桂，朱砂进行定性鉴别；薄层色谱法对黄芪、五味子进行定性鉴别；用滴定法测定朱砂的含量^[1]。结果 显微检出党参，肉桂、朱砂；TLC法检出黄芪，五味子；朱砂含量测定加样回收率为98．99％，RSD为3．22％(n=9)。结论 该方法灵敏，简便，重现性好，可作为该制剂的质量控制标准。     

不同剂型克拉霉素口服固体制剂质量比较

摘要：目的 比较不同剂型克拉霉素口服固体制剂的质量,并完善质量标准。方法 采用法定检验方法结合探索性研究 对不同剂型249批次克拉霉素口服固体制剂进行检验。结果 按法定标准检验,249批次样品的合格率为99.6%,不合格项目为 干燥失重。采用新建立的杂质谱分析方法,确证了各杂质的结构;不同生产企业溶出曲线存在较大差异;高温会加速主成分降 解,高湿条件下样品中水分增大。结论 克拉霉素胶囊平均溶出量略低于片和分散片,克拉霉素颗粒的总杂质高于其他剂型。 克拉霉素口服固体制剂总体质量较好;现行质量标准有待提高,建议增/修订有关物质检查方法;统一克拉霉素片、分散片、胶 囊溶出方法;严格控制药品生产、流通、贮藏过程中的温湿度。     

高效液相色谱梯度洗脱法测定克拉霉素的含量

目的建立高效液相色谱梯度洗脱法测定克拉霉素的含量。方法采用kromasil-C18(4.6mm×150mm,5μm)柱,乙腈-0.476%磷酸二氢钾溶液(pH值4.4)为流动相梯度洗脱,检测波长为205nm,流速1.1mL/min。结果克拉霉素在0.49～2.48mg/mL内呈良好的线性相关性,相关系数r为0.9999,检测限为0.8ng/mL,定量限为2.4ng/mL。结论该方法准确可靠,灵敏度高,可用于克拉霉素的含量测定及质量控制。     

炒蛴螬的工艺及质量标准研究

目的：建立炒蛴螬药材的工艺及质量标准研究。方法：用清炒法,制定炒蛴螬药材最佳的生产工艺。采用显微鉴别、薄层色谱鉴别及含量测定方法,控制其质量标准。结果：经验证,实验确定的炒蛴螬药材工艺重现性好、生产工艺稳定,所制定的质量标准测定结果重现性好。结论：本实验炒蛴螬工艺可行,制定的质量控制方法可用于炒蛴螬的质量控制。     

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.     

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.