脑缺血合剂质量标准研究

目的建立脑缺血合剂的质量标准。方法采用薄层色谱（TLC）法对芍药苷、大黄素、大黄酚进行鉴别,采用高效液相色谱（HPLC）法测定芍药苷含量。结果TLC鉴别芍药苷、大黄素、大黄酚具有很好的分离效果,HPLC平均回收率为98.0%（RSD＝1.11%）。结论所建立的鉴别方法专属性强,定量方法简便、准确,可用于脑缺血合剂的质量控制。     

少腹逐瘀颗粒的质量标准

目的:建立少腹逐瘀颗粒质量标准.方法:采用TLC法对处方中赤芍、当归、川芎、延胡索、五灵脂进行定性鉴别;采用HPLC法测定了芍药苷含量.结果:在TLC图谱中可检出赤芍等药材的特征斑点;测得芍药苷平均回收率为99.4%,RSD=0.6%(n=6).结论:所采用方法准确、可靠,可行性及重复性良好,能有效控制该制剂的质量.     

提高八味痛经胶囊质量标准的研究

目的建立八味痛经胶囊的质量控制标准。方法采用TLC法对八味痛经胶囊中当归、桂枝、牡丹皮、延胡索进行鉴别,用HPLC法测定八味痛经胶囊中的牡丹皮和白芍共同有效成分芍药苷的含量。结果薄层色谱可鉴别出当归、桂枝、牡丹皮、延胡索的特征斑点,且阴性对照无干扰;HPLC法测定芍药苷0.2575~2.5750μg线性关系良好,平均加样回收率为98.98%,RSD=1.0%(n=6)。结论该方法简便可靠,专属性强,重现性好,可用于八味痛经胶囊的质量控制。     

香砂脘痛胶囊质量标准研究

目的建立香砂脘痛胶囊质量标准。方法采用薄层色谱（TLC）法对香砂脘痛胶囊中木香、党参和郁金进行鉴别;采用高效液相色谱（HPLC）法测定香砂脘痛胶囊中芍药苷的含量。结果 TLC色谱中均能检出木香、党参和郁金;芍药苷在0.1296～2.0736μg范内呈良好线性关系（r=0.9999）;平均加样回收率为98.94%,RSD=0.81%（n=6）。结论本方法简便、专属性强、重现性好,结果稳定,可有效控制香砂脘痛胶囊的质量。     

盆炎灵合剂质量标准研究

目的建立盆炎灵合剂的质量标准。方法采用TLC法对盆炎灵合剂中当归、延胡索药材进行定性鉴别 用HPLC法对芍药苷进行定量研究。色谱柱为Agilent C18（250 mm×4.6 mm,5μm）。流动相为甲醇-0.1%磷酸溶液（25∶75）,流速为1.0 mL.min-1,检测波长为230 nm,柱温为35℃。结果在TLC色谱中均能检出当归、延胡索,芍药苷在0.015~0.15 mg.mL-1与峰面积呈良好的线性关系（r=0.999 9）,平均回收率为98.66%,RSD为0.94%（n=9）。结论该方法操作简便,结果准确,灵敏度高,重现性好,适用于盆炎灵合剂的质量控制。     

生津润燥合剂质量标准研究

目的对生津润燥合剂进行质量标准建立。方法采用TLC对制剂中玄参、赤芍进行鉴别;采用HPLC对生津润燥合剂中芍药苷进行含量测定。结果用TLC能检出玄参、赤芍,芍药苷在0.002～0.10 g.L-1范围内线性关系良好,r=0.999 6,平均回收率为94.83%,RSD为0.79%。结论该方法可靠,易操作,重现性好,专属性强,可用于控制生津润燥合剂的质量。     

清热消炎合剂质量标准研究

目的：探讨清热消炎合剂的质量标准。方法：用薄层色谱法(TLC法)鉴别制剂中黄芩、大黄、黄柏、山豆根，用高效液相色谱法(HPLC法)测定黄芩苷的含量。结果：在TLC色谱中黄芩、大黄、黄柏、山豆根均能得到很好的鉴别；HPLC法测黄芩苷，线性范围为1．2～57．6μg／mL，平均回收率为99．06％，RSD为0．69％(n=3)。结论：采用的方法能有效控制清热消炎合剂的质量。     

基于多指标成分定量的痛舒凝胶贴膏质量评价研究

目的 基于多指标成分TLC鉴别及HPLC定量分析评价痛舒凝胶贴膏质量。方法 采用TLC法对剂型改良后的痛舒凝胶贴膏中延胡索乙素、芍药苷、粉防己碱、乌药醚内酯以及苍术、枳壳进行定性鉴别;HPLC法测定该剂型中主要有效成分延胡索乙素、芍药苷、粉防己碱、乌药醚内酯的含量。结果 组方中6味药材TLC结果斑点清晰,显色良好且阴性无干扰。延胡索乙素、芍药苷、粉防己碱、乌药醚内酯分别在4.30～272.50μg/mL(r=0.999 9)、21.10～1 350.00μg/mL(r=0.999 8)、4.10～262.40μg/mL(r=0.999 8)、3.60～232.50μg/mL(r=0.998 6)的浓度范围内线性关系良好,平均加样回收率范围区间为98.96%～99.52%,RSD均≤1.54%(n=9)。结论所建立的多指标TLC定性鉴别及HPLC定量方法专属性高,操作简便易行,可用于该组方剂型改进后的质量评价。     

十全大补丸的质量标准

目的完善十全大补丸的质量标准。方法采用TLC法鉴别方中黄芪,用HPLC法测定方中芍药苷的含量。结果TLC鉴别色谱特征斑点明显。芍药苷进样量在0.1038~1.0376μg范围的线性关系良好。平均加样回收率大蜜丸为97.2%,RSD=1.1%(n=6);水蜜丸为100.5%,RSD=2.5%(n=6)。结论所建立的TLC和HPLC方法专属性强、重复性好,可用于十全大补丸的质量控制。     

胃肠舒颗粒的质量标准研究

目的建立胃肠舒颗粒的质量标准。方法以TLC法鉴别黄芪、白芍、丹参、延胡索和甘草;以HPLC法测定芍药苷含量。结果 TLC法鉴别分离度好,专属性强。芍药苷在12.96～259.27μg·mL~(-1)范围内与峰面积线性关系良好(r=0.999 9),平均回收率为98.92%,RSD值为1.79%。结论该方法快速、简便、灵敏,重复性好,可用于胃肠舒颗粒的质量控制。     

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.     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

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.

     

Lung disease and PKCs

The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.     

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.