用RP-HPLC法测定七厘散中羟基红花黄色素A的含量

目的：建立RP-HPLC法测定七厘散中羟基红花黄色素A的含量。方法：采用Mucleodur C18色谱柱（250 mm×4.6 mm,5 μm）;流动相：乙腈-0.1%磷酸溶液 （11∶89）;流速：1.0 ml/min;检测波长：403 nm;柱温：35 ℃。结果：羟基红花黄色素A保留时间约为19 min,与相邻峰的分离度〉1.5。羟基红花黄色素A在8.0～160.0 μg/ml范围内线性关系良好,回归方程：Y=0.016 11 X＋1.217（r=0.999 9）。平均加样回收率为99.5%,RSD为0.94%。结论：该方法准确、灵敏、重现性好,可用于七厘散中羟基红花黄色素A的含量测定。     

HPLC法测定红花跌打胶囊中羟基红花黄色素A的含量

目的 建立高效液相色谱法测定红花跌打胶囊中羟基红花黄色素A的含测方法.方法 采用高效液相色谱法,紫外检测器C18柱(4.6 mm×250 mm,5 μm),以甲醇-乙腈-0.7%磷酸溶液(26:2:72)为流动相,检测波长为403 nm,对样品中的羟基红花黄色素A进行测定.结果 通过方法学的系统考察和3批样品的含量测定,建立了制剂中羟基红花黄色素A的高效液相色谱的含量测定方法:线性范围为0.001 2~0.121 7 mg·mL-1,平均回收率99.5%.回归方程Y=584.79X-0.160 4,r=1.结论 本方法简便,快速,准确,灵敏度高,重复性好,可用于红花跌打胶囊中羟基红花黄色素A含量的测定.     

高效液相色谱法测定伊赫汤中羟基红花黄色素A的含量

目的建立伊赫汤中羟基红花黄色素A的含量测定方法。方法采用高效液相色谱法(HPLC),色谱柱为大连依力特C18柱(250 mm×4.6 mm,5μm),流动相为甲醇-0.5%乙酸溶液(20∶80),检测波长为403 nm,流速为1.0 ml/min。结果羟基红花黄色素A在0.816 0～32.64μg/ml浓度范围内具有良好的线性关系,r=0.999 9,平均加样回收率为101.0%,RSD为1.8%(n=6)。结论本方法快速、准确、重复性好,可用于伊赫汤中羟基红花黄色素A的含量测定。     

HPLC法测定正天丸和正天胶囊中羟基红花黄色素A的含量

目的:建立HPLC法测定正天丸和正天胶囊中羟基红花黄色素A的含量。方法:以十八烷基硅烷键合硅胶为填充剂,以甲醇-乙腈-0.7%磷酸溶液(26∶2∶72)为流动相,检测波长为403 nm。结果:羟基红花黄色素A在6.038 4～150.96μg·mL-1范围内呈良好的线性关系;平均回收率为100.0%,RSD=0.8%(n=6)。结论:本方法准确、快速、重现性好,可用于测定正天丸、正天胶囊中羟基红花黄色素A的含量。     

HOLC法测定肤痒颗粒中羟基红花黄色素A的含量

目的:建立肤痒颗粒的鉴别和含量测定的方法.方法:采用HPLC法测定羟基红花黄色素A的含量.结果:羟基红花黄色素A含量在0.02046～0.2046μg范围内有良好的线性关系r=0.9998,平均回收率为99.85%,RSD=0.10%n=5.结论:方法专属性强、重复性好,简便易行,可用于该制荆的质量控制.     

红花鼻炎丸中羟基红花黄色素A的含量测定方法考察

目的:建立红花鼻炎丸中羟基红花黄色素A的含量测定方法.方法:采用反相高效液相色谱法,色谱主为C18柱,以甲醇-乙腈-0.7％磷酸(19∶2∶79)为流动相,流速:1.0mL/min,检测波长为403nm.结果:羟基红花黄色素A在0.01657～0.6628μg范围内呈良好的线性关系,r=-1.000,平均回收99.9％,RSD为0.1％(n=9).结论:实验所用方法专属性强、重现性好、精密度高,能准确地对羟基红花黄色素A进行含量测定.     

反相高效液相色谱法测定红花清肝十三味丸中羟基红花黄色素A的含量

目的:建立红花清肝十三味丸中羟基红花黄色素A的含量测定方法.方法:采用反相高效液相色谱法,色谱柱为Agilent Eclipse XDB-C18柱(250 mm×4.6 mm,5 μm),流动相为甲醇-0.18%乙酸溶液(20:80),检测波长为403 nm,流速为1.0 mL·min-1.结果:羟基红花黄色素A在0.168～16.8 μg范围内具有良好的线性关系,r=0.999 9,平均加样回收率为99.76%,RSD为0.6%.结论:本方法快速、准确,重复性好,可用于红花清肝十三味丸中羟基红花黄色素A的含量测定.     

高效液相色谱法测定复方红花滴丸中羟基红花黄色素A的含量

目的:建立复方红花滴丸中羟基红花黄色素A含量测定的方法。方法:应用高效液相色谱法,以甲醇-乙腈-0.00332‰磷酸(20:2:78)为流动相,流速0.9mL/min;室温403nm测定。结果:羟基红花黄色素A进样量在0.0620~0.3100μg范围内与色谱峰面积有良好的线性关系,r=0.9999,回收率为98.08%,RSD=1.69%。结论:本方法简便易行,结果准确可靠。     

七味红花殊胜丸中药材的鉴定及羟基红花黄色素A的测定

建立七味红花殊胜丸的鉴别及含量测定的方法,提高质量标准.方法采用TLC法鉴别方中麻黄素、诃子和红花;采用HPLC法测定红花中的羟基红花黄色素A.采用C18柱,流动相为甲醇-乙腈- 0.7％磷酸溶液(26:2:27),检测波长403 nm.结果盐酸麻黄碱、诃子、红花的薄层色谱斑点清晰,专属性强.羟基红花黄色素A进样量0....     

HPLC法测定蒙成药小儿清肺八味丸中羟基红花黄色素A的含量

目的:建立蒙成药小儿清肺八味丸中羟基红花黄色素A的含量测定方法。方法:采用HPLC法,应用Agilent TC-C 18色谱柱(4.6 mm×250 mm,5μm),流动相为甲醇-乙腈-0.7%磷酸水溶液(16∶1∶83),用三乙胺调pH值为6.0,流速1.0 mL·min^-1,柱温30℃,进样量为10μL,检测波长为403 nm。结果:羟基红花黄色素A进样量范围在0.10~2.00μg时,进样量与峰面积线性关系良好(r=0.9999);平均回收率为102.48%,RSD为1.52%。结论:该方法简便、灵敏、准确,可用于小儿清肺八味丸中羟基红花黄色素A的测定。     

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.

     

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.     

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.