清热解毒口服液主要活性成分的定量分析

目的:建立清热解毒口服液中黄芩苷、栀子苷、连翘苷、绿原酸的定量测定方法.方法:色谱柱Shim-Pack VP-ODS C18色谱柱(250 mm×4.6 mm,5 μm);流动相甲醇-0.1%磷酸梯度洗脱;检测波长为227 nm.结果:黄芩苷、栀子苷、连翘苷、绿原酸分别在0.200 2~2.002 mg·ml-1(r=0.999 8)、0.144 6~1.446 mg·ml-1(r=0.999 9)、0.102 8~1.028 mg·ml-1(r=0.999 9)、0.129 8~1.298 mg·ml-1(r=0.999 5)范围内线性关系良好;其各自平均回收率分别为96.49%、96.09%、95.64%和97.82%.结论:该方法准确、简便、快速,可以用于定量测定清热解毒口服液中黄芩苷、栀子苷、连翘苷、绿原酸的含量.     

不同采收时期及干燥方法对栀子中栀子苷含量的影响

目的:评价不同采收期以及不同干燥方法对栀子苷的影响.方法:应用高效液相色谱法测定,色谱柱为Agilent Zorbax XDB-C18色谱柱(150 mm×4.6 mm,5 μm);流动相为乙腈-水(15:85),流速1.0 ml·min-1;柱温:30℃;检测波长238 nm.结果:栀子苷的线性范围为0.31～155.76 μg·ml-1(r=0.999 9),加样回收率为100.9%(RSD=1.2%);定量分析了6个采收时间、12种干燥方法的栀子中栀子苷含量.结论:不同采收时期、不同干燥方法对栀子中栀子苷的含量有一定的影响.     

HPLC法测定蓝芩口服液中的栀子苷含量

建立高效液相色谱法测定蓝芩口服液中的栀子苷含量的方法.色谱柱:Kromasil C18柱;流动相:0.05mol·L-1磷酸氢二钠-甲醇(70:30);流速1.0ml·min-1;检测波长238nm.栀子苷在9.6～48.0μg·ml -1之间峰面积与浓度呈良好的线性关系,r =0.9999,平均回收率为98.5%(n =6),RSD为0.66% . 该方法可用于蓝芩口服液中栀子苷的质量控制.     

HPLC测定鼻窦炎颗粒中的栀子苷

目的:采用HPLC法测定鼻窦炎颗粒中的栀子苷.方法:色谱柱为Agilent ZORBAX SB-C18(250 mm×4.6 mm,5μm),流动相为水.乙腈.磷酸(86:14:0.01),检测波长238 am,流速1.0 ml·min-1,柱温30℃.结果:栀子苷浓度3.36～126μg·ml-1,与峰面积的线性关系良好(r=0.999 9),平均加样回收率98.09%,RSD=1.69%.结论:所建方法准确、重复性好,可用于测定鼻窦炎颗粒中的栀子苷.     

HPIC法测定三臣七味颗粒中栀子苷的含量

目的:建立高效液相色谱法测定三臣七味颗粒中栀子苷的含量.方法:反相高效液相色谱法,乙睛-水(12:88)为流动相,流速为1.0 ml·min-1,检测波长为238 nm,用外标法定量.结果:栀子苷在25.344-50.688 μg·m-1范围内有良好的线性关系,Y=0.9993,平均回收率为100.16%(RSD=0.70%,N=5).结论:方法可行,重现性好,准确监控该制剂的质量.     

栀柏合剂的制备及质量控制

目的制备栀柏合剂并建立其质量控制方法.方法采用薄层色谱法对栀子、黄柏进行定性鉴别,用高效液相色谱法测定栀子中栀子苷含量.结果栀子苷含量在25～100 mg·L-1范围内线性关系良好(r=0.999 7),平均回收率为99.73%,RSD为0.88%(n=5).结论该制备工艺合理,质量控制方法可行.     

UPLC法快速测定栀子复方制剂中栀子苷和西红花苷-1含量

目的建立快速测定栀子复方制剂复方牛黄消炎胶囊、清胃黄连丸和龙泽熊胆胶囊中栀子苷和西红花苷-1的方法。方法采用UPLC法。色谱柱为BEH C18柱(50mm×2.1mm,1.7μm);流动相:甲醇-水以不同梯度洗脱;流速:0.3mL·min~(-1);检测波长:0~7min为238nm,7~20min为440nm;柱温:30℃;进样量为2μL。结果 3种复方制剂中栀子苷在0.010~1.000mg·mL~(-1)范围内呈良好的线性关系(r=0.999 9),平均回收率分别为98.2%,99.9%和100.3%,RSD分别为1.3%,1.4%和1.0%;西红花苷-1在0.1~10.0μg·mL~(-1)范围内呈良好的线性关系(r=0.999 9)。平均回收率分别为99.6%,97.4%和98.3%,RSD分别为1.3%,1.4%和1.5%。结论栀子苷和西红花苷-1在20min内获得良好分离,该方法简便、准确、快速,可用于栀子复方制剂中栀子苷和西红花苷-1的测定。     

HPLC法测定肝宁丸中栀子苷的含量

目的:应用高效液相色谱法对肝宁丸中栀子苷进行含量测定.方法:选用依利特Hypersil C18分析柱(150 mm×4.6 mm,5μm),乙腈-水(11:89)为流动相,检测波长为238 nm,流速1.0 ml · min-1.结果:栀子苷在0.016 7～0.333 2 mg·ml-1具有良好的线性关系,r=1.000 0,平均回收率为96.10%,RSD为0.96%.结论:本试验所确定的质量分析方法稳定可靠,可作为肝宁丸中栀子苷的含量测定方法.     

HPLC法测定栀子柏皮软胶囊中栀子苷和小檗碱的含量

目的:建立栀子柏皮软胶囊中指标性成分栀子苷和小檗碱的含量测定方法。方法:采用 Diamonsil ODS-C_(18)柱(5μm,4.6 mm×150 mm);栀子苷的测定以乙腈-水(15:85)为流动相,流速:1.0 mL·min~(-1),检测波长为238 nm;小檗碱的测定以乙腈-0.05%磷酸水溶液-十二烷基硫酸钠(55:45:0.1)为流动相,流速:1.0 mL·min~(-1),检测波长为265 nm。结果:栀子苷的线性范围为10.2～50.3 mg·mL~(-1),平均回收率为96.8%(n=9),RSD 为1.5%;小檗碱在9.5～66.4μg·mL~(-1)浓度范围内线性关系良好,平均回收率为97.4%(n=9),RSD 为1.3%。结论:本方法简便、灵敏,重现性好,适用于栀子柏皮软胶囊的质量控制。     

高效液相色谱法测定五味沙棘散中栀子苷的含量

目的:建立高效液相色谱法测定五味沙棘散中栀子苷的含量.方法:色谱柱为Waters Xttera C18(4.6 mm×250mm,5μm),流动相为乙腈一水(13:87),流速为1.0 mL·min-1,柱温为25℃,检测波长为238 nm.结果:在10.24～102.4 mg·L-1范围内,栀子苷的进样浓度与吸收峰积分值呈良好的线性关系,r=0.9995,平均回收率为100.77%,RSD为1.73%.结论:该方法简便,准确,可用于五味沙棘散中栀子苷的含量测定.     

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.

     

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.