阿莫西林克拉维酸钾口服干混悬剂含量测定方法研究

目的：对阿莫西林克拉维酸钾口服干混悬剂含量测定方法研究。方法：采用高效液相色谱法，在３×３ＣＲＣ１８柱（４ｍｍ×３．５ｃｍ）上，以ｐＨ４．４磷酸二氢钠溶液－甲醇（９５∶５）为流动相，流速１．０ｍｌ·ｍｉｎ－１，检测波长为２２０ｎｍ。结果：阿莫西林和克拉维酸浓度分别在２５～５００μｇ·ｍｌ－１及１０～２００μｇ·ｍｌ－１范围内有良好的线性关系，平均方法回收率分别为９９．４％±１．９％和９９．５％±２．０％，日内精密度分别在１．１％～２．３％和１．７％～２．６％之间，日间精密度分别＜３．１％和＜２．５％。结论：本法实用简便，结果可靠。     

口服甲苯咪唑微丸的药物动力学及生物利用度

目的：比较５ 只家兔单剂量口服甲苯咪唑微丸及片剂后的药动学与生物利用度。方法：采用ＲＰＨＰＬＣ 法测定血药浓度,３Ｐ８７ 程序计算药动学参数。结果：微丸的Ｃｍａｘ、Ｔ１／２ 、ＡＵＣ分别为６４３．４９ ｎｇ·ｍｌ－ １ 、１ ．０５ ｈ、８ １７０ ．９４ ｈ·ｎｇ·ｍｌ－１ 。结论：微丸与片剂的ＡＵＣ有统计学显著性差异（ Ｐ＜０ ．０５）,相对生物利用度为５２８ ．６０ ％ 。     

反相高效液相色谱法测定六神丸中蟾毒内酯的含量

本文首次采用ＲＰ－ＨＰＬＣ法测定六神丸中蟾毒内酯的含量，固定相为Ｓｐｈｅｒｉ－５，２２０ｍｍ×４．６ｍｍ，ＯＤＳ柱；流动相为甲醇－水（６０：４０）；流速１ｍｌ／ｍｉｎ；检测波长２９９ｎｍ；外标法；回收率为９８．４％；在１８．９～９４．５μｇ／ｍｌ浓度范围内线性良好，ｒ＝０．９９９４。     

RP—HPLC测定天乐口服液中橙皮苷的含量

采用ＲＰ－ＨＰＣＡ测定天乐口服液中橙皮苷的含量,以μ－ＢｏｎｄａｐａｋＣ１８柱（１０μｍ,４．６ｍｍ×２５０ｍｍ）为固定相,２％甲醇的乙腈溶液－０．１％磷酸和０．１％三乙胺的水溶液（２０：８０）为流动相进行测定,紫外检测波长２８４ｎｍ,平均回收率为９９．９５％,ＲＳＤ＝０．９３％。     

五种含铜宫内节育器避孕效果的对比研究

对随机放置Ｔｃｕ３８０Ａ，ＭＬ３７５，Ｆｉｎｃｏｉｄ－３５０，Ｔｃｕ２２０ｃ和镀铜宫腔形ＩＵＤ（ＵＣＤｃｕ）各１００例，临床观察３年，随访率９９．２％，结果表明：５年ＩＵＤ的妊娠率分别为５．５％，３．１％，５．２％，２．１％及３．０％，各组间差异无显著性意义（Ｐ〉０．０５），脱落率为６．６％，３．１％，６．４％，５．１％及２．０％，其中Ｔｃｕ３８０Ａ最高为６．６％，ＵＣＤｃｕ最低２．０％，二者间相     

RP－HPLC法测定牛蒡子中木脂素的含量

用ＲＰ－ＨＰＬＣ法分离并测定了牛蒡子中５种２，３－二苄基丁内酯型木脂素——牛蒡甙（Ⅰ）、牛蒡酚Ａ（Ⅱ）、牛蒡酚Ｆ（Ⅲ）、牛蒡甙元（Ⅳ）、牛蒡素Ｂ（Ⅴ）。以安定为内标，分析柱Ｃ１８，甲醇－水－乙腈－四氢呋喃（５７：４９：１１：１）为流动相，梯度流速，１．０～１．５ｍ１／ｍｉｎ。检测波长２２０ｎｍ，线性范围０．０２９～０．２４２μｇ，相关系数ｒ＝０．９９９３～０．９９９９，回收率９６．１４～１０４．９９％。本法简便、快速、灵敏。     

泰赛喷雾剂的研制与质量控制

本文报道了泰赛喷雾剂的研制，并且应用高效液相色谱法（ＨＰＬＣ），在ＹＷＧ－Ｃ１８（４×２５０ｍｍ）色谱柱上，以磷酸－三乙胺缓冲液∶甲醇∶０．０５ｍｏｌ·Ｌ－１四丁基溴化铵（２４∶５∶１）为流动相，同时测定了泰赛喷雾剂中氧氟沙星和地塞米松磷酸钠的含量，检测波长为２４０ｎｍ，内标为苯甲酸，平均回收率和相对标准偏差分别为９９．５％，１．１１％；９８．５％，２．９８％。     

硫酸长春地辛及其注射剂含量测定方法的改进

采用反相高效液相色谱法，改进了硫酸长春地辛及其注射剂含量测定条件。以Ｃ１８柱（１５０ｍｍ×４．６ｍｍ），甲醇－１．５％二乙胺（７０３０，磷酸调节ｐＨ至７．５）为流动相，测得原料药及注射剂的平均回收率分别为９９．９８％和９９．８０％，ＲＳＤ分别为０．１９％和１．５％。结果准确、稳定     

5—单硝酸异山梨醌制剂溶出度的研究

对５－单硝酸异山梨酯两种市售制剂的溶出度进行ＲＰ－ＨＰＬＣ外标法测定。流动相为甲醇－水，检测波长２２０ｎｍ，线性范围２－８０μｇ／ｍｌ，最低检测浓度０．１μｇ／ｍｌ，ＲＳＤ小于１％。经非线性回归，证实缓释制剂的释药符合一级方程Ｄｔ＝Ｄｍａｘ「７０％（１－ｅ＾－ｋ（ｔ＝ｔ０））＋３０％」。     

反相高效液相色谱法测定非洛地平缓释片的含量

采用ＲＰ－ＨＰＬＣ法测定非洛地平缓释片的含量。以ＮＯＶＡ－ＰＡＫＣ１８柱为分析柱,甲醇－水（８０：２０）为流动相,检测波长为２３８ｎｍ。该法线性良好（ｒ＝０．９９９９）,精密度ＲＳＤ＝２．２％,平均加样回收率９９．１％,ＲＳＤ＝０．７％（ｎ＝５）。     

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.