HPLC法测定耆鹿逐痹胶囊中补骨脂素和异补骨脂素的含量

ＨＰＬＣ法测定耆鹿逐痹胶囊中补骨脂素、异补骨脂素的含量。补骨脂素１．０～６．０μｇ／ｍｌ范围内呈线性关系，回收率为１００．９％（ＲＳＤ＝２．０％）；异补骨脂素１．８～１０．８μｇ／ｍｌ范围内呈线性关系，回收率９９．１％（ＲＳＤ＝１．９％）。     

反相高效液相色谱法测定大蒜素的血药浓度

目的：建立反相高效液相色谱法测定血清中大蒜素的浓度。方法：血清样品用１０％三氯醋酸沉淀蛋白,正己烷提取后进样。采用Ｐｈｅｎｏｍｅｎｅｘ Ｃ１８（２５０ｍｍ × ４．６ｍｍ,５μｍ）柱;流动相：乙腈－１％冰醋酸（６２：３８,Ｖ／Ｖ）,ｐＨ＝３．５;流速：１．２ｍｌ／ｍｉｎ,在室温下;波长：２４０ｎｍ检测。结果：该方法回收率为（９９．２±６．６）％,最低检测浓度为０．１８μｇ／ｍｌ,大蒜素血药浓度在０．２９～１２．４μｇ／ｍｌ范围内峰面积与浓度线性关系良好（ｒ＝０．９ ９７７）,日内 ＲＳＤ＜５．５％（ｎ＝５）,日间 ＲＳＤ＜５．８％（ｎ＝５） 结论：本法快速、准确、灵敏,能较好满足大蒜素临床药代动力学研究的需要。     

卡托普利片的钨蓝比色测定

以磷钨酸作显色剂，用分光光度法测定卡托普利片含量。测定波长为７００ｎｍ。在１～６μｇ／ｍｌ范围内回归方程为Ａ＝０．１１７８Ｃ＋０．００６，ｒ＝０．９９９１。平均回收率为９９．６４％（ＲＳＤ＝０．４３％，ｎ＝５），方法简便、快速。     

重组人生长激素中宿主蛋白的点─免疫结合测定法

本文应用碱性磷酸酶免疫斑点法，检测重组人生长激素中Ｅ．ｃｏｌｉ蛋白质。该法的最低检出量为１．９ｎｇ；线性范围为２．５～０．０３９μｇ／ｍｌ；平均回收率为１１５．２％，ＲＳＤ＝６．９９％（ｎ＝８）。并具有灵敏、特异、操作简便等特点。     

紫外分光光度法测定达美康片的含量

本文采用紫外分光光度法直接测定达美康片剂的含量。实验结果表明：本法简便、准确、重现性好。线性范围５．０１８２５．０９μ４ｇ／ｍｌ，γ＝０．９９９９，平均回收率９９．８１％（ｎ＝５），ＲＳＤ＝１．９０％     

高效液相色谱法梯度法脱测定三七中三七皂苷R1含量

目的：以ＨＰＬＣ梯度法脱测定三七中三七皂苷Ｒ１含量。采用Ｓｐｈｅｒｉｃｏｒｂ ＮＨ２柱,流动相为ＣＨ３ＣＮ－ＣＨ３ＯＨ－Ｈ２Ｏ,梯度洗脱浓度５５：３０：１５→７０：２０：１０,波长２１０ｎｍ,外标一点法测定。结果：以峰面积计算,三七皂苷Ｒ１在５～４０μｇ．ｍｌ＾－１呈线性相关,γ＝０．９９４,最低检测限为０．６μｇ．ｍｌ＾－１（Ｓ／Ｎ）＝３。平均回收率１０２．６％,ＲＳＤ为１．４３％,日内误差ＲＳＤ＝１．７％（ｎ＝５）,日间误差ＲＳ＝３．０％（ｎ＝４）。结论：本法专属性强,结果准确,操作简便。     

硝苯地平的分光光度测定

采用分光光度法测定硝苯地平的含量，测定波长为４９２ｎｍ，在１～２０μｇ／ｍｌ范围内回归方程为Ａ＝０．０２５＋０．０２８Ｃ，ｒ＝０．９９９０，平均回收率为９９．７６％（ＲＳＤ＝０．２１％，ｎ＝５）方法简便，快速。     

转移因子致大疱性表皮松解坏死型药疹死亡一例

本文采用紫外分光光度法直接测定诺氟沙星胶囊的含量。实验结果表明：本法简便、正确、重现性好，线性范围４．８１６－１４．４４８μｇ／ｍｌ，ｒ＝０．９９９９，回收率９９．６％（ｎ＝５）ＲＳＤ＝０．６４％。     

双波长分光光度法测定替硝唑环丙沙星注射液含量

目的：应用双波长分光光度法测定替硝唑、环丙沙星注射液含量。方法：以ｐＨ４．５的醋酸盐缓冲液为溶剂,在波长３１７,２９７．６,２７７,３５４．２ｎｍ处进行测定。。结果：替硝唑浓度在４～２０μｇ·ｍｌ－１之间,环丙沙星浓度在２～１０μｇ·ｍｌ－１之间符合比尔定律,浓度与吸收度差值呈良好的线性关系。替硝唑平均回收率为１００．８％,ＲＳＤ为１．０％（ｎ＝９）,环丙沙星平均回收率为９８．８％,ＲＳＤ为０．８％（ｎ＝９）。结论：该方法简便、快速、准确可靠。     

卡托普利片含量及其溶出度的流动注射分析

以亚硝基铁氰化钠的碱性溶液为显色剂，采用流动注射分析技术，测定卡托普利片含量及其溶出度。在２０～９０μｇ／ｍｌ的范围内其回归方程为Ｃ＝１．００２×１０￣（－５）Ｈ＋１５．４９（ｒ＝０．９９９９１），测定６０μｇ／ｍｌ样品回收率为９９．７％（ＲＳＤ＝０．６７％，ｎ＝５）。本法测定速度诀，选择性好，灵敏度高。     

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.     

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.