养血育发颗粒质量标准的提高

摘 要 目的：为提高养血育发颗粒的质量,进一步完善其质量控制标准。方法: 对方中制首乌、枸杞子、地黄、丹参和女贞子5味药进行薄层色谱鉴别,同时采用高效液相色谱法对方中芍药苷进行含量测定。结果: 薄层色谱中斑点清晰,专属性强;芍药苷在14.3~286.0μg·mL^-1范围内成良好的线性关系（r=0.999 4）,平均回收率为96.61%,RSD=0.86%（n=9）。结论:所用方法简便,重复性好,定量方法准确可靠,可用于养血育发颗粒的质量控制。     

HPLC法测定参芪苓口服液中党参炔苷的含量

摘 要 目的： 建立测定参芪苓口服液中党参炔苷含量测定的的方法。方法: 采用高效液相色谱法。色谱柱为Agilent ZORBAX SB C₁₈（250 mm×4.6 mm,5 μm）,流动相为乙腈 0.2%磷酸溶液(16∶84,V/V),流速:1.0 ml·min^-1,柱温为25℃,检测波长284 nm,进样量为10 μl。结果: 党参炔苷在0.019 7～0.236 4 mg·ml^-1范围内与其峰面积积分值呈良好线性关系（r=0.999 9）,平均回收率为98.92%,RSD=0.86%(n=9)。结论: 本方法简便可靠,重复性好,可用于参芪苓口服液中党参炔苷的含量测定。     

苦牛止咳口服液质量标准的建立

摘 要 目的：建立苦牛止咳口服液的质量标准。方法: 采用TLC法对苦牛止咳口服液中的主要药味牛蒡子、前胡、桔梗、陈皮、甘草进行定性鉴别。采用HPLC测定苦牛止咳口服液中主要有效成分苦杏仁苷、牛蒡苷的含量。结果:TLC法可对牛蒡子、前胡、桔梗、陈皮、甘草进行鉴别,斑点清晰,专属性较强;HPLC测定结果显示,苦杏仁苷在25.26~151.6 μg·ml^-1,范围内线性关系良好（r=0.999 8）,牛蒡苷在22.98～137.9 μg·ml^-1,范围内线性关系良好（r=0.999 8,n=6）,平均回收率分别为99.96%（RSD=2.81%,n=9）、99.83%（RSD=2.82%,n=9）。结论:本方法重复性好、简便、快速,可作为有效控制苦牛止咳口服液质量标准的方法。     

平疣颗粒的质量标准提升研究

摘 要 目的： 研究建立平疣颗粒的质量控制标准。方法: 采用薄层色谱法对方中赤芍、红花、薏苡仁、香附进行定性鉴别;采用高效液相色谱法测定赤芍中芍药苷的含量：色谱柱为Lichrospher-C18（250 mm×4.6 mm,5 μm）,流动相为甲醇-0.2%醋酸（24∶76）,检测波长为232 nm。结果: 薄层色谱鉴别斑点清晰、阴性对照无干扰;芍药苷在6.560～104.920 μg·mL^-1的范围内呈良好的线性关系（r=0.999 9）,平均回收率为98.77%,RSD为2.73%（n=9）。结论: 所建立的定性鉴别方法专属性强,重复性好,定量方法操作简便,准确可靠,可用于平疣颗粒的质量控制。     

前列丹颗粒的质量控制方法研究

摘 要 目的： 建立前列丹颗粒的质量控制方法。方法: 采用薄层色谱法薄层对方中半枝莲、黄芪、炙甘草、补骨脂、姜黄进行定性鉴别;以高效液相色谱法对君药半枝莲中野黄芩苷进行含量测定。结果: 薄层斑点清晰,分离良好,阴性无干扰;野黄芩苷在3.96~79.20 μg·mL^-1范围内呈良好线性关系（r=0.999 9）,平均加样回收率为99.34%（RSD=1.25%,n=9）。结论:本研究建立的质量控制方法准确、可靠、稳定、专属性强,可有效用于前列丹颗粒的质量控制。     

伤痛宁胶囊的质量标准研究

摘 要 目的： 建立伤痛宁胶囊的质量标准。方法: 采用显微鉴别方法对方中僵蚕、全蝎、土鳖虫、地龙、三七、天麻进行鉴别;采用薄层色谱法对方中川芎、当归、三七、续断、甘草进行定性鉴别;采用高效液相色谱法对甘草苷进行含量测定：色谱柱为Agilent TC C₁₈（250 mm×4.6 mm,5 μm）,流动相为乙腈-水（15∶85）,流速为1.0 ml·min^-1,检测波长为276 nm。结果: 显微鉴别特征明显可见;薄层色谱鉴别斑点清晰、分离较好,阴性对照无干扰;甘草苷在0.341～1.193 μg范围内与峰面积呈良好的线性关系（r=0.999 9）,平均加样回收率为98.97%,RSD=0.77%（n = 6）。结论:方法准确可靠、重现性好,能有效控制伤痛宁胶囊的药品质量,为完善和提高伤痛宁胶囊的质量标准提供了依据。     

扶正抗瘤丸的质量标准

摘 要 目的： 为提高扶正抗瘤丸的质量,现进一步完善其质量控制标准。方法: 对方中虎杖、丹参、黄芪、当归和川芎5味药进行薄层色谱鉴别,同时采用高效液相色谱法对方中黄芩苷进行含量测定。结果: 薄层色谱中斑点清晰,专属性强;黄芩苷在31~310 μg·mL^-1范围内成良好的线性关系,平均回收率为101.11%（RSD=1.26%,n=9）。结论:本方法简便、准确、可靠、重现性好,可用于扶正抗瘤丸的质量控制。     

止血养元口服液质量标准研究

摘 要 目的： 建立止血养元口服液的质量标准。方法: 采用薄层色谱法鉴别止血养元口服液中小蓟、蒲黄和川芎;高效液相色谱法测定止血养元口服液中蒲黄主要成分香蒲新苷的含量。结果: TLC中,供试品在与对照药材或对照品相应位置上出现相同颜色的斑点,阴性对照无干扰;HPLC中香蒲新苷浓度在20～320 μg·ml^-1范围内线性关系良好 （r=0.999 8）,平均回收率为97.0％,RSD为2.0％（n=6）。结论: 本方法准确、可靠、重复性好,可用于该制剂的质量控制。     

多波长HPLC法同时测定皮肤康洗液中5种有效成分的含量

摘 要 目的：建立多波长切换高效液相色谱法同时测定皮肤康洗液中芍药苷、甘草苷、甘草酸铵、大黄素和蛇床子素5种有效成分的含量。方法: 色谱柱为 Diamonsil C18柱(200 mm×4.6 mm,5 μm);流动相为乙腈 0.1%盐酸水溶液,梯度洗脱;流速为1.5 ml·min^-1;柱温为30℃;检测波长为232 nm(0～6 min,检测芍药苷)、277 nm(6～10 min,检测甘草苷)、254 nm(10 min以后,检测甘草酸铵、大黄素、蛇床子素）。结果: 芍药苷、甘草苷、甘草酸铵、大黄素和蛇床子素的线性范围分别为28.20～282.0 μg·ml^-1（r=0.999 7）、12.150～121.500 μg·ml^-1（r=0.998 8）、13.420～134.200 μg·ml^-1（r=0.999 5）、0.047～0.466 μg·ml^-1（r=0.999 9）、2.380～23.800 μg·ml^-1（r=0.999 9）,平均加样回收率分别为98.49%,99.00%,98.38%,97.36%,97.70%,RSD分别为0.71%,0.62%,0.85%,0.92%,0.78%（n=6）。结论:该方法简便、准确、灵敏度高、重复性好,可用于同时测定皮肤康洗液中上述5个有效成分的含量。     

六味颈康胶囊质量标准的建立

摘 要 目的：建立六味颈康胶囊质量标准。方法: 用TLC法对处方中白芍、甘草、续断、粉葛进行定性鉴别;用HPLC法测定其主要活性成分葛根素、芍药苷、甘草苷、甘草酸铵的含量,色谱柱为ZORBAX SB C₁₈柱(250 mm×4.6 mm,5 μm);流动相为乙腈 0.1%磷酸水溶液,进行梯度洗脱;流速为1.0ml·min^-1;柱温为30℃;检测波长为0～7 min、在250 nm波长下检测葛根素,7～10 min在232 nm波长下检测芍药苷,10～14 min在276 nm波长下检测甘草苷,14 min在250 nm波长下检测甘草酸铵;进样量为10 μl。结果: TLC法可鉴别白芍、甘草、续断、粉葛的特征斑点且阴性样品无干扰,4个有效成分的线性范围分别为：葛根素2.644～26.440μg·ml^-1（r=0.999 9）、芍药苷65.200～652.000 μg·ml^-1（r=0.999 2）、甘草苷12.620～126.200 μg·ml^-1（r=0.999 9）、甘草酸铵13.280～132.800 μg·ml^-1（r=0.998 9）,平均加样回收率分别为98.74%,99.24%,98.69%,98.19%,RSD分别为0.71%,0.40%,0.78%,0.84%（n=6）。结论:该方法简便、准确、灵敏度高、重复性好,可有效控制六味颈康胶囊的产品质量。     

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.