降糖甲胶囊薄层定性和定量方法的研究

目的 建立降糖甲胶囊的薄层定性和定量方法。方法采用薄层色谱法对处方中的黄芪、黄精、地黄进行鉴别；同时采用薄层扫描法测定黄芪甲苷的含量。结果薄层斑点显色清晰，阴性对照无干扰；黄芪甲苷平均回收率为97．56％，RSD=1．20％。结论结果准确，方法重复性好，可作为该制剂的质量控制指标。     

益肾胶囊的质量标准

目的：建立益肾胶囊的质量标准。方法：采用薄层色谱法对黄芪、山茱萸、丹参进行定性鉴别；用双波长锯齿扫描法测定黄芪中黄芪甲苷的含量。结果：黄芪甲苷含量在1．012－9．108μg范围内线性关系良好（r=0.9991)，平均回收率为97．7％，RSD为1．81％（n＝4）。结论：制定的质量标准可以保证益肾胶囊的质量。     

骨蚀扶正胶囊的制备及主药含量测定

目的：探讨骨蚀扶正胶囊的制备及其主要成分黄芪甲苷含量的测定方法。方法：采用水煮醇沉法制备胶囊；采用双波长薄层扫描法测定该制剂中黄芪甲苷的含量，结果：得膏率为22．50％；黄芪甲苷的平均回收率为97．26％，RSD为2．30％（n=5）。结论：制备工艺简单，得膏率高；含量测定方法灵敏，准确，专属性强。     

复方黄芪口服液质量标准的研究

目的：建立复方黄芪口服液的质量标准。方法：采用TLC法对处方中的何首乌，枸杞子进行定性鉴别；用薄层扫描法测定黄芪甲苷的含量。结果：在TLC色谱中均能检出何首乌，枸杞子；黄芪甲苷在1．001～8．008μg范围呈良好的残性关系，r=0．9991，平均回收率95．5％，RSD为1．4％。结论：所建立的方法能够准确地进行定性，定量检测，可用于该制剂的质量控制。     

薄层扫描法测定肾特康胶囊中黄芪甲苷含量

目的 建立测定肾特康胶囊中黄芪甲苷含量的薄层扫描法。方法 采用薄层扫描法测定黄芪甲苷含量，硅胶G板，氯仿-乙酸乙酯-甲醇-水（15：40：22：10）10℃以下放置过夜的下层溶液为展开剂，测定波长510nm，参比波长700nm。结果 黄芪甲苷点样量在O．4-2μg之间和吸收度积分值呈良好的线性关系，平均回收率为98．3％，RSD=1．20％。结论 薄层扫描法便捷、灵敏、准确，可作为肾特康胶囊的质量控制方法。     

三消丹的定性定量分析

目的：建立三消丹的定性定量分析方法。方法：采用薄层色谱法对制剂中丹参、葛根、黄芪和玄参进行定性分析；用薄层扫描法对黄芪中的黄芪甲苷进行定量分析。结果：黄芪甲苷在1．025～5．125斗g范围内线性关系良好(r=0．9995)，平均回收率为98．4％，RSD=0．57％。结论：该方法可作为该制剂的质量控制。     

五黄膏质量标准研究

本文对五黄膏中黄芩、黄芪、防已进行了薄层色谱鉴别研究，结果表明方法简便、易操作、重现性好，无干扰；同时用薄层扫描法测定了黄芪中黄芪甲苷的含量，结果表明方法可靠、稳定、灵敏度高。其平均回收率为95．85％，RSD为1．25％。     

益气通脉口服液的薄层鉴别及黄芪甲苷的含量测定

目的：建立益气通脉口服液的鉴别及含量测定方法。方法：采用薄层色谱法对其中丹参，延胡索，当归进行鉴别，并用薄扫描法测定其中黄芪甲苷的含量。结果：黄芪甲苷线性关系良好，线性范围1．03－5．15μg，加样回收率95．1％，RSD＝1．1％（n=5)。结论：该方法简便，重复性好，可用于该制剂的质量控制。     

薄层扫描法测定当归补血口服液中黄芪甲苷含量

目的用薄层扫描法测定当归补血口服液中黄芪甲苷的含量。方法采用以1％羧甲基纤维素钠作黏合剂的硅胶G薄层板,以10℃以下放置过夜的氯仿-甲醇-水（13：6：2）下层溶液为展开剂,双波长（As=520nm,An=700nm）扫描法测定当归补血口服液中黄芪甲苷的含量。结果黄芪甲苷点样量在1．006—8．048μg范围内与峰面积呈良好线性关系（n=0．9993）,平均加样回收率为98．28％,RSD=1．76％（n=6）。结论所用方法简单、准确、重现性好,可用于当归补血口服液的质量控制。     

前列复通颗粒的制备及质量控制

目的：研究提供前列复通颗粒的质量控制方法。方法：采用薄层色谱法（TLC）进行定性鉴别、薄层扫描法（TLCS）测定成品中黄芪甲苷的含量，并以此为指标进行方法学考察。结果：TLC鉴别专属性强，重现性好。黄芪甲苷加样回收率为98．4％；RSD为2．2％（n=5）。结论：方法操作简便，实用可行，可以有效控制成品的质量。     

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.