胃消合剂质量标准研究简

目的研究胃消合剂的质量控制方法。方法用薄层色谱（TLC）法对白术、玄胡索进行定性鉴别,采用高效液相色谱（HPLC）法对黄连中盐酸小檗碱的含量进行测定。结果薄层色谱图清晰,专属性强;盐酸小檗碱进样量在0．062～1．804μg范围内与峰面积呈良好线性关系（r=0．9999）,平均加样回收率为95．98％,RSD为0．89％（n=6）。结论该方法操作简便,准确,重现性好,能有效控制胃消合剂的质量。     

HPLC法测定交泰片中盐酸小檗碱的含量

目的：采用高效液相测定交泰片中盐酸小檗碱的含量。方法：采用Hypersil C18色谱枉（250mm×4．6mm,10μm）,以乙腈-0．1％磷酸（含磷酸二氢钾0．2％、十二烷基硫酸钠0．04％）（45：55）为流动相,检测波长345nm,流速1．0ml·min^-1。结果：盐酸小檗碱在1．01～30．30μg范围内线性关系良好,r=0．9999;平均回收率为99．6％（n=6）,RSD=0．88％。结论：该方法准确,简便,快速,为交泰片中盐酸小檗碱建立了质量控制方法。     

高效液相色谱法测定双黄消炎片中黄芩苷和盐酸小檗碱的含量

目的 建立高效液相色谱法同时测定双黄消炎片中黄芩苷和盐酸小檗碱含量的方法。方法采用ODS C18（200mm×4．6mm，5μm）色谱柱，流动相为乙腈0．05mol·L^-1磷酸二氢钾溶液三乙胺（25：75：0．05），流速为1．0mL·min^-1，检测波长为265nm。结果黄芩苷和盐酸小檗碱分别在19．0-380．0μg·mL^-1（r=0．9999）、1．01-20．18μg·mL^-1（r=0．9999）内线性关系良好，平均加样回收率（n=6）分别为100．1％和98．5％。结论该方法简便、准确、重复性好，可同时测定双黄消炎片中黄芩苷和盐酸小檗碱的含量。     

烧伤擦剂质量标准的建立

目的：建立烧伤擦剂的质量标准。方法：采用TLC法对方中黄连、黄柏进行定性鉴别,采用HPLC法测定制剂中盐酸小檗碱的含量。结果：薄层色谱斑点清晰,分离度好;盐酸小檗碱在0．2～1．2μg范围内,与峰面积呈良好线性关系（r=0．9997）,平均回收率为99．07％,RSD=0．31％（n=6）。结论：该方法专属性强,准确,重复性好,简便易行,可作为烧伤擦剂的质量控制方法。     

HPLC法测定双黄消炎片中盐酸小檗碱的含量

目的采用高效液相色谱法测定双黄？肖炎片中盐酸小檗碱的含量。方法Kromasil C18色谱柱（250mm×4．6mm,5μm）;乙腈-0．05mol·L^-1磷酸二氢钾溶液（25：75）为流动相,流速为1．0ml·min^-1;检测波长为347am。结果盐酸小檗碱线性范围为9．2。146．4mg·L^-1（r=0．9999,n=5）,平均回收率为99．93％,RSD=0．60％（n=6）。结论该方法准确、简便,可用于该制剂的质量控制。     

高效液相色谱法测定痔疮片中盐酸小檗碱含量

目的：建立高效液相色谱法（HPLC法）以测定痔疮片中盐酸小檗碱的含量。方法：采用Alltima C18柱，以0．033mol／L的磷酸二氢钠溶液-乙腈（70：30）为流动相，流速为1．0mL／min，检测波长为265nm。结果：痔疮片中盐酸小檗碱线性范围是84.24—421．2ng，r=0．9999；平均回收率为98．72％，RSD为0．76％（n=6）。结论：HPLC法准确、重现性好，可作为该制剂的质量控制方法。     

高效液相色谱法测定消渴平胶囊中盐酸小檗碱含量简

目的建立测定消渴平胶囊中盐酸小檗碱含量的高效液相色谱法。方法色谱枉为InertsilC18枉（250mm×4．6mm,5μm）,流动相为0．1％磷酸溶液（每100mL加十二烷基磺酸钠0．1g）-乙腈（52：48）,检测波长为265nm。结果盐酸小檗碱进样量线性范围为0．03095～0．07225μg,r=0．9999;平均加样回收率为100．60％,RSD=0．93％（n=6）。结论该方法线性关系良好、简便、准确、专属性强,可作为控制消渴平胶囊原药材和成品质量的方法。     

高效液相色谱法测定小儿肠胃康颗粒中盐酸小檗碱含量

目的建立小儿肠胃康颗粒盐酸小檗碱含量的测定方法。方法采用反相Prodigy ODS3色谱柱（250mm×4．6mm，5μm），柱温为35℃，流动相为乙腈-水（含0．4％磷酸，0．7％三乙胺）溶液（25：75），测定波长为350nm，以外标法定量。结果盐酸小檗碱质量浓度在4．01～200．5μg／mL范围内与峰面积线性关系良好（r=0．9999），平均回收率为98．45％，RSD=0．81％（n=6）。结论用高效液相色谱法测定小儿肠胃康颗粒中盐酸小檗碱的含量，操作简便，结果准确。     

泌感片的薄层鉴别和盐酸小檗碱的含量测定

目的应用薄层色谱法对黄柏、甘草、柴胡、续断进行鉴别和高效液相色谱法测定盐酸小檗碱的含量。方法采用薄层色谱鉴别黄柏、甘草、柴胡、续断及高效液相色谱测定盐酸小檗碱含量,Shim—pack—C18柱（5μm,250mm×4．6mm）,乙腈0．05mol·L^-1-磷酸二氢钠溶液（28：72）为流动相,检测波长347nm。结果薄层斑点清晰,含量测定线性范围为9．95～99．5mg·L^-1;r=1．0000,回收率为99．42％,RSD=1．21％。结论薄层色谱可用于黄柏、甘草、柴胡、续断的定性鉴别,且高效液相色谱法测定泌感片中盐酸小檗碱的含量具有操作简便、结果准确、灵敏的特点,可用于该制剂的质量控制。     

HPLC法测定盐酸黄连素溶液中盐酸小檗碱含量

目的：建立HPLC法测定盐酸黄连素溶液中盐酸小檗碱含量。方法：使用Hypersil ODS2 C18（200mm×4．6mm,5μm）;乙腈：磷酸盐缓冲液[0．05mol·L^-1磷酸二氢钾和0．05mol·L^-1庚烷磺酸钠（1：1）]（50：50）为流动相,流速1ml·min^-1,检测波长263nm。结果：盐酸小檗碱在0．848～4．240μg进样范围内线性关系良好（r=0．9999）,平均回收率99．0％（RSD=1．11％）。结论：本法快速、简便、准确。     

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.