高效液相色谱法测定生津消渴胶囊中黄芩苷的含量

目的:建立生津消渴胶囊中黄芩苷的含量测定方法。方法:采用HPLC法测定黄芩苷的含量,流动相为:甲醇-水-磷酸(47:53:0．2)。检测波长:280nm。结果:本法可用于测定生津消渴胶囊中黄芩苷的含量。     

HPLC法测定不同厂家银黄颗粒中黄芩苷的含量

目的建立RP—HPLC测定银黄颗粒制剂中黄芩苷含量的方法及测定不同厂家银黄颗粒制剂中黄芩苷的含量。方法采用HPLC法检测银黄颗粒制剂中黄芩苷的含量,色谱条件：Kromasil C18色谱柱,以乙腈-0．4％磷酸水溶液（含0．6％三乙胺,28：72）为流动相,流速1ml／min,检测波长275nm,柱温为室温。结果黄芩苷在0．504～16．128mg／L范围内与峰面积呈良好的线性关系（r=0．99985）,平均回收率为97．25％,RSD=2．54％（n=6）。结论本文中所建立的色谱方法可以简便、准确测定银黄颗粒中黄芩苷的含量,重现性较好。各厂家生产的银黄颗粒中黄芩苷含量差别较大,有必要建立黄芩苷的定量控制方法。     

高效液相法测定宁神灵颗粒中黄芩苷的含量

目的：探讨高效液相法测定宁神灵颗粒中黄芩苷含量的方法,控制其质量。方法：Agilent C18（4．6mm×150mm,50μm）色谱柱,流动相为甲醇-水-磷酸（47：53：0．2）,流速为1ml／min,检测波长为280nm．结果：黄芩苷在0．056—1．395μg范围内呈良好的线性关系,回归方程为Y=136．67593X＋107．10440（r=0．9990）,平均回收率为99．84％（RSD=0．313％）,重现性RSD=0．877％。结论：本方法简便、快速、灵敏、准确、重现性好,可作为宁神灵颗粒中黄芩苷的质量控制标准。     

黄芩苷在不同溶媒中的稳定性研究

目的:研究黄芩苷在不同溶媒中的稳定性。方法:采用HPLC法测定黄芩苷的含量。结果:黄芩苷在0．1～50．0μg· ml-1范围内线性关系良好平均回收率为97．6％,RSD=2．0％。黄芩苷在pH=7．4的磷酸盐缓冲液中不稳定。结论:低浓度的黄芩苷在不同pH值溶液中的稳定性差异较大,为透皮扩散研究时pH值和浓度的选择提供了依据。     

枇杷清热养颜颗粒两种主要活性成分的质量控制研究

目的建立高效液相色谱法同时测定枇杷清热养颜颗粒中绿原酸和黄芩苷的含量。方法Agilent SB—C18柱,流动相：甲醇-0．2％磷酸水溶液（52：48）;流速：1．0ml／min;检测波长：324nm;柱温：室温。结果绿原酸线性范围为0．86～41．28mg／L,平均回收率为100．14％（RSD=1．06％）,回归方程为Y=4028．2X-13．106,r=0．9999;黄芩苷在0．7841．13mg／L范围内呈良好的线性关系,回归方程为：Y=3430．2X＋119．99（r=0．9992）,平均回收率为100．06％（RSD=1．09％）。结论此方法简便可靠,结果稳定,重复性好,可用于枇杷清热养颜颗粒中绿原酸和黄芩苷的含量测定。     

HPLC法测定风热颗粒中黄芩苷的含量

目的:建立HPLC法测定风热颗粒中黄芩苷含量的方法.方法:采用反相色谱柱;流动相为甲醇-水-冰醋酸(50:50:1);检测波长为274 nm.结果:黄芩苷在0.1248～0.624 0 μg范围内线性关系良好(r=0.999 9),平均回收率为100.25%,RSD为0.36%(n=6).结论:本方法灵敏、准确,可作为风热颗粒的质量控制方法.     

参柴颗粒的质量控制标准研究

目的：探讨参柴颗粒的质量标准。方法：采用TLC法对处方中黄芩,人参进行鉴别;用HPLC法测定黄芩苷的含量,结果：在TLC色谱中均能检出黄芩,人参;含量限度黄芩苷不得少于3．0％,结论：所用方法简便易行,测量结果准确,重复性好,可用来控制参柴颗粒的质量。     

热炎清颗粒的质量标准

目的：建立热炎清颗粒的质量标准。方法：采用薄层色谱法（TLC）对本品的黄芩、金银花进行鉴别;采用HPLC法测定本品中黄芩苷的含量。结果：薄层色谱中阴性样品无干扰;黄芩苷在0．18～1．13g（r=0．9997）范围内呈良好线性关系。平均加样回收率为97．9％（RSD=1．87％）。结论：该法简便,准确可靠。     

HPLC法测定平肝颗粒中芍药苷的含量

目的:建立HPLC法测定平肝颗粒中芍药苷的含量。方法:色谱柱:HYPERSIL ODS-2(150 mm×4．6 mm,5μm)。乙腈:水(17:83)为流动相。流速为0．8 ml·min-1,检测波长230 nm,柱温30℃。结果:芍药苷在0．04-0．23μg范围内线性关系良好,r=1．000 0,平均回收率为99．6％,RSD为0．9％。结论:方法灵敏准确,适用于该制剂的含量测定。     

HPLC 法测定双黄滴丸中黄芩苷和绿原酸的含量

目的建立HPLC法测定双黄连滴丸中黄芩苷和绿原酸含量的方法。方法采用C18色谱柱,乙腈-0．1％磷酸溶液为流动相（梯度洗脱）,流速为1．0ml-min^-1,检测波长为318nm。结果黄芩苷线性范围为0．1-0．5g·L^-1,平均回收率=98．50％,RSD=1．13％;绿原酸线性范围为0．024-0．12g·L^-1,平均回收率=98．25％,RSD=0．37％。结论该方法简便、可靠、准确,可用于该制剂的质量控制。     

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.     

Gender-related symptoms and correlates of alcohol dependence among men and women with a lifetime diagnosis of alcohol use disorders

This study explored gender-related symptoms and correlates of alcohol dependence in a crosssectional study of 150 men and 150 women with a lifetime diagnosis of alcohol use disorders (AUD). Participants were recruited in equal numbers from treatment settings, correctional centres and the general community. Standardized measures were used to determine participants' use of substances, history of psychiatric disorders and psychosocial stress, their sensation seeking and family history of substance use and mental health disorders. Multivariate analyses were used to detect patterns of variables associated with gender and the lifetime severity of AUD. Men had a longer history of severe AUD than women. Women had similar levels of alcohol dependence and medical and psychological sequelae as men, despite 6 fewer years of AUD. More women than men had a history of severe psychosocial stress, severe dependence on other substances and antecedent mental health problems, especially mood and anxiety disorders. There were differences in family history of alcohol-related problems approximating same-gender aggregation. The severity of a lifetime AUD was predicted by its earlier age at onset and the occurrence of other disorders, especially anxiety, among both men and women. The limitations in the generalizability of these findings due to sample idiosyncrasies are discussed.