清热败毒颗粒剂的质量标准研究

目的 建立清热败毒颗粒剂的质量标准。方法 采用薄层色谱法（TLC）鉴别处方中的板蓝根、连翘、紫花地丁和甘草,采用高效液相色谱法（HPLC）测定绿原酸的含量,色谱柱为Agilent ZORBAX SB-C₁₈柱（4.6 mm×250 mm,5 μm）;流动相为乙腈（A）与含0.2%甲酸的水溶液（B）,梯度洗脱：0~12 min,11%~12%A;流速：1.0 ml/min;柱温：30 ℃;检测波长：327 nm;进样量：20 μl。结果 薄层鉴别色谱中特征斑点明显,专属性强。绿原酸在6.19~396.00 μg/ml浓度范围内呈良好线性关系,其回归方程为Y=60.239 4X+9.096 3（r>0.999 9）,回收率为99.66%（RSD=2.82%）。结论 该法简便、稳定可靠、重复性好,为控制清热败毒颗粒的质量标准提供了可借鉴的依据。     

复方颠茄合剂质量标准研究

目的 提高复方颠茄合剂的质量控制标准。方法 采用薄层色谱法（TLC）对复方颠茄合剂中的吗啡进行定性鉴别;采用高效液相色谱法（HPLC）测定复方颠茄合剂中吗啡的含量。以WondaSil C₁₈（4.6 mm×150 mm,5 μm）为色谱柱;A相：0.01 mol/L磷酸二氢钾溶液-0.002 5 mol/L庚烷磺酸钠溶液（含0.1%三乙胺,磷酸调pH至2.5）,B相：乙腈,A∶B=90∶10为流动相;流速：1.0 ml/min;检测波长：220 nm;柱温：30 ℃。结果 在TLC图谱中可检出吗啡的特征斑点。吗啡在0.525~10.5 μg/ml范围内与其峰面积线性关系良好（r=0.999 9）,平均回收率为99.44%,RSD= 0.23%（n=9）。结论 本方法简便准确,专属性强,能够用于复方颠茄合剂的含量测定和质量控制。     

复方黑参颗粒质量标准研究

目的 建立复方黑参颗粒的质量标准。方法 采用TLC法对复方黑参颗粒中玄参和射干进行定性鉴别,应用HPLC法同时测定肉桂酸、射干苷和次野鸢尾黄素的含量,色谱柱为Kromasil C₁₈柱（150 mm×4.6 mm,5 μm）,流动相为乙腈（A）-0.1%磷酸（B）水溶液,进行梯度洗脱;柱温30℃,检测波长270 nm;流速1.0 ml/min。结果 采用TLC法对玄参和射干进行定性鉴别具有良好的专属性,阴性对照无干扰。肉桂酸、射干苷、次野鸢尾黄素分别在16.22~113.57 μg/ml（r=0.999 8）、48.19~337.34 μg/ml（r=0.999 8）、16.40~114.80 μg/ml（r=0.999 9）范围内与峰面积呈良好的线性关系,平均加样回收率分别为99.23%、98.82%、99.17%。结论 本实验建立的方法快速、简便、重复性好,可用于复方黑参颗粒的质量标准控制。     

高效液相色谱法测定康得灵胶囊中黄芩苷的含量

目的 建立康得灵胶囊中黄芩苷的HPLC测定方法。方法 色谱柱为Agilent Tc-C₁₈色谱柱（4.6 mm×250 mm,5 μm）,柱温为30 ℃;流动相为乙腈-0.5‰磷酸溶液（26：74）,流速为1.0 ml/min,检测波长265 nm。结果 黄芩苷保留时间约为16 min。以峰面积（Y）对进样浓度（X, μg/ml）线性回归,得回归方程：Y=22 114.67 X－112 836.7,r=0.998 8,线性范围5.410~108.2 μg/ml。平均加样回收率为98.78%,RSD为0.74%。结论 本方法操作简便,测定结果准确可靠,可用于康得灵胶囊中黄芩苷的含量测定。     

康咳灵合剂质量标准研究

目的 建立康咳灵合剂的质量标准。方法 采用薄层色谱法（TLC）对矮地茶、百部进行定性鉴别;采用高效液相色谱法（HPLC）测定岩白菜素的含量。色谱柱为Lichrospher C₁₈柱（4.6 mm×250 mm,5 μm）;流动相：甲醇-水（20：80）;检测波长：275 nm;柱温：30℃;流速：1 ml/min。结果 TLC法能准确鉴别矮地茶和百部,斑点清晰;岩白菜素在0.064 8~0.648 μg（r=0.9998）范围内线性关系良好,平均回收率100.24%（RSD为1.9%,n=6）。结论 本实验建立的方法简便、专属性高、重复性好,结果准确可靠,可用于康咳灵合剂的质量控制。     

高效液相色谱法测定气管炎颗粒中黄芩苷的含量

目的 建立高效液相色谱法测定气管炎颗粒中黄芩苷的含量。 方法 采用HPLC法,色谱柱:ZORBAX SB-C₁₈柱(4.6 mm×150 mm,5 μm),以甲醇-0.1%磷酸(47:53)为流动相,流速为1 ml/min,检测波长为280 nm。 结果 黄芩苷在6.63~210 μg/ml范围内呈良好线性关系(r=0.999 8,n=6),平均加样回收率为98.16%,RSD为1.89%。 结论 本法简便、灵敏、准确、重复性好,结果可靠,可有效地控制气管炎颗粒的质量。     

健脾补肾颗粒的质量标准研究

目的 建立健脾补肾颗粒的质量标准。方法 采用薄层色谱法（TLC）鉴别制剂中黄芪、丹参、党参、陈皮和白芍五味药材。用高效液相色谱法（HPLC）测定白芍中芍药苷的含量：色谱柱：Agilent Eclipse Plus C₁₈柱（4.6 mm×250 mm,5 μm）;流动相：乙腈-0.1%磷酸水溶液梯度洗脱;流速：1.0 ml/min;柱温：25℃;检测波长：230 nm。结果 5种药材的TLC图谱斑点清晰,无阴性对照干扰;芍药苷在8.676~277.632 μg/ml范围内线性关系良好,（r=0.999 9）。结论 该法操作简单、重复性好,能够有效控制健脾补肾颗粒的质量。     

高效液相色谱法测定壮骨颗粒中补骨脂素与异补骨脂素的含量

目的 建立高效液相色谱法测定壮骨颗粒中补骨脂素和异补骨脂素的含量。方法 色谱柱为Agilent Zorbax C₁₈柱（4.6 mm×250 mm,5 μm）,流动相为甲醇-水（45：55）,检测波长为245 nm,流速为1.0 ml/min,柱温为25 ℃,进样量为10 μl。采用70%乙醇水浴方法提取壮骨颗粒中的补骨脂素和异补骨脂素。结果 补骨脂素与异补骨脂素在3.75~40 μg/ml范围内呈良好的线性关系,对方法精密度（n=6）、重复性（n=6）和稳定性（12 h）进行考察,相对标准偏差（RSD）均小于2%。加样回收率（n=6）为94%~105%。结论 该测定方法简便、快速、准确,可用于壮骨颗粒的临床快速质量控制。     

益视明目颗粒质量标准研究

目的 建立益视明目颗粒的质量标准。方法 用薄层色谱法（TLC）鉴别制剂中的枸杞子、丹参;用高效液相色谱法（HPLC）定量测定丹参素钠的含量。色谱柱：Kromasil C₁₈柱（4.6 mm×150 mm,5 μm）;流速：0.4 ml/min;检测波长：280 nm;柱温：30 ℃;进样量：10 μl;流动相：甲醇-0.5%醋酸水溶液（10∶90）。结果 薄层色谱斑点清晰可见、阴性干扰小,可用于鉴别益视明目颗粒中的枸杞、丹参;丹参素钠在2.00~60.00 μg/ml范围内线性关系良好,r=0.999 7（n=6）,平均加样回收率105.6%,RSD=1.60%。结论 建立的方法简便、准确、可靠性高、重现性好,可作为控制益视明目颗粒质量的有效方法。     

医院制剂感冒颗粒质量标准研究

目的 建立医院制剂感冒颗粒的质量标准。方法 采用薄层色谱法（TLC）对黄芩、黄柏、柴胡进行薄层鉴别;采用高效液相色谱法（HPLC）测定黄芩苷的含量,色谱柱为Agilent HC-C₁₈（250 mm×4.6 mm,5 μm）,流动相为甲醇-0.2%磷酸（43：57）,流速为1.0 ml/min,柱温30℃,检测波长为280 nm。结果 黄芩、黄柏、柴胡的薄层色谱图均斑点清晰,阴性无干扰;黄芩苷在1.81~72.40 μg/ml范围内浓度与峰面积线性关系良好（r=0.999 9）,平均回收率为98.55%,RSD为1.91%（n=9）。结论 本研究建立的鉴别方法重现性更好,确定了黄芩苷的含量测定方法,增强了该制剂质量的可控性。     

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.     

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.     

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.