HPLC测定抗脑衰胶囊中葛根素的含量

目的建立抗脑衰胶囊中葛根素的含量测定方法。方法采用50%甲醇提取,HPLC法测定。结果加样回收率为99·77%,RSD=1·23%(n=5),tR=11.2min。结论所用方法可用于抗脑衰胶囊的质量控制。     

高效液相色谱法测定抗脑衰胶囊中大黄素的含量

目的采用高效液相色谱法测定抗脑衰胶囊中大黄素的含量,以控制该制剂的质量.方法精密称定不同批次的抗脑衰胶囊内容物,经水解、提取、用高效液相色谱测定.结果大黄素在11.0～33.0 mg·L-1内呈良好的线性关系,r=0.999 9,平均加样回收率为97.0%(RSD为1.8%,n=5).结论本法测定抗脑衰胶囊中大黄素的含量,结果准确,重复性好.     

抗脑衰胶囊制剂HPLC指纹图谱建立及质量相关性研究

目的:以抗脑衰胶囊为对象,研究准确反映制剂内在整体质量的分析方法。方法:采用高效液相色谱分析法建立抗脑衰胶囊制剂的指纹图潜,指纹图谱中28个共有吸收峰为抗脑衰胶囊内在物质的指纹特征。通过成药、药材、标准物对照品及相应药材阴性的对比研究,确定了相对保留时间21.3 min 为葛根素专属吸收峰(9号),相对保留时间23.2 min 为芍药苷专属吸收峰(12号),相对保留时间36.7 min 为黄芩苷专属吸收峰(19号)。其 HPLC 指纹图谱条件为:天河 Kromasil ODS C_(18)柱(4.6 mm×250 mm,5μm);甲醇-0.6%醋酸水溶液系统梯度洗脱:流动相比例0 min,10:90;60 min,90:10;流速:0.9 mL·min~(-1);柱温25℃;检测波长:280 nm。利用2004年 A 版《中药色谱指纹图谱相似度评价系统》计算软件,对10批次制剂指纹图谱的相似度进行评价。结果:不同批号制剂的相似度有较大差异,其中010105、020523、020850三个批次制剂相似度低于0.8,说明这些批次制剂可能在原料药材选择、提取工艺及干燥过程中存在问题。结论:抗脑衰胶囊制剂的指纹图谱能够全面反映制剂的整体质量,是一种有效的中药制剂质量分析的方法。     

反相高效液相色谱法测定脑得生胶囊中葛根素的含量

目的采用高效液相色谱法测定脑得生胶囊中葛根素的含量,以控制该制剂的质量.方法以C18化学键合硅胶柱分离葛根素,以甲醇-乙腈-水(9∶8∶90)为流动相,UV检测波长250nm.结果方法的平均加样回收率为98.8%,RSD=1.08%(n=5).葛根素在0.25～2.5μg范围内,进样量与吸收面积值呈良好的线性关系.结论本法测定脑得生胶囊中葛根素的含量,结果准确,重复性好.     

HPLC法同时测定益脑复健胶囊中葛根素和芍药苷的含量

目的:建立测定益脑复健胶囊中葛根素和芍药苷含量的HPLC法.方法:色谱柱为HypersilBDS C18(250 mm×4.6 mm,5 μm),流动相为水-甲醇-乙腈(81:9:10),流速为1.0 ml·min-1,检测波长为230 nm.结果:葛根素在0.121～0.727 μg范围内线性关系良好,r=0.999 8,平均回收率为99.77%,RSD为0.8%(n=9);芍药苷在0.106～0.634 μg范围内线性关系良好,r=0.999 5,平均加样回收率为99.38%,RSD为0.8%(n=9).结论:本方法操作简便、结果准确、重复性好,可用于益脑复健胶囊的质量控制研究.     

反相高效液相色谱法测定脑得生胶囊中葛根素的含量

目的　采用高效液相色谱法测定脑得生胶囊中葛根素的含量 ,以控制该制剂的质量。方法　以C1 8化学键合硅胶柱分离葛根素 ,以甲醇 -乙腈 -水 (9∶8∶90 )为流动相 ,UV检测波长 2 5 0nm。结果　方法的平均加样回收率为 98.8% ,RSD =1 0 8%(n =5 )。葛根素在 0 .2 5～ 2 .5 μg范围内 ,进样量与吸收面积值呈良好的线性关系。 结论　本法测定脑得生胶囊中葛根素的含量 ,结果准确 ,重复性好     

HPLC法测定障眼明胶囊和片剂中葛根素和芍药苷的含量

目的:建立用高效液相色谱法测定障眼明胶囊和片剂中葛根素和芍药苷含量的方法.方法:采用Diamonsil-C18色谱柱(250 mm×4.6 mm,5 μm),流动相:乙腈-0.1%磷酸溶液(13:87),柱温20℃,流速为1.0 ml·min-1,检测波长为230 nm和250 nm.结果:葛根素在49.98～374.85 ng范围内线性关系良好(r=0.997 8),平均回收率为98.6%和98.7%.芍药苷在182.14～1 366.05 ng范围内线性关系良好(r=0.999 9),平均回收率为99.5%和98.7%.结论:该法简便,可靠,准确,可作为测定障眼明胶囊和片剂中葛根素和芍药苷含量的方法.     

HPLC法测定抗感解毒胶囊中葛根素的含量

目的建立抗感解毒胶囊中葛根素的高效液相色谱含量测定方法。方法采用HPLC法,C18色谱柱(250mm×4.6mm,5μm),以甲醇-水(25∶75)为流动相,流速:1.0mL·min-1,检测波长:250nm。结果葛根素浓度在4.008～200.4μg·mL-1的范围内与峰面积呈良好的线性关系,Y=0.0126X+0.0141,r=1.000(n=6),平均回收率为99.95%,RSD=0.19%。结论该方法简便、准确,可作为抗感解毒胶囊的质量控制方法。     

反相高效液相色谱法测定脑得生胶囊中葛根素的含量

目的：采用高效液相色谱法测定脑得生胶囊中葛根素的含量，以控制该制剂的质量。方法：以C18化学键合硅胶柱分离葛根素，以甲醇-乙腈-水（9：8：90）为流动相，UV检测波长250nm。结果：方法的平均加样回收率为98.8％，RSD=1.08%(n=5)。葛根素在0.25-2.5μg范围内，进样量与吸收面积值呈良好的线性关系。结论：本法测定脑得生胶囊中葛根素的含量，结果准确，重复性好。     

葛根异黄酮胶囊葛根素含量测定

目的:建立高效液相色谱法测定葛根异黄酮胶囊葛根素含量的方法。方法:采用HPLC外标法,测定以30%乙醇超声溶解提取葛根异黄酮胶囊的葛根素含量,固定相为Kromasil C18,流动相为甲醇-水(25∶75),UV检测波长为250 nm。结果:葛根素溶液在9.66~96.60μg/ml浓度范围内浓度与峰面积成良好线性关系,r=0.9999,平均加样回收率为99.51%,RSD=1.55%(n=6)。结论:方法简便具有良好的准确性和精密性,结果可靠。     

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.     

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.