比浊法自动测定可利霉素片的效价

目的:建立比浊法测定可利霉素片效价的方法。方法:以金黄色葡萄球菌为试验菌,加菌量为0.5%(V/V),温度为(37±0.5)℃,培养时间3.5～4.0h测定。结果:抗生素线性最佳浓度范围为6.4～15.7 u.mL-1,平均回收率为100.7%(n=9),RSD=1.7%。结论:本方法灵敏、快速、实用,可作为测定可利霉素片效价的方法。     

交沙霉素片含量的浊度测定法

建立浊度法测定交沙霉素片的方法.以肺炎克雷伯菌为试验菌,加菌量0.8%～1.0%(V/V),37℃±0.5℃培养4～5h左右测定.抗生素线性浓度为4.0～12.0u·mL-1,二剂量法的平均回收率为100.9%,RSD为2.0%(n=9).该方法灵敏,快速,影响因素较少,可作为测定交沙霉素片效价的方法.     

微生物比浊法测定口服阿奇霉素的效价含量

目的 建立以微生物比浊法测定口服阿奇霉素效价含量的方法.方法 采用比浊法测定阿奇霉素的含量,并对微生物比浊法、管碟法测定阿奇霉素效价的结果进行评价.结果 阿奇霉素的线性范围为0.4～1.32 u·mL-1(r=0.995 9),分散片与颗粒的平均回收率分别为100.11%,100.27%,方法重复性良好(RSD为0.4%),比浊法与管碟法测定结果一致.结论 微生物比浊法具有简便、精确、快速的特点,可以应用于该产品的质量控制.     

比浊法在线自动测定阿奇霉素制剂的效价

目的:建立比浊法测定阿奇霉素制剂的效价。方法:肺炎克雷伯菌为实验菌,加菌量1.5%～2.5%,(37±0.5)℃培养3.5～4.5 h 测定。结果:抗生素线性浓度为0.96～2.34 u·mL~(-1),高、中、低3种浓度的平均回收率分别为101.6%,99.4%与101.7%;RSD 分别为3.3%,1.4%,2.3%(n=3)。结论:本方法方便、快速、灵敏,可信限率低,结果准确,精密度好,可作为阿奇霉素原料及其制剂效价的测定方法。     

浊度法测定12-去羟基阿奇霉素的效价

目的建立浊度法测定12-去羟基阿奇霉素效价的方法。方法以肺炎克雷伯菌为试验菌,加菌量0.6%-1.0%（V/V）,37℃±0.5℃培养4h左右测定。结果抗生素线性浓度为2.0-10.0U/ml,二剂量法原料的平均回收率为101.2%,RSD为2.2%（n=9）。结论本方法灵敏,快速,影响因素较少,可作为测定12-去羟基阿奇霉素的效价的方法。     

浊度法测定盐酸米诺环素原料及其片剂的效价

目的 建立浊度法测定盐酸米诺环素原料及其片剂效价的方法.方法 :以金黄色葡萄球菌为实验菌,加菌量2.0%～4.0%(V/V),37 ℃±0.5 ℃培养约4 h测定.结果 :抗生素线性浓度为0.03～0.10 μg·mL-1,原料二剂量法的平均回收率为99.42%,RSD为2.1%(n=9);片剂二剂量法的平均回收率为100.22%,RSD为1.9%(n=9).结论 :本方法灵敏,快速,影响因素较少,可作为测定盐酸米诺环素原料及其片剂的效价的方法.     

浊度法测定土霉素原料药及其片剂的效价

目的:建立测定土霉素原料药及其片剂效价的浊度法。方法:采用浊度法,试验菌为金黄色葡萄球菌,加菌量为1.0%～1.5%(V/V),培养温度为37℃,培养时间为4h左右;同时与管碟法比较效价测定结果。结果:土霉素检测浓度的线性范围为0.05～0.4IU·mL-1,原料药平均回收率为99.59%(RSD=2.0%),片剂平均回收率为99.51%(RSD=1.91%);与管碟法比较含量无显著性差异。结论:本方法灵敏、快速、影响因素较少,可用于测定土霉素原料药及其片剂的效价。     

比浊法测定阿奇霉素效价的研究

目的:建立测定阿奇霉素效价的方法。方法:采用比浊法测定阿奇霉素的效价,并与管碟法比较。结果:阿奇霉素检测浓度的线性范围为0.4～2.0I U.mL-1(r=0.999 1) ;回收率为99.70%～100.02%(RSD为0.22%～0.46%) ;比浊法与管碟法的测定结果无显著性差异。结论:本方法操作更快捷、方便。     

微生物比浊法测定阿奇霉素颗粒的效价

目的 建立测定阿奇霉素颗粒效价的微生物比浊法.方法 分别采用微生物比浊法和管蝶法对阿奇霉素的含量进行测定和比较研究.结果 阿奇霉素的线性范围为1～10U·mL-1,r=0.9996,平均回收率为99.43%,RSD=0.3%.结论 微生物比浊法具有简便、精确、快速的特点,可以应用于该产品的质量控制.     

浊度法测定地红霉素效价

目的:建立浊度法测定地红霉素效价的方法,及效价测定的最佳条件并探讨地红霉素含量测定的最佳方法。方法:浊度法以金黄色葡萄球菌为实验菌,加菌量为1.5%～3%(V/V),(37±1)℃培养4～6h 测定。同时以高效液相色谱法、管碟法对样品及对照品进行测定。结果:地红霉素浊度法抗生素线性浓度范围为1.0～10.0μg·mL~(-1),回归方程为 A=384.448C 588.816,r=0.9998;一剂量、二剂量的平均回收率分别为102.5%(n=5)、101.7%(n=6),口内 RSD 分别为1.45%,0.94%;日间 RSD 分别为1.97%,1.12%。结论:浊度法灵敏,快速,可作为地红霉素效价测定法。     

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.