复方奥硝唑大黄口腔膜的制备工艺优化

目的：优化复方奥硝唑大黄口腔膜的制备工艺。方法：以奥硝唑和大黄提取物为主药,聚乙烯醇（PVA）、羧甲基纤维素纳（CMC—Na）、甘油和甜味素为辅料。以黏附力、黏膜累积透过率为筛选指标,采用正交试验优化复方奥硝唑大黄口腔膜的制备工艺,并用高效液相色谱测定膜剂中奥硝唑体外释放度。结果：最优处方为PVA17-88：CMC—Na=2：1,甘油为4％,水为18倍。该膜剂在体外试验中24h后仍有药物释放。结论：该口腔膜制备工艺简便,兼有良好的缓释作用。     

奥硝唑加替沙星滴鼻液的制备与质量控制

目的:制备奥硝唑加替沙星滴鼻液并建立质量标准.方法:以奥硝唑、加替沙星为原料制备滴鼻液,并采用高效液相色谱法测定滴鼻液中奥硝唑和加替沙星含量.结果:本制剂稳定性好,无刺激性,含量测定方法快速准确.奥硝和加替沙星的线性范围均为2～10 mg·L-1,其平均回收率分别为100.36%,100.69%.结论:本制剂制备工艺简单,质量控制易行,稳定性好.     

处方和工艺参数对奥硝唑生物可降解凝胶剂体外释药曲线的影响

目的：考察处方和制备工艺对奥硝唑生物可降解凝胶剂体外释药曲线的影响。方法：以乳酸一羟基乙酸共聚物[poly（lactic-co-glycolic acid），PLGA]为载体材料制备了奥硝唑凝胶剂，采用高效液相色谱法测定凝胶剂中药物的含量，紫外分光光度法测定体外释放度。考察PLGA的型号、溶媒、PLGA与溶媒的比例，药物与PLGA的比例等因素对奥硝唑凝胶体外释放度的影响。结果：以PLGA（50：50，10000）为载体材料，以N-甲基-2-吡咯烷酮为溶媒制备凝胶。当处方中含药物2oA，PLGA（50：50，10000）49％，NMP49％时，奥硝唑凝胶可缓释7d，0～5d以近零级的方式缓释（R^2=0．9943）。结论：奥硝喳凝胶剂具有较好的缓释特征，处方和制备工艺简单可行。     

复方环丙沙星栓剂的制备及其含量测定

目的 制备环丙沙星-奥硝唑复方栓剂并建立其含量测定方法.方法 以PEG400,PEG6000为基质,熔融法制备环丙沙星-奥硝唑复方栓剂,采用高效液相色谱法进行含量测定.结果 制备得到水溶性基质的环丙沙星-奥硝唑复方栓剂;环丙沙星在41.6～416 μg·mL-1浓度范围内线性关系良好(r=0.999 1),平均回收率为(98.45±0.51%)%;奥硝唑在43～430 μg·mL-1浓度范围内线性关系良好(r=0.999 6),平均回收率为(98.70±0.49)%.结论 该制备工艺简单,含量测定方法操作简便,测定结果准确可靠,可用于复方环丙沙星栓剂的质量控制.     

高效液相色谱法测定奥硝唑片的含量

奥硝唑是第三代硝基咪唑类衍生物,对本品的含量测定方法常采用紫外分光光度法[1,2],有文献报道采用高效液相色谱法[3],本文参考有关文献[4]建立了测定奥硝唑片含量的高效液相色谱法,结果可靠.     

高效液相色谱法测定奥硝唑片的含量

目的建立奥硝唑片中奥硝唑的含量测定方法。方法采用高效液相色谱法，固定相：ODS-C18色谱柱(4.6 mm×150 mm，5 μm)；流动相：甲醇∶纯化水(30∶70)；流速：1.0 mL·min^-1；外标法定量；检测波长：318 mm。结果奥硝唑在20～200 μg·mL^-1范围内峰面积与浓度呈良好的线性关系，r＝0.999 9，平均回收率100.13%，RSD＝0.76%。结论该方法简便、快速、准确，适于奥硝唑片的含量测定。     

高效液相色谱法同时测定复方奥硝唑阴道生物黏附膜中2组分的含量

<正>复方奥硝唑阴道生物黏附膜是以壳聚糖为主要成膜材料,采用固体分散和溶解技术加入奥硝唑、盐酸环丙沙星等药物制成,是应用于阴道黏膜而缓慢定位释放药物的一种生物黏附药物传输系统[1]。本试验建立的高效液相色谱(HPLC)法同时测定复方奥硝唑阴道生物黏附膜中奥硝唑、盐酸环丙     

复方奥硝唑泡腾栓的制备与质量控制

目的 制备复方奥硝唑泡腾栓并建立其质量控制方法. 方法 以奥硝唑,硝酸咪康唑为主药制成泡腾栓,采用高效液相色谱法测定栓剂中奥硝唑及硝酸咪康唑的含量,并考查该制剂稳定性. 结果 制剂稳定性较好. 含量测定方法 准确,奥硝唑及硝酸咪康唑均在40~200 μg.mL^-1浓度范围内线性关系良好,平均回收率分别为100.09%(RSD=0.15%),100.02%(RSD=0.35%). 结论 复方奥硝唑泡腾栓处方及制备工艺合理,质量稳定可控.     

奥硝唑含漱液的制备及质量控制

目的制备奥硝唑含漱液并建立其含量测定方法。方法以高效液相色谱法测定制剂中奥硝唑的含量。结果奥硝唑在20~200μg.mL-1峰面积与浓度呈良好线性关系,r=0.999 9,平均回收率为100.13%,RSD为0.31%。结论本制剂制备和含量测定方法简便、快速、准确、质量可控。     

右旋酮洛芬贴片的制备与体外释放度测定

目的 建立复方奥硝唑缓释膜的制备与质量控制方法，验证基临床疗效。方法 以奥硝唑为主药配伍地塞米松，以聚乙烯醇为缓释剂，制备复方奥硝唑缓释膜。采用高效液相色谱法测定含量，并进行临床观察。结果 采用高效液相色谱法测定奥硝唑含量的平均回收率为100.12%，RSD为1.21%。复方奥硝唑缓释膜治疗牙周炎、冠周炎的总疗效与奥硝唑片相近。结论 复方奥硝唑缓释膜的制备工艺合理，含量测定结果准确，质量控制方法简便、快捷、准确，临床疗效较好，值得推广。     

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.     

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.