荷移分光光度法测定阿奇霉素含量

目的建立测定阿奇霉素(阿泽红霉素)制剂含量的方法.方法利用阿泽红霉素与茜素红在水-醇介质中发生电荷转移反应,形成电荷转移络合物,采用可见分光光度法测定.结果荷移反应生成的荷移络合物在525nm处有最大吸收,表观摩尔吸光系数是1.26×104L/(mol·cm),药物浓度在5～55mg/L内服从比耳定律,方法平均回收率在97.0%以上,RSD为0.95%(n=6).结论方法稳定、准确、灵敏、快速,对样品的测定结果令人满意.     

阿奇霉素片的茜素红荷移分光光度法测定

阿奇霉素与茜素红在乙醇-水溶液中发生荷移反应,由此建立了荷移分光光度法测定阿奇霉素片的含量.荷移反应生成1:2型络合物,最大吸收波长为538 nm,摩尔吸收系数为1.23×10 4L·mol-1·cm-1.阿奇霉素在10～60μg/ml浓度范围内线性关系良好.含量测定结果与HPLC法结果基本相符.     

克拉霉素与茜素红的荷移反应及其测定

目的建立测定克拉霉素制剂含量的方法。方法利用克拉霉素与茜素红在水-醇介质中发生电荷转移反应,形成电荷转移络合物,采用可见分光光度法测定。结果荷移反应生成的荷移络合物在526nm处有最大吸收,络合物的组成比是1∶1,表观摩尔吸光系数是7.71×103L.mol-1.cm-1,药物浓度在5~90mg/L范围内服从比耳定律,方法平均回收率在98.0%以上,RSD为1.3%(n=6)。结论方法稳定、准确、灵敏、快速,对样品的测定结果令人满意。     

荷移反应测定克拉霉素片的含量

目的 采用荷移反应法快速测定克拉霉素胶囊中的有效含量.方法 通过克拉霉素与2,4-二硝基苯酚的荷移反应,采用分光光度法测定克拉霉素片的含量.结果 克拉霉素与2,4-二硝基苯酚在乙醇-丙酮介质中发生电荷转移反应,产物的最大吸收波长为364 nm,表观摩尔吸光系数为1.55×10~4 L·mol~(-1)·cm~(-1),荷移络合物的组成比为1:1,相对标准偏差为0.98%(n=8),药物5～45 mg·L~(-1)与吸光度呈线性关系,回收率符合要求.结论 所用方法简便易行,条件易控,灵敏度高.     

荷移比色法测定交沙霉素

目的:建立测定交沙霉素制剂含量的方法。方法:利用交沙霉素与茜素红在水-醇介质中发生电荷转移反应,形成电荷转移络合物,采用可见分光光度法测定。结果:荷移反应生成的荷移络合物在530nm处有最大吸收,表观摩尔吸光系数是5.92×103L.mol-1.cm-1,药物浓度在0~120mg/L范围内服从比耳定律,平均回收率在98.0%以上,RSD为1.0%(n=6)。结论:方法稳定、准确、灵敏、快速,对样品的测定结果令人满意。     

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.     

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.     

阿奇霉素胶囊溶出度测定方法的改进

目的:以茜素红荷移分光光度法改进阿奇霉素胶囊溶出度的测定方法.方法:依<中国药典>二部附录X C溶出度测定方法项下二法,以600 mL pH 5.0的磷酸盐缓冲液为溶剂,转速为100 r·min-1.经45 min取样,以茜素红荷移分光光度法在524 nm处测定阿奇霉素胶囊的溶出度,限度为75%.结果:阿奇霉素在12.5～62.0 mg·L-1范围内线性关系良好(r=0.991 3),平均回收率为100.3%.结论:该方法准确、简便,可用于阿奇霉素胶囊溶出度的测定.     

高效液相色谱法测定阿奇霉素的含量

目的:用高效液相色谱法测定阿奇霉素的含量.方法:以日本岛津CLC-CN柱为固定相,0.1 mol·L-1磷酸二氢钠-甲醇-乙腈(85∶7∶8)为流动相,在pH 3.0～3.5,流速:1 mL·min-1,柱温:40 ℃,紫外检测波长210 nm,灵敏度为0.08 AUFS的条件下分离测定阿奇霉素,并对方法进行了认证.结果:阿奇霉素与其杂质能完全分离,在100～1 000 mg·L-1范围内,浓度与峰面积线性关系良好,r=0.999 6(n=3).阿奇霉素的平均回收率为100.3%(n=9),日内RSD在0.35%～3.90%之间(n=9),日间RSD在0.35%～4.40%(n=9),重复进样精度RSD%在2%以下(n=5).在pH 3～9之间的溶液中及3%双氧水中,阿奇霉素在12 h内含量基本保持不变.结论:本法简便、迅速、灵敏度高及重现性好,可用于测定阿奇霉素的含量.     

浊度法测定阿奇霉素的效价

目的建立浊度法测定阿奇霉素效价的方法。方法金黄色葡萄球菌为实验菌,加菌量1.5%~2.0%(V/V),培养温度35℃~37℃,培养时间4~6h测定。结果阿奇霉素线性浓度1.42u·mL-1~5.67u·mL-1,(R=0.99)。二剂量法的平均回收率103.4%(n=6),RSD为1.7%。结论本方法灵敏,快速、可作为测定阿奇霉素效价的方法。     

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.     

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.     

Biochemical and molecular characterisation of cubozoan protein toxins

Class Cubozoa includes several species of box jellyfish that are harmful to humans. The venoms of box jellyfish are stored and discharged by nematocysts and contain a variety of bioactive proteins that are cytolytic, cytotoxic, inflammatory or lethal. Although cubozoan venoms generally share similar biological activities, the diverse range and severity of effects caused by different species indicate that their venoms vary in protein composition, activity and potency. To date, few individual venom proteins have been thoroughly characterised, however, accumulating evidence suggests that cubozoan jellyfish produce at least one group of homologous bioactive proteins that are labile, basic, haemolytic and similar in molecular mass (42-46 kDa). The novel box jellyfish toxins are also potentially lethal and the cause of cutaneous pain, inflammation and necrosis, similar to that observed in envenomed humans. Secondary structure analysis and remote protein homology predictions suggest that the box jellyfish toxins may act as α-pore-forming toxins. However, more research is required to elucidate their structures and investigate their mechanism(s) of action. The biological, biochemical and molecular characteristics of cubozoan venoms and their bioactive protein components are reviewed, with particular focus on cubozoan cytolysins and the newly emerging family of box jellyfish toxins.     

Dose tolerability of chronically inhaled voriconazole solution in rodents

Invasive pulmonary aspergillosis (IPA) is a fungal disease of the lung associated with high mortality rates in immunosuppressed patients despite treatment. Targeted drug delivery of aqueous voriconazole solutions has been shown in previous studies to produce high tissue and plasma drug concentrations as well as improved survival in a murine model of IPA. In the present study, rats were exposed to 20 min nebulizations of normal saline (control group) or aerosolized aqueous solutions of voriconazole at 15.625 mg (low dose group) or 31.25 mg (high dose group). Peak voriconazole concentrations in rat lung tissue and plasma after 3 days of twice daily dosing in the high dose group were 0.85 ± 0.63 μg/g wet lung weight and 0.58 ± 0.30 μg/mL, with low dose group lung and plasma concentrations of 0.38 ± 0.01 μg/g wet lung weight and 0.09 ± 0.06 μg/mL, respectively. Trough plasma concentrations were low but demonstrated some drug accumulation over 21 days of inhaled voriconazole administered twice daily. Following multiple inhaled doses, statistically significant but clinically irrelevant abnormalities in laboratory values were observed. Histopathology also revealed an increase in the number of alveolar macrophages but without inflammation or ulceration of the airway, interstitial changes, or edema. Inhaled voriconazole was well tolerated in a rat model of drug inhalation.