复方乳酸左氧氟沙星滴眼液的制备与含量测定

目的：研究复方乳酸左氧氟沙星滴眼液的制备及含量测定方法。方法：用紫外分光光度法和化学分析法对乳酸左氧氟沙星和地塞米松磷酸钠进行定性鉴别，用反相高效液相色谱法(RP HPLC)进行含量测定。以ODS C18分析柱(4.6 mm×250 mm，5 μm)为固定相，0.2%三乙胺水溶液(用磷酸调pH至2.7) 乙腈(68∶32)为流动相，检测波长240 nm，流速1.0 mL·min 1。结果：乳酸左氧氟沙星的线性范围12～60 μg·mL 1，r＝0.999 9，平均回收率99.66%，RSD＝1.9%(n＝5)。地塞米松磷酸钠的线性范围3～15 μg·mL 1，r＝0.999 1，平均回收率100.8%，RSD＝1.8%(n＝5)。结论：该制剂处方设计合理，制备方法可行，灵敏度高，测定结果准确，精密度良好。     

复方乳酸左氧氟沙星缓释滴鼻液的制备及稳定性研究

目的研究复方乳酸左氧氟沙星缓释滴鼻液的制备、质量控制方法及稳定性。方法以壳聚糖为缓释剂，拟订处方组成及制备工艺；用紫外分光光度法在293nm波长处测定乳酸左氧氟沙星的含量，用旋光法测定盐酸麻黄碱的含量；用初均速法考察制剂的稳定性。结果乳酸左氧氟沙星检测质量浓度在2～12μg／mL范围内与吸收度线性关系良好（r=0．9999，n=6），平均回收率为99．72％，RSD=0．42％（n=9）。结论该制剂组方合理，制备工艺简单，质量控制方法可靠，稳定性较好，室温贮存有效期为2．1年。     

复方乳酸左氧氟沙星烧伤凝胶的制备及质量控制

目的:制备复方乳酸左氧氟沙星烧伤凝胶,并建立其质量控制方法.方法:以乳酸左氧氟沙星、盐酸达克罗宁和硫酸锌为主药,以壳聚糖等为辅料制备凝胶;采用双波长紫外分光光度法测定乳酸左氧氟沙星和盐酸达克罗宁的含量,配位滴定法测定硫酸锌的含量.结果:制备的凝胶均匀细腻,分散性好;乳酸左氧氟沙星检测质量浓度在2～8 mg·L1范围内线性关系良好(r=0.999 9,n=6),平均回收率为99.79%,RSD为0.33%(n=9);盐酸达克罗宁检测质量浓度在4～16mg·L-1范围内线性关系良好(r=0.999 8,n=6),平均回收率为99.43%,RSD为0.81%(n=9).结论:本制剂组方合理,制备工艺简便可行,质量稳定可控.     

左氧氟沙星凝胶的制备及质量控制

目的 建立制备左氧氟沙星凝胶剂及质量控制的方法。方法 用聚乙烯醇124作凝胶基质，制备左氧氟沙星凝胶；采用紫外分光光度法进行含量测定，测定波长为293nm；一元线性回归分析．线性范围为2.0～12．0mg／L，r=0．9999．结果 含量测定平均回收率为99．8％．RSD=0．15％(n=5)。结论 制备该凝胶工艺简单，质量稳定，测定方法可靠，应用无刺激，可供临床应用。     

复方乳酸左氧氟沙星壳聚糖凝胶剂的制备与质量控制

目的:制备复方乳酸左氧氟沙星壳聚糖凝胶剂,建立其质量控制方法.方法:以壳聚糖、羧甲基纤维素为凝胶材料制备复方乳酸左氧氟沙星壳聚糖凝胶剂;采用紫外分光度法测量乳酸左氧氟沙星含量,采用容量法测定谷氨酸锌含量.结果:乳酸左氧氟沙星的线性范围为4.5～20.5 μg·ml-1,平均回收率为100.2%,RSD为0.18%(n=9).结论:该凝胶剂制备工艺简单,质量控制方法可靠,质量稳定.     

复方左氧氟沙星锌乳膏的制备及质量控制

目的:研制复方左氧氟沙星锌乳膏并建立其质量控制方法。方法:取左氧氟沙星和硫酸锌制成左氧氟沙星锌,加入基质制备乳膏;采用紫外分光光度法于293nm波长处测定左氧氟沙星含量。结果:制备的乳膏均匀细腻,易于涂布;左氧氟沙星检测浓度在2～10μg/ml范围内线性关系良好(r=0.9999,n=5),平均回收率为99.8%,RSD=0.44%(n=5)。结论:本制剂组方合理,制备工艺简便可行,质量稳定可控。     

复方左氧氟沙星滴耳剂的制备及质量控制

目的制备复方左氧氟沙星滴耳剂,并对其进行质量控制。方法运用紫外分光光度法测定含量(双波长分光光度法测定左氧氟沙星、替硝唑的含量)。结果左氧氟沙星的线性范围为1～5ug/ml,回归方程,y=1×10-3 0.0524C(r=0.9997,n=5)回收率为98.63%～102.03%;替硝唑的线性范围2～10ug/ml,回归方程y=-3.4×10-3 0.0276C(r=0.9998,n=5),回收率为99.06%～101.20%。结论复方左氧氟沙星滴耳剂的制备简单,本方法准确可靠。     

复方左氧氟沙星混悬剂的制备和方法学研究

目的 制备复方左氧氟沙星混悬荆,并对其进行质量控制.方法 运用紫外分光光度法测定含量(双波长分光光度法测定盐酸左氧氟沙星、盐酸达克罗宁的含量).结果 盐酸左氧氟沙星的线性范围为2～10μg/ml,回归方程,y=-1.8 × 10-3 0.0580C(r=0.9997,n=5),回收率为98.47%～103.72%;盐酸达克罗宁的线性范围5～25μ g/ml,回归方程Y=9.3 × 10-3 0.044 7C (r=0.9999,n=5),回收率为102.12%～104.21%.结论 复方左氧氟沙星混悬剂的制备简单,本方法准确可靠.     

复方左氧滴眼液的制备及疗效观察

目的：制备复方左氧滴眼液，用于治疗眼部细菌感染。方法：用高效液相色谱法对滴眼液中乳酸左旋氧氟沙星及地塞米松磷酸钠进行含量测定，并考察其稳定性、刺激性和临床疗效。结果：复方左氧滴眼液的疗效明显好于对照组，且乳酸左氧氟沙星及地塞米松磷酸钠的平均回收率分别为98．83％，100．31％，RSD分别为0．56％，0．73％（n=6）。结论：复方左氧滴眼液制备工艺及质量控制方法可行，临床疗效满意。     

一阶导数光谱法测定氧氟沙星滴耳液含量

目的测定复方氧氟沙星栓剂中氧氟沙星和甲硝唑的含量。方法采用一阶导数光谱法,选择273.5nm为氧氟沙星的测定波长,260.5nm为甲硝唑的测定波长,结果一阶导数光谱法测定复方氧氟沙星栓剂中氧氟沙星和甲硝唑的含量,线性关系良好,同时可排除栓剂中基质的干扰,测得氧氟沙星平均回收率为99.952%,RSD=1.283%,r=0.9995(n=5),甲硝唑平均回收率为100.002%,RSD=0.941%,r=0.9999(n=5)。结论一阶导数光谱法简便、快速、准确。     

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.