高效液相色谱法同时测定氯霉素地塞米松滴眼液两组分的含量

目的 :采用HPLC法测定氯霉素地塞米松滴眼液中氯霉素和地塞米松磷酸钠的含量。方法 :采用C18色谱柱 ,流动相为甲醇 0 .0 2 5mol·L- 1的磷酸二氢钠溶液 (4 8∶52V/V) ,检测波长为 2 40nm。结果 :氯霉素的线性范围为 75～ 1 75μg·ml- 1,r=0 .9994,回收率 99.6 6 %。RSD =1 .0 3%;地塞米松磷酸钠的线性范围为 1 5～ 35μg·ml- 1;r =0 .9992 ,回收率 1 0 4.2 4%。结论 :该方法简便、准确 ,可同时测定滴眼液中氯霉素和地塞米松磷酸钠的含量。     

高效液相色谱法同时测定水氯地搽剂中水杨酸、氯霉素和地塞米松磷酸钠含量

目的建立水氯地搽剂中水杨酸、氯霉素和地塞米松磷酸钠含量的方法。方法采用HPLC法,色谱柱为Zorbax ODS-C18column（150 mm×4.6 mm,5μm）;以甲醇-乙腈-0.05 mol.L^-1磷酸二氢钠溶液（用磷酸调pH至2.5）（50∶4∶46）;流速：1 mL.min^-1;测定波长242 nm;柱温：30℃,进样量：20μL。结果水杨酸、氯霉素和地塞米松磷酸钠的线性范围分别为32.24-257.92 mg.L^-1（r=0.999 5）、19.52-156.16 mg.L^-1（r=0.999 8）、2.00-16.00 mg.L-1（r=0.999 4）,平均回收率分别为99.84%、100.14%和100.09%,RSD分别为0.92%、1.03%和1.56%（n=9）。结论本方法快速、准确,可用于水氯地搽剂的质量控制。     

薄层扫描法测定注射用硫酸庆大霉素中3组分的含量

目的 :建立注射用硫酸庆大霉素中3组分含量的快速测定方法。方法 :采用薄层扫描法 ,以甲醇 -氯仿 -28 %氨水 (1∶1∶1)为展开剂 ,新配制的茚三酮的乙醇 -冰醋酸溶液为显色剂 ,测定波长为500nm。结果 :注射用硫酸庆大霉素中3组分的点样量均在2μg～12μg 范围内线性关系良好 (r1=0. 9993、r2=0. 9996、r1a=0 .9991)。结论 :薄层扫描法可作为注射用硫酸庆大霉素中3组分含量的快速测定方法。     

高效液相色谱法同时测定滴鼻剂中三组分的含量

目的采用高效液相色谱(HPLC)法同时测定滴鼻剂中盐酸麻黄碱、盐酸苯海拉明、地塞米松磷酸钠的含量.方法采用C18色谱柱,流动相为甲醇-0.05 mol*L-1 KH2PO4-三乙胺(58∶42∶0.2),检测波长为221 nm.结果盐酸麻黄碱在1600～2400 mg*L-1浓度范围内线性关系良好(r=0.9994),回收率为99.8%,RSD为1.0%.盐酸苯海拉明80～120 mg*L-1浓度范围内线性关系良好(r=0.9996),回收率为101.0%,RSD为0.9%.地塞米松磷酸钠160～240 mg*L-1浓度范围内线性关系良好(r=0.9991),回收率为99.6%,RSD为0.8%.结论该方法可同时测定滴鼻剂中盐酸麻黄碱、盐酸苯海拉明、地塞米松磷酸钠.     

HPLC法测定银杏达莫氯化钠注射液的含量

目的建立HPLC法测定银杏达莫氯化钠注射液中银杏总黄酮和双嘧达莫含量的方法。方法色谱柱:Diamonsil C18柱(4.6 mm×200.0 mm,5μm),流动相:甲醇-乙腈-30 mmol.L-1磷酸二氢钠溶液(体积比为20∶20∶80),检测波长:360 nm,测定3种黄酮苷元(槲皮素、山柰酚和异鼠李素);流动相:质量分数为0.1%的磷酸二氢钠溶液-甲醇(体积比为30∶70),检测波长:290 nm,测定双嘧达莫。结果槲皮素在0.01~0.09 g.L-1(r=0.999 3)、双嘧达莫在0.005~0.035 g.L-1(r=0.999 4)内呈良好的线性关系,平均回收率分别为102.5%(RSD=1.6%)、100.6%(RSD=1.1%)。结论本法可用于银杏达莫氯化钠注射液的质量控制。     

HPLC法同时测定顺气化痰片及顺气化痰颗粒中氨茶碱和马来酸氯苯那敏的含量

目的:为控制顺气化痰片及顺气化痰颗粒质量,建立高效液相色谱法同时测定顺气化痰片及其颗粒剂中氨茶碱和马来酸氯苯那敏的含量。方法:采用C18(150 mm×4.6 mm,5μm)色谱柱,流动相为甲醇-0.05 mol.L-1磷酸二氢钠(40∶60,用磷酸调节pH 3.5),流速1.0 mL.min-1,检测波长275 nm(茶碱)、264 nm(马来酸氯苯那敏)。结果:茶碱的线性范围为2.03～101.4μg.mL-1(r=0.9998);马来酸氯苯那敏的线性范围为1～50μg.mL-1(r=0.9998)。片剂中茶碱的平均回收率为99.4%,RSD=2.0%;马来酸氯苯那敏的平均回收率为99.8%,RSD=0.84%;颗粒剂中茶碱的平均回收率为101.5%,RSD=1.6%;马来酸氯苯那敏的平均回收率为99.9%,RSD=0.89%。结论:该方法简便、灵敏、准确,适用于顺气化痰片剂及颗粒剂中氨茶碱和马来酸氯苯那敏的同时测定及该品种的质量控制。     

高效液相色谱法测定抗炎涂剂中氯霉素和地塞米松磷酸钠的含量

目的:建立同时测定抗炎涂剂中氯霉素和地塞米松磷酸钠含量的方法.方法:用C18柱为固定相,甲醇-0.34%磷酸二氢钾溶液(60:40)为流动相,氢化可的松为内标物,流速1.0mL·min-1,检测波长240 nm.结果:氯霉素和地塞米松磷酸钠分别在160～640 mg·L-1(r=0.999 9),4～16 mg·L-1(r=0.999 9)范围内线性关系良好;平均回收率分别为100.0%,100.8%;精密度RSD分别为0.16%,0.15%.结论:此方法简便、快速、准确.     

HPLC法测定氨茶碱注射液的含量

目的建立测定氨茶碱注射液含量的HPLC法。方法采用C18柱(150mm×4.6mm,5μm),流动相为甲醇-0.05mol.L-1磷酸二氢钾溶液-三乙胺(25:75:0.2),流速1mL.min-1,检测波长271nm,柱温30℃。结果无水茶碱在9.675～96.75mg.L-1范围内线性关系良好(r=0.9999,n=6),测得平均回收率为99.6%,RSD为0.5%。结论该方法简便,准确,专属性强。     

HPLC法测定麻地滴鼻液中两组分含量

目的建立HPLC法测定麻地滴鼻液中盐酸麻黄碱和地塞米松磷酸钠的含量。方法采用Hypersil ODS2(4.6 mm×250mm,5μm)色谱柱,以甲醇∶0.025 mol.L-1磷酸二氢钠溶液(54∶46)为流动相,流速1.0 m l.m in-1,检测波长258 nm。结果盐酸麻黄碱和地塞米松磷酸钠的线性范围分别为102~510 mg.L-1,(r=0.999 9),2.5~12.5 mg.L-1,(r=1.0);平均加样回收率分别为100.9%(RSD=1.1%),101.1%(RSD=1.5%)。结论该方法简便、准确,适用于麻地滴鼻液的质量控制。     

高效液相色谱法测定复方地塞米松庆大霉素滴鼻液中两组分含量

目的探讨用高效液相色谱法（HPLC法）同时测定复方地塞米松庆大霉素滴鼻液中盐酸麻黄素和地塞米松磷酸钠的含量。方法采用美国Waters高效液相色谱仪，流动相为甲醇-0．1mol／L醋酸铵溶液（50：50，用磷酸调pH值至4．0），流速为1．0mL／min，检测波长为256nm。结果盐酸麻黄碱和地塞米松磷酸钠在此条件下可实现基线分离，两组分质量浓度线性范围分别为50—500μg／mL（r=0．9995）和3．5～35μg／mL（r=0．9994），平均回收率分别为99．5％（RSD=0．8％）和99．4％（RSD=1．3％）。结论HPLC法简便快速，准确可靠，可作为复方地塞米松庆大霉素滴鼻液的质量控制方法。     

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.