阿那曲唑片的人体生物利用度测定(英文)

目的 :评价国产和进口阿那曲唑片的生物等效性。方法 :2 0名受试者随机分成 2组 ,交叉口服试验品与对照品各 1片 (1mg× 1片 ) ,用气相色谱法测定血药浓度。方法线性范围为 0 .5～ 2 0 0 .0μg·L- 1血浆 (r =0 .9997,n =90 ) ,低、中、高浓度(1.0 ,10 .0 ,2 0 .0 μg·L- 1血浆 )方法回收率分别为93.50 % ,10 0 .17% ,98.96 %。天内与天间精密度均小于 13%。结果 :试验片与对照片相比 ,其Tmax分别为 1.2h± 0 .5h和 1.3h± 0 .4h ,Cmax分别为10 μg·L- 1± 3μg·L- 1和 10 .2 μg·L- 1± 2 .5μg·L- 1,AUC0 T 分别为 386 μg·L- 1± 117μg·L- 1和385μg·L- 1± 117μg·h- 1·L- 1,T1/ 2 分别为 36h±14h和 32h± 10h。试验片平均相对生物利用度(10 0± 9) % (n =2 0 ,以AUC0 T计算 )。结论 :试验片与对照片两者生物等效。     

复方甲硝唑乳膏的制备及质量控制

目的:制备复方甲硝唑乳膏并建立其质量控制方法。方法:以甘油、硬脂酸等为基质制备乳膏;采用高效液相色谱法测定其中主药含量。结果:制备的乳膏性状、鉴别、检查等均符合2005年版《中国药典》相关规定;甲硝唑、氯霉素检测浓度线性范围分别为10·16～101·60(r=0·9995,n=6)、10·02～100·20mg·L-1(r=0·9999,n=6);平均回收率分别为96·82%(RSD=0·94%,n=6)、98·11%(RSD=0·85%,n=6)。结论:本制剂组方合理,制备工艺简便可行,质量稳定可控。     

高效液相色谱法测定氯氟液中氯霉素和地塞米松磷酸钠的含量

目的建立高效液相色谱法同时测定氯氟液中氯霉素和地塞米松磷酸钠含量。方法色谱柱为Inertsil C8-3,流动相为甲醇-乙腈-水(72∶3∶25),流速为1.0mL·min-1,柱温为40℃,检测波长为240nm。结果氯霉素和地塞米松磷酸钠检测质量浓度分别为62.1～745.2mg·L-1(r=0.9999)和6.22～74.64mg·L-1(r=0.9999),平均加样回收率分别为101.02%(RSD为2.0%)和100.05%(RSD为1.6%)。结论方法简便易行、准确可靠,可用于该制剂的含量测定。     

柱前衍生化HPLC法测定硫酸庆大霉素和硫酸新霉素的含量

目的 :建立一种测定硫酸庆大霉素滴眼液中庆大霉素和复方地塞米松滴眼液中硫酸新霉素含量的HPLC法。方法 :硫酸庆大霉素和硫酸新霉素经氯甲酸芴甲酯 (FMOC Cl)衍生化后用HPLC法分析。采用AgilentC18柱 (15 0mm× 4 6mm ,5 μm)为色谱柱 ,乙腈 -水 (95∶5 ,V/V)为流动相 ,紫外检测波长 2 6 5nm ,流速 1mL·min-1,柱温 2 5℃。结果 :硫酸庆大霉素在 2～ 10 0mg·L-1浓度范围内有良好的线性关系 (r=0 9997,n =6 ) ,回收率为 (98 5± 0 6 5 ) % ,RSD =0 6 6 % ,(n =9) ,最低检测质量浓度为 1mg·L-1;硫酸新霉素在 1～ 10 0mg·L-1浓度范围内有良好的线性关系 (r =0 9993,n =7) ,回收率为 (99 2 6± 1 70 ) % ,RSD =1 71% ,(n =9) ,最低检测质量浓度为 0 5mg·L-1。结论 :本方法可以用于硫酸庆大霉素滴眼液和复方地塞米松滴眼液的质量控制     

高效液相色谱法测定氯麻滴鼻液中氯霉素和盐酸麻黄碱的含量

目的 :建立测定氯麻滴鼻液中氯霉素和盐酸麻黄碱含量的高效液相色谱法。方法 :采用反相 μ Bondpak色谱柱 ,甲醇- 0 .0 2mol·L-1磷酸二氢钾 (5 5∶45 ,磷酸调 pH值3.5 )为流动相 ,检测波长 2 5 4nm。结果 :氯霉素和盐酸麻黄碱的线性范围分别为 2 0～ 12 0 μg·ml-1(r =0 .9998) ,80～ 480 μg·ml-1(r =0 .9998) ;加样回收率分别为 10 1.4% ,RSD =0 .5 %及 10 0 .8% ,RSD =0 .9% (n =5 ) ,日内RSD分别为 0 .9%和 0 .4% (n =5 ) ,日间RSD分别为 1.0 %和 0 .8% (n =4)。结论 :HPLC法可用于本制剂的含量测定和质量控制 ,方法简便、灵敏、结果准确     

紫外分光光度法测定苯妥英钠血药浓度

目的 :建立一种简单、准确的紫外分光光度法 ,用于苯妥英钠血药浓度监测。方法 :采用紫外分光光度法测定苯妥英钠血药浓度 ,检测波长 2 5 0nm ,以环己烷为提取剂。结果 :苯妥英钠 10 ,4 0 ,80mg·L-13个浓度的平均回收率为 93 5 0 %。日内RSD <8% (n =4 ) ,日间RSD <10 % (n =5 )。分析方法的最低定量限为 1 1mg·L-1。线性范围为 5～ 80mg·L-1,线性回归方程为A =1 5 81× 10 -3 c+7 917× 10 -4,r=0 9992 (n =5 )。该方法监测口服苯妥英钠患者 6例 ,血药浓度为 8 4 8～ 37 4 5mg·L-1。结论 :该方法简单、快速 ,适用于基层单位临床血药浓度监测     

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。     

高效液相色谱法测定人血浆中麦考酚酸的血药浓度

目的 :建立测定麦考酚酸 (MPA)血药浓度的方法并对肾移植病人给药后的血药浓度进行测定。方法 :采用高效液相色谱 (HPLC)法测定血药浓度 ,检测波长 30 3nm。乙腈 (含有 0 .1mol·L- 1磷酸 )作为血样的蛋白沉淀剂。色谱柱 :AgilentXDBC18(15 0mm× 4 .6mm ,5 μm) ;流动相 :乙酸钠缓冲液 (pH =3.0 ,30mmol·L- 1)∶乙腈 =5 7∶4 3(V/V) ;流速 :1mL·min- 1。结果 :MPA血药浓度线性范围为 0 .6～ 30mg·L- 1(r =0 .9995 ,n =6 ) ,其血浆最低检测浓度为 0 .2mg·L- 1;低、中、高 3种浓度MPA的方法回收率为 (98.9± 1.5 ) % ,提取回收率为 (10 6 .73± 0 .2 7) % ;相应 3种浓度MPA的精密度RSD均小于 5 %。结论 :HPLC法能快速、准确对MPA进行血药浓度测定 ,可以用于MPA的临床血药浓度监测和药动学研究。     

口服抗肿瘤药赛特铂在大鼠的药动学

目的 :观察口服抗肿瘤药赛特铂(satraplatin)在大鼠的药动学。方法 :石墨炉原子吸收分光法测定体内赛特铂的总铂浓度。结果 :剂量为 5 0mg·kg- 1和 10 0mg·kg- 1时 ,主要药动学参数分别为 :T12 β(4 3±s 34)h和 (5 8± 38)h ,Tmax(5 .0± 2 .0 )h和 (6 .0± 1.0 )h ,Cmax(12 .6± 2 .5 )mg·L- 1和 (13.4± 1.5 )mg·L- 1,AUC0 ∞(4 2 2± 12 0 )mg·h·L- 1和 (70 2± 118)mg·h·L- 1。组织分布以肝、肾最高。 4 8h后药物排出已基本完成 ,主要经粪便排出 ,约 5 5 % ,尿排出小于 6 % ,2 4h胆中排出0 .2 3%。结论 :赛特铂的药时曲线为口服一级吸收2室模型。     

HPLC法测定维丁乳膏中2主药的含量

目的:建立以高效液相色谱法测定维丁乳膏中2主药含量的方法。方法:色谱柱为YWG-C18,柱温为30℃,进样量为20μL,2组分丁酸氢化可的松和维生素E(VitE)的流动相分别为水-乙腈-冰醋酸(55:45:0·5)、甲醇-乙醚(90:10),检测波长分别为240、285nm。结果:丁酸氢化可的松和VitE检测浓度的线性范围分别为15～65(r=0·9999)、200～950mg·L-1(r=0·9996);平均回收率分别为97·9%(RSD=0·7%,n=6)、97·3%(RSD=1·7%,n=6)。结论:本方法准确、可靠、重现性好,可用于该制剂的质量控制。     

Nachweis einiger Heilmittel in der Kniegelenksynovialflüssigkeit

Zusammenfassung Mittels Gaschromatographie und Dünschichtchromatographie wiesen die Autoren 11 Substanzen nach, welche durch Injektion oder nach Verabreichung per os in die Kniegelenksynovialflüssigkeit eindrangen. In ihrer Aufstellung konnten sie eine direkte Beziehung zwischen Struktur sowie chemischphysikalischen Eigenschaften der Substanz und ihrer Fähigkeit, aus dem Blut in die Kniegelenksynovialflüssigkeit einzudringen, nicht nachweisen, außer der Tatsache, daß Substanzen mit starker Affinität zu Eiweißstoffen erst in höheren Dosen nachweisbar waren.     

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.     

Emerging drugs for epilepsy

Epilepsy affects ≤ 1% of the world's population. Antiepileptic drugs (AEDs) are the mainstay of treatment, although more than a third of patients are not rendered seizure free with existing medications. Uncontrolled epilepsy is associated with increased mortality and physical injuries, and a range of psychosocial morbidities, posing a substantial economic burden on individuals and society. Limitations of the present AEDs include suboptimal efficacy and their association with a host of adverse reactions. Continued efforts are being made in drug development to overcome these shortcomings employing a range of strategies, including modification of the structure of existing drugs, targeting novel molecular substrates and non-mechanism-based drug screening of compounds in traditional and newer animal models. This article reviews the need for new treatments and discusses some of the emerging compounds that have entered clinical development. The ultimate goal is to develop novel agents that can prevent the occurrence of seizures and the progression of epilepsy in at risk individuals.     

盐酸达泊西汀中甲磺酸甲酯、甲磺酸乙酯及甲磺酸异丙酯的顶空毛细管GC-ECD法测定

建立了衍生化顶空毛细管气相色谱-电子捕获检测器(ECD)法测定盐酸达泊西汀中的甲磺酸甲酯(MMS)、甲磺酸乙酯(EMS)和甲磺酸异丙酯(IMS).应用碘化钠衍生技术,使用PW-5毛细管柱,载气为氮气,ECD检测,程序升温.MMS、EMS和IMS分别在0.03～0.30、0.05～0.50和0.05～0.50 μg/ml浓度范围内线性关系良好,平均回收率分别为63.5％、100.3％和96.2％,最低检测限分别为0.30、0.50和0.50 ng/ml.     

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.