Development of a new choroidal metastasis in resistance to crizotinib therapy in anaplastic lymphoma kinaserearranged non-small cell lung cancer

INTRODUCTION Non-small cell lung cancer（NSCLC）is a common malignant disease with an extremely poor prognosis.Lung cancer has been reported to metastasize to the eye in 0.2%to7%of patients based on clinical studies,and in 6%to 7%of patients based on postmortem histopathologic studies.

Pre-Formulation Development of Lamivudine 300 mg and Tenofovir Disoproxil Fumarate (TDF) 300 mg Fixed Dose Combination Tablets

Introduction: In this study, physical and chemical characteristics of Lamivudine, Tenofovir Disoproxil Fumarate (TDF) and potential excipients were systematically followed and documented [1]. Objective: The objective of this scientific work was to carry out pre-formulation studies including compatibility studies on Lamivudine and Tenofovir Disoproxil Fumarate with their potential excipients prior a direct compression process [2]. Methodology: The interaction was studied in three set of environments namely uncontrolled room conditions for Zone VI b (30°C ± 2°C), oven conditions in which the oven was set at 50°C and accelerated climatic conditions in which a climatic chamber was set at 40°C ± 2°C/75% ± 5% Relative Humidity (RH %). Sample preparation was done by mixing the amount of formulation excipients to active substances at a ratio of 1:10, whereas active substance to another active substance at a ratio of 1:1, active substance to coating materials at 1:4, coating materials to the whole set of excipients 1:4. The whole set of samples was geometrically mixed and triturated by mortar and pestle to very fine uniform powder to ensure homogeneity of the mixture. HPLC analytical method was used for simultaneous quantitative determination of lamivudine and tenofovir disoproxil fumarate. Transmittance of the mixture was determined by Near Infra-Red (NIR) technique. Results: The amount of Lamivudine as on day 0 was comparable to day 90 for in all tested conditions (Room, Oven and Climatic Chamber), whereas for Tenofovir Disoproxil Fumarate only the amount of the drug at Room (30°C ± 2°C) was comparable to results on day 90. A significant drop of amount of Tenofovir Disoproxil Fumarate (TDF) exposed to moisture (Climatic chamber at 40°C ± 2°C/75% ± 5% Relative Humidity (RH %)) and temperature of 50°C was observed. Colour change was observed for samples subjected to moisture (Climatic chamber at 40°C ± 2°C/75% ± 5% Relative Humidity (RH %)) and as well picked up in the NIR region 400 to 1500 cm-1 (Finger print region) by a significant shift in Transmittance. Conclusion: It can be concluded that microcrystalline cellulose, cross linked sodium carboxymethyl cellulose, magnesium stearate and sodium carbxymethyl cellulose can be compressed together with Lamivudine and Tenofovir Disoproxil Fumarate (TDF) to produce a pharmaceutically acceptable solid dosage form, tablet. The produced tablets should be packed in moisture and light protective containers as Tenofovir Disoproxil Fumarate (TDF) has diester linkages which can be hydrolysed into the active drug Tenofovir in the presence of moisture.

Assessment of Moisture Permeability and Closure Systems of High Density Polyethylene Plastic Bottles Used as Primary Packaging Containers for Moisture Sensitive Medicines

Introduction: Moisture permeability and a loose closure system might allow a significant gain of moisture into container and this could lead to significant loss of potency of drug sensitive to moisture and as well promoting the growth of microorganisms. Typical examples of the drugs sensitive to moisture include Tenofovir Disoproxil Fumarate (TDF). Product claimed to be a “Tight container” does not make it a tight container until proved practically. A plastic container is tight if “not more than one of the 10 tested containers exceeds 100 mg per day per L in moisture permeability. Objectives: The goal of this study was to determine rate of moisture permeability of selected High Density Polyethylene plastic bottles for packaging of moisture sensitive medicines in particular Lamivudine/Tenofovir Disoproxil fumarate tablets. Methodology: The determination of rate of moisture permeability was achieved by assessing closure systems of plastics as per USP 37 method, while the difference in absorption pattern was achieved by assessing the spectrum obtained through transmittance by Fourier Transform-Infrared (FT-IR). The plastic bottles were randomly selected from supplier A, B and C. Results: The plastic bottles from supplier A and B had an average moisture permeability of 12.57 and 51.55 mg/day/L with none of the containers exceeding moisture permeability of 100 mg/day/L whereas containers from supplier C had an average of 149.95 mg/day/L with seven of the containers exceeding of 100 mg/day/L. Conclusion: Containers from supplier A and B met the USP specifications hence could be used as primary packaging for moisture sensitive medicines whereas the containers from supplier C did not meet the USP specifications for them to be regarded as “Tight Containers” and hence, unsuitable for packaging of moisture sensitive medicines.

中医译家翻译思想研究的概况与思考

不限时间检索国内有关中医译家翻译思想研究的文献,发现在中医翻译领域,译家翻译思想研究发文量极低,仅有15篇;发文期刊选择面很小,仅7种期刊刊载过此类论文;研究对象主要集中于魏迺杰、文树德、李照国和谢竹藩等译者;论文类型主要有译家点评、专著介评、译文评析以及史学研究等4种方法。表明国内中医译家翻译思想研究尚处于萌芽、探索阶段,鲜有研究者关注。中医译家翻译思想研究是中医翻译研究的重要组成部分,对中医翻译的理论建设有重要启示意义。今后的相关研究应引入理论指导、深化现有研究、拓宽研究对象、优化研究方法,进一步提高研究数量和质量。

毛细管气相色谱法测定JS1-1-01原料药中溶剂残留量

目的建立直接进样毛细管气相色谱法测定JS1-1-01原料药中7种有机溶剂残留量。方法采用DB-5色谱柱(30 mm×0.32 mm,1.0μm),氮气作为载气,氢火焰离子化检测器,采用N,N-二甲基甲酰胺作为溶剂,外标法分析,检测JS1-1-01原料药中残留溶剂。结果甲醇、乙醇、丙酮、二氯甲烷、甲基环己烷、吡啶和甲基吡咯烷酮线性关系良好(r=0.999 5~0.999 8),平均回收率为86.8%~100.7%,定量限分别为3.02、5.00、5.01、12.05、4.79、2.03和、4.26 mg·L-1。结论建立的方法简单、快速、分离效果好,适用于JS1-1-01中7种残留溶剂的同时检测。

大叶井口边草乙酸乙酯部位化学成分研究

目的:研究大叶井口边草乙酸乙酯部位的化学成分。方法:采用硅胶柱色谱、Sephadex LH-20柱色谱、RP-C18柱色谱和半制备高效液相色谱法对大叶井口边草乙酸乙酯部位的化学成分进行分离纯化,通过理化性质、1H-NMR、13C-NMR和MS等方法鉴定化合物结构。结果:从大叶井口边草乙酸乙酯部位中分离纯化了17个化合物,分别鉴定为:ent-3β-hydroxy-kaur-16-ene(1)、ent-2β,15α-dihydroxy-kaur-16-ene(2)、ent-3β,19-dihydroxy-kaur-16-ene(3)、ent-2β,6β,15α-trihydroxy-kaur-16-ene(4)、蕨素B(5)、芹菜素(6)、木犀草素(7)、槲皮素(8)、6-甲氧基槲皮素(9)、6-甲氧基柚皮素(10)、槲皮素-3-O-β-D-吡喃葡萄糖苷(11)、木犀草苷(12)、芹菜素-7-O-β-D-葡萄糖苷(13)、芹菜素-7-O-β-D-葡萄糖醛酸苷甲酯(14)、咖啡酸(15)、咖啡酸甲酯(16)、β-谷甾醇(17)。结论:其中,化合物1、3、7~16为首次从该植物中分离得到。

Evaluation of antiplasmodial properties in 15 selected traditional medicinal plants from India

Objective:The objective of this study was to evaluate the in vitro antiplasmodial properties against malaria parasite in 15 plants mentioned in Indian traditional medicine texts.Methods:In vitro antiplasmodial activity of methanolic extracts obtained from Indian traditional medicinal plants was evaluated on Plasmodium falciparum of FCK2 and INDO strains using schizont maturation inhibition assay and parasite lactate dehydrogenase inhibition assay.Results:Methanolic extracts of Adhatoda zeylanica,Embelia ribes,Piper nigrum and Plumbago zeylanica exhibited more than 50%inhibition in both the stains in schizont maturation inhibition assay.Methanolic extracts of seven medicinal plants exhibited antiplasmodial activity at half maximal inhibitory concentration(IC50)<100 mg/m L,and methanolic extracts of five medicinal plants exhibited antiplasmodial activity at IC50<50 mg/m L in P.falciparum lactate dehydrogenase(PfLDH)inhibition assay.A.zeylanica,E.ribes and P.nigrum exhibited promising antiplasmodial activity in PfLDH inhibition assay.A.zeylanica and E.ribes exhibited improved activity against resistant in comparison to sensitive strain.Conclusion:A.zeylanica and E.ribes were the most promising extracts from this study and deserve further investigation of their antiplasmodial properties.

热熔挤出技术制备利伐沙班固体分散体

目的:利用热熔挤出技术制备利伐沙班固体分散体,提高其体外溶出度。方法:通过单因素试验,以体外溶出为指标分别对辅料种类、药物与辅料的比例、挤出温度、挤出机螺杆转速进行筛选,并通过差示扫描量热法(DSC)、X射线衍射法(XRD)、傅里叶红外光谱法(FTIR)对最优固体分散体进行表征。结果:以PVP VA 64为载体、药物辅料比例为1∶8、挤出温度为180℃、螺杆转速为200 r·min^(-1)制得的固体分散体体外溶出可达97%。结论:通过热熔挤出技术制备的利伐沙班固体分散体能显著提高利伐沙班的体外溶出度。