三氮唑核苷在5种输液中的配伍实验

三氮唑核苷在５种输液中的配伍实验唐德珍，白梅（桂林市中医院５４１００ｚ）吕高荣（桂林三金制药集团）三氮唑核苷是一种较为新型的抗病毒药，对多种病毒有抑制作用。在临床使用中常将三氮唑核苷注射液加入各种输液中静脉滴注。我院曾发现该药与５％、１０％葡萄糖注射...     

旋光法测定三氮唑核苷注射液的含量

本文根据三氮唑核苷具有旋光性质、直接测定三氮唑核苷注射液的含量，适合药厂对产品中间体的质量控制和快速分析。     

三氮唑核苷注射液与输液的配伍稳定性考察

三氮唑核苷注射液与输液的配伍稳定性考察吴奥苓鞍山钢铁公司药品检验所１１４００３三氮唑核苷注射液被广泛用于治疗各种病毒感染，临床上常将它加入输液中进行静滴。关于三氮唑核苷注射液与输液的配伍稳定性研究尚未见报道。由于比色法［１］所用的显色剂３，５－二羟基...     

肌注三氮唑核苷致过敏反应3例

三氮唑核苷引起过敏反应，文献报道不多。现将我们在临床实际工作中肌注三氮唑核苷致过敏反应3例报道如下：     

利巴韦林与6种药物的配伍变化考察

目的：考察２０ ℃下６ ｈ 内,注射用三氮唑核苷与６ 种药物的配伍稳定性。方法：采用分光光度法测定配伍后６ ｈ 内三氮唑核苷的含量,同时观察外观并测定ｐ Ｈ 值。结果：２０ ℃下６ ｈ 内配伍液外观澄明无变色,未见气泡或沉淀,ｐ Ｈ 值及三氮唑核苷等含量均无明显变化。结论：２０ ℃下６ ｈ 内注射用三氮唑核苷与６ 种药物在５ ％ 葡萄糖氯化钠注射液中配伍可以使用。     

鲎试剂用于三氮唑核苷注射液细菌内毒素检测的探讨

目的建立三氮唑核苷注射液的细菌内毒素检测法。方法考察三氮唑核苷注射液对细菌内毒素检查法的干扰作用,根据中国药典1995年版二部收载的细菌内毒素检查法的要求进行实验。结果将三氮唑核苷注射液经20倍稀释后可排除干扰,用标示灵敏度0.5EU·ml     

旋光法测定三氮唑核苷注射液含量

本文报告了三氮唑核苷(病毒唑)注射液的旋光测定法。用本法测定三氮唑核苷注射液与分光光度法结果一致。本法简便,快速。     

三氮唑核苷对流行性出血热患者红细胞系统影响的研究

三氮唑核苷(ribavirin)又名病毒唑,是一种广谱抗病毒的核苷化合物,能抑制多种DNA和RNA病毒,并能治疗多种病毒性疾病。近年来,我们用病毒唑治疗流行性出血热(EHF)患者取得了有效的结果,并进行了三氮唑核苷和安慰剂组患者红细胞系统的检测,以探讨三氮唑核苷对EHF患者红细胞系统的影响。 1,病例选择:病例选自1985年12月至1986年3月,1986年10月至1987年3月EHF流行季节收治住院的244例患者,经EHF     

氮杂核苷类似物的研究进展

对于核苷类化合物糖环部分的化学改造一直是发现新的具有抗病毒、抗肿瘤或其他生物活性的核苷类先导化合物的重要途径之一。作为天然核苷受体的竞争性抑制剂,糖环部分化学改造的核苷类似物在过去的几十年中得到了深入的研究。本文综述了氮杂核苷类似物,即含有氮杂核糖片段的化合物的化学研究进展,为新型核苷类化合物的设计合成提供参考。     

高效液相色谱法测定三氮唑核苷注射液的含量

目的：建立高效液相色谱法检测三氮唑核苷的含量。方法：用YWG－C18色谱柱,0.05mol/L磷酸二氢钾－甲醇（75：25）,pH4.0为流动相,检测波长225nm。结果：该方法回收率为100．8％,相对标准偏差为0．12％（n=5)。结论：本方法能较准确地测定三氮唑核苷的含量,可作为三氮唑核苷注射液的质量控制方法。     

司他夫定衍生物的合成及抗肿瘤活性评价

目的设计合成一系列司他夫定类衍生物,并评价其抗肿瘤活性。方法以司他夫定为原料,经磺酸酯化后与叠氮化钠反应生成5'-叠氮基司他夫定,再通过Huisgen 1,3-偶极环加成反应得到目标化合物。采用MTT法分别以人肝癌细胞(BEL-7402)、人胃癌细胞(BGC-823)、肺癌细胞(A549)为测试细胞株对目标化合物进行体外抗肿瘤活性评价。结果与结论合成了14个5'-脱氧司他夫定衍生物,目标化合物的结构经核磁共振氢谱和碳谱确证。其中化合物4k对人肝癌细胞(BEL-7402)、人胃癌细胞(BGC-823)、肺癌细胞(A549)具有中等的抑制作用。     

Nucleoside transport in primary cultured rabbit tracheal epithelial cells

The present study aimed at elucidating the mechanisms of nucleoside transport in primary cultured rabbit tracheal epithelial cells (RTEC) grown on a permeable filter support. Uptake of ³H-uridine, the model nucleoside substrate, from the apical fluid of primary cultured RTEC was examined with respect to its dependence on Na⁺, substrate concentration, temperature and its sensitivity to inhibitors, other nucleosides and antiviral nucleoside analogs. Apical ³H-uridine uptake in primary cultured RTEC was strongly dependent on an inward Na⁺ gradient and temperature. Ten micromolar nitro-benzyl-mercapto-purine-ribose (NBMPR) (an inhibitor of es-type nucleoside transport in the nanomolar range) did not further inhibit this process. ³H-uridine uptake from apical fluid was inhibited by basolateral ouabain (10 μM) and apical phloridzin (100 μM), indicating that uptake may involve a secondary active transport process. Uridine uptake was saturable with a K_m of 3.4 ± 1.8 μM and the V_max of 24.3 ± 5.2 pmoles/mg protein/30 s. Inhibition studies indicated that nucleoside analogs that have a substitution on the nucleobase competed with uridine uptake from apical fluid, but those with modifications on the ribose sugar including acyclic analogs were ineffective. The pattern of inhibition of apical ³H-uridine, ³H-inosine and ³H-thymidine uptake into RTEC cells by physiological nucleosides was consistent with multiple systems: A pyrimidine-selective transport system (CNT1); a broad nucleoside substrate transport system that excludes inosine (CNT4) and an equilibrative NBMPR-insensitive nucleoside transport system (ei type). These results indicate that the presence of apically located nucleoside transporters in the epithelial cells lining the upper respiratory tract can lead to a high accumulation of nucleosides in the trachea. At least one Na⁺-dependent, secondary, active transport process may mediate the apical absorption of nucleosides or analogous molecules.     

Functional and Molecular Characteristics of Na+-dependent Nucleoside Transporters

Pharmaceutical Research - Nucleoside transporters play a critical role in the absorption, disposition, and targeting of therapeutically used nucleosides and nucleoside analogs. This review is...     

Purine nucleoside antimetabolites in development for the treatment of cancer

Purine nucleoside analogs are an important class of drugs that are used in the treatment of cancer. Five purine analogs have been approved by the FDA (mercaptopurine, thioguanine, fludarabine monophosphate, deoxycoformycin and cladribine) and four compounds are currently being evaluated clinically (clofarabine, immucillin-H, nelarabine and 8-chloroadenosine). In addition, two gene therapy approaches are being evaluated that are based on the selective activation of purine nucleoside analogs (ganciclovir, fludarabine monophosphate and others) in tumor cells. Even though nucleoside analogs have been extensively evaluated over the last 50 years, the development of these new compounds demonstrates that there is still much promise in identifying new anticancer drugs from this class of compounds.     

核苷类抗肿瘤抗病毒药物及其合成的进展

综述重要的核苷类抗肿瘤,抗病毒药物及其结构改造和合成的某些进展。     

碳环核苷类化合物的合成

通过氯代环戊烯和相应的嘧啶碱基缩合,再环氧化和开环得到了5′-去羟甲基碳环核苷类似物。所合成化合物经体外L₁₂₁₀和肝癌细胞筛选,并用2215细胞株进行抗乙肝病毒筛选,均未发现有意义的活性。     

New nucleoside analogs in the treatment of solid tumors

Physiologic deoxynucleotides are required for an error-proof DNA replication, repair and synthesis. Any inaccuracy in this process results in a block in DNA synthesis until the error is corrected. If the cell enzymes are unable to correct the error, a signal for apoptosis is generated. This mechanism is the main target for anticancer nucleoside analogs. They also interact with the metabolism of physiological nucleosides, and consequently, have a large number of intracellular targets to induce cytotoxicity. In addition, it is now reported that some analogs may interfere directly with RNA synthesis. A great deal of synthesized nucleoside analogs provide the opportunity to understand the structure-based differences in their metabolism and mechanisms of action as well as to identify the specific intracellular targets and diseases, in which each of these newer nucleoside analogs acts most efficiently. This paper summarizes developments in the area of new nucleoside analogs undergoing clinical evaluation for the treatment of solid tumors, namely tezacitabine, troxacitabine, DMDC, CNDAC, ECyD, clofarabine, and decitabine.     

Nucleoside natural products and related analogs with potential therapeutic properties as antibacterial and antiviral agents

Nucleoside natural products possess a variety of interesting biological activities, including antibacterial, antiviral and antitumor properties, and are therefore expected to be potential candidates for developing drugs. Complex nucleoside natural products exhibiting antibacterial activity by specific inhibition of bacterial cell wall peptidoglycan biosynthesis are described. In addition to the class of antibacterial nucleoside natural products, the newest members of nucleoside natural products exhibiting interesting antiviral activity are briefly described. In spite of promising properties, no nucleoside natural products and their analogs are presently used in the clinic. A global structure–activity relationship of these classes of nucleoside natural products clearly indicates that it is very important to: i) modulate the cell entry ability; and ii) simplify hydrophilic core structures in order to reduce the size of molecules and stabilize the chemically labile structure.