RP-HPLC法测定阿苯达唑口服乳剂中阿苯达唑的含量

目的 建立RP-HPLC法测定阿苯达唑口服乳剂的含量.方法 采用RP-HPLC法.色谱柱:Diamonsil C18(250 mm×4.6 mm,5 μm);流动相:甲醇-水(70∶30);流速:1.0 mL·min-1;检测波长:295 nm;柱温:35 ℃.结果 阿苯达唑的线性范围为质量浓度50～200 mg·L-...     

阿苯达唑自微乳释药系统在大鼠体内组织分布

目的:通过高效液相色谱法,对大鼠口服阿苯达唑(ABZ)自微乳后组织分布作初步的研究。方法:高效液相色谱法,以阿苯达唑原料药和市售片剂做对照,对口服阿苯达唑自微乳浓缩液进行大鼠体内组织分布研究,考察不同制剂体内的药物分布是否有显著性差异。结果:组织匀浆液浓度测定方法的回收率均大于70%,日内、日间精密度均小于12%;自微乳在大鼠体内分布较广,与原料药及片剂相比,各组织均有不同程度的增加,其中在体内药物浓度分布趋势为肝>肺>肠>脾>肾>胃>脑。结论:与原料药和片剂比较,ABZ-SMEDDS体内分布迅速,组织分布广泛,促进了药物口服吸收,改变了ABZ在体内的组织分布。     

抗寄生虫药阿苯达唑新活性研究

阿苯达唑在临床上作为一种广谱的抗寄生虫药物使用已有近30年。20世纪90年代末期,阿苯达唑的抗肿瘤研究开始逐渐引起药物研究者的关注,其抗微管聚合的作用机制已经得到证实。同时1H-苯并咪唑-2-氨基甲酸酯作为合成阿苯达唑的前体化合物在体外与体内均也表现出抗肿瘤作用。苯并咪唑类化合物潜在的抗肿瘤作用,给药物研究者将其作为抗肿瘤先导化合物进行改造提供了思路和方向。     

阿苯达唑的合成

阿苯达唑(albendazole,1),化学名为5(6)-丙硫基苯并咪唑-2-氨基甲酸甲酯,是美国Smith Kline公司1977年上市的一种广谱、高效、低毒的驱虫药。据文献报道,1的合成路线达7种以上。目前,国内工业化生产多用邻硝基苯胺路线。但这一路线所用的主要原料有毒性,且单耗也大。现介绍一种以农药多菌灵为起始原料,二步合成1的简捷方法。多菌灵价廉易得,质     

阿苯达唑精制方法

介绍了阿苯达唑精制的四种成盐游离方法:1.混合溶剂法,2.稀溶剂法,3.水法,4.盐析分离法。     

阿苯达唑片的紫外导数光谱测定法

采用一阶导数紫外分光光度法测定阿苯达唑片含量。阿苯达唑浓度为5～30μg/ml 时,239nm处的振幅与浓度有良好的线性关系,r=0.9998,平均回收率100.5%,cv 0.78%。     

抗棘球蚴药物研究：阿苯达唑代谢物及其类似物的合成

合成了共２５个阿苯达唑代谢物及其类似物。感染棘球蚴小鼠试验表明，其中７个化合物对细粒棘球蚴有较好的作用，而以阿苯达唑亚砜（１３）效果最好，治疗剂量仅为阿苯达唑的一半，抗小鼠继发生细粒棘球蚴病的疗效高于后者。另一个代谢物阿苯达唑砜则无杀虫作用。     

阿苯达唑的不良反应

阿苯达唑（albendazole,商品名：肠虫清）是一种高效广谱驱虫新药。较常见的不良反应有头晕、头痛、发热等。但有关该药新的不良反应时有报道,现综述如下：1过敏性紫席多畸,多满祥［‘j报道1女患儿,12岁,服用阿苯达硅片0．4g,sh后出现过敏性紫盛。2白细胞和血小板减少温浩,姚秉礼,邹培范［’j报道用该药治疗包虫病时出现白细胞减少。国外学者也报道了该药引起白细胞减少的病例。Davis报道服用该药治疗包虫病时有血小板减少病例发生。3恶性脱发刘光汉,李建元［”报道用该药治疗脑囊虫病时,有2例病人出现恶性脱发。Davis亦报道治疗…     

阿苯达唑的不良反应

阿苯达唑的不良反应０５６０００河北医科大学附属第二医院药剂科苏春平，杨香爱，崔晓红，王川平石家庄市第二医院苏春晓阿苯达唑（丙硫咪唑，肠虫清，Ａｌｂｅｎｄａｚｏｌｅ，Ｚｅｎｔｅｌ），由美国ＳｍｉｔｈＫｌｉｎ，厂商开发，并于１９７７年首次上市，属高效低毒...     

Nano-based antileishmanial agents: A toxicological study on nanoparticles for future treatment of cutaneous leishmaniasis

Cutaneous leishmaniasis (CL) is endemic in the tropical and subtropical countries. Antileishmanial drugs that are traditionally used for treatment of CL are mainly toxic, ineffective for some parasite isolates, and mostly expensive. Previous studies showed that some metal and metal oxide nanoparticles have antimicrobial activity. Moreover, the use of nanoparticles together with ultra violet (UV) and infra red (IR) light increases toxic effects of nanoparticles by generation of reactive oxygen species (ROSs) and heat, respectively. There is little information on antileishmanial activity of nanoparticles, alone or together with UV/IR. Thus, the purpose of this research was to study antileishmanial effects of some nanoparticles including silver nanoparticles (Ag NPs), gold nanoparticles (Au NPs), titanium dioxide nanoparticles (TiO₂ NPs), zinc oxide nanoparticles (ZnO NPs), and magnesium oxide nanoparticles (MgO NPs) on Leishmania major parasites under UV, IR, and dark conditions. After 24 h exposure to nanoparticles, different biological parameters such as cell viability, proliferation, infectivity, and infection index were investigated under UV/IR/dark conditions. In this study, the highest antileishmanial activity was seen for Ag NPs, followed by Au NPs, TiO₂ NPs, ZnO NPs, and MgO NPs. Both UV and IR light increased antileishmanial properties of all nanoparticles. In spite of antileishmanial activity of nanoparticles under UV, IR, and dark conditions, these nanoparticles had high cytotoxicity on macrophages, which must be considered in future studies. The authors declare that the use of nanoparticles for treatment of CL may have both positive and negative consequences.     

Quantitative determination of albendazole metabolites in sheep spermatozoa and seminal plasma by liquid chromatographic analysis with fluorescence detection

A new analytical method for the simultaneous quantitative determination of albendazole metabolites in sheep spermatozoa and seminal plasma at levels down to 46.5 ng/mL for albendazole sulphoxide (ABZ-SO), 7.5 ng/mL for albendazole sulphone (ABZ-SO₂) and 12 ng/mL for albendazole 2-aminosulphone (ABZ-SO₂NH₂) has been developed. Analytes were extracted from alkalinized samples with ethyl acetate. Separation was carried out on a C₁₈ column in the presence of tetra-n-butylammonium (TBA) hydrogen sulphate and octanesulphonate sodium (OCT), as ion-pair agents. Fluorometric detection was performed with excitation and emission wavelengths set at 290 and 320 nm, respectively. Accuracy data showed overall recoveries (±S.E.M.) of 83.1±1.2% for ABZ-SO, 98.8±0.6% for ABZ-SO₂ and 85.3±0.7% for ABZ-SO₂NH₂, in spermatozoa. Respective values in seminal plasma were 88.0±0.9%, 97.7±0.5% and 93.2±1.7%. Precision data suggested coefficient of variation (CV%) values lower than 5.9% for spermatozoa and 3.8% for seminal plasma. The method was successfully applied for the determination of the three albendazole metabolites in semen samples collected from rams that had been orally administered albendazole.     

Triglyceride-coated nanoparticles: Skin toxicity and effect of UV/IR irradiation on them

Triglyceride (TG) is an important compound on the skin, produced by sebaceous glands, and may change cytotoxicity of different nanoparticles. To date, there is no report about toxicity of nanoparticles coated with TG. On the other hand, the use of ultraviolet (UV) and infrared (IR) with nanoparticles changes nanoparticle cytotoxicity. The combination of nanoparticles with UV or IR is applicable, because it may be used for treatment or detection of local cancers, surface microbial infections and other skin diseases. In this study, different nanoparticles including titanium dioxide, zinc oxide, magnesium oxide, silver, gold, and TG-coated form of these nanoparticles, were added to suspensions of Balb/c skin cells, and then incubated for 24 h at 37 °C. Additionally, TG-coated nanoparticles were treated with UV and IR irradiation for 1 h. Different methods were applied for evaluation of cytotoxicity, including 5-diphenyl-tetrazolium bromide assay, lactate dehydrogenase (LDH) assay, cell metabolic assay, ATP assay, and reactive oxygen species (ROS) generation assay. This research showed that TG-coated nanoparticles had less LDH release and ROS generation with higher cell viability, cell metabolic activity, and ATP level, compared with pristine nanoparticles. In contrast, the combination of UV and IR with TG-coated nanoparticles led to higher LDH release and ROS generation with less cell viability, cell metabolic activity, and ATP level, in comparison with pristine nanoparticles. Overall, pristine metal nanoparticles without irradiation had higher cytotoxicity than metal oxide nanoparticles.     

Stability studies on diloxanide furoate: effect of pH, temperature, gastric and intestinal fluids

The degradation of the amoebicide diloxanide furoate in alkaline medium at different temperatures was investigated using both a spectrophotometric and a developed HPLC method. In solutions, the drug was found to undergo decomposition, i.e., temperature and pH dependent. The pH-rate profile at pH between 7.6 and 9.6 indicated a first-order dependence of Kobs on [-OH]. Arrhenius plot obtained at pH 8 was linear between 40 and 63 degrees C. The estimated activation energy of hydrolysis was found to be 18.25 kcal degree.mol(-1). The effect of simulated gastric and intestinal fluids on the drug was also investigated. A new thin-layer chromatographic (TLC) procedure for the fractionation of the drug and its alkaline hydrolysis products has been developed and was found to compare favorably with that of the British Pharmacopoeia. Three hydrolysis products of a basic methanolic solution of the drug, namely furoic acid, diloxanide and methylfuroate could be identified by the use of TLC, HPLC, infrared and mass spectrometry.     

What do we (need to) know about the kinetic properties of nanoparticles in the body?

Nowadays the development and applications of nanotechnology are of major importance in both industrial and consumer areas. However, the knowledge on human exposure and possible toxicity of nanotechnology products is limited. To understand the mechanism of toxicity, thorough knowledge of the toxicokinetic properties of nanoparticles is warranted. There is a need for information on the absorption, distribution, metabolism and excretion (ADME) of nanoparticles and validated detection methods of these man-made nanoparticles. Determination of the ADME properties of nanoparticles requires specialised detection methods in different biological matrices (e.g. blood and organs). In this paper, the current knowledge on the kinetic properties of nanoparticles is reviewed. Moreover, knowledge gaps from a kinetic point of view (detection, dose, ADME processes) are identified.     

紫球藻(Porphyridiumcruentum)原生质体分离研究

收集对数生长期的紫球藻细胞,经1%氯化苄预处理后,用1.8%纤维素酶和1.2%果胶酶组成的混合水解酶液（含0.6mol/LNaCl,pH7.2）,在28℃下缓慢振荡酶水解细胞壁,4h后原生质体分离率比未预处理组提高74%,在最佳分离条件下的原生质体分离率高达56.4%,基本能满足原生质体融合的需求。     

HPLC法测定阿苯达唑颗粒的含量

目的:建立阿苯达唑颗粒含量的高效液相测定方法.方法:色谱柱为Waters C18 柱(4.6mmx150mm,5μm),流动相为甲醇一水(75:25),流速为1.0ml/min,检测波长为295nm,柱温为30℃.结果:阿苯达唑在1- 20μg/ml浓度范围内呈良好线性关系(r=1.0),平均加样回收率为100.1%(...     

复方制剂中双羟萘酸噻嘧啶及阿苯达唑含量测定方法的研究

本文采用双波长法分别测定驱虫药复方制剂的有效成份双羟萘酸噻嘧啶及阿苯达唑，进行了方法学研究、线相关系、加样回收等实验工作，两种效成分的回收率分别为１００．６±０．６８％，９９．２７±０．５９％（ｎ＝２），含量在其标示量的±２０％范围内线性关系良好，分别为ｒ＝０．９９９９，ｒ＝－９９９８。     

Review of health safety aspects of nanotechnologies in food production

Due to new, previously unknown, properties attributed to engineered nanoparticles many new products are introduced in the agro-food area. Nanotechnologies cover many aspects, such as disease treatment, food security, new materials for pathogen detection, packaging materials and delivery systems. As with most new and evolving technologies, potential benefits are emphasized, while little is known on safety of the application of nanotechnologies in the agro-food sector. This review gives an overview of scientific issues that need to be addressed with priority in order to improve the risk assessment for nanoparticles in food. The following research topics are considered to contribute pivotally to risk assessment of nanotechnologies and nanoparticles in food products.

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Set a definition for NPs to facilitate regulatory discussions, prioritization of research and exchange of study results.     

高效液相色谱法测定阿苯达唑的含量

目的:建立高效液相色谱法测定阿苯达唑的含量。方法:采用Lichrospher 100 RP-18(5μm,250mm×4mm)柱。以甲醇-0.1 mol/L醋酸钠缓冲液(用醋酸调节pH=3.1)(60:40)为流动相,用紫外检测器于254nm波长处检测。结果:阿苯达唑浓度在0.1～0.8mg/ml范围内有较好的线性关系(r=0.9992),RSD=0.5％(n=6)。结论:本法快速简便,准确。