丙硫咪唑对异盘并殖吸虫皮层及肠上皮作用的扫描电镜观察

将丙硫咪唑按100mg/kg/d×2灌胃治疗大鼠异盘并殖吸虫病。扫描电镜显示虫体皮层明显水肿,尾部塌陷。治疗后第5天口吸盘周围皮层水肿呈棉絮状,腹吸盘周围皮层灶性坏死,尾部尚见肿胀之乳突,肠上皮灶性坏死,片层融合成板状。     

HPLC测定复方阿苯达唑片的含量

目的　用HPLC法测定复方阿苯达唑片中阿苯达唑和双羟萘酸噻嘧啶的含量。方法　采用硅胶柱 ,以乙腈 -混合液[水 -乙酸 -二乙胺 (2 .5∶2 .5∶1) ](5 4∶1)为流动相 ,检测波长 2 88nm。结果　阿苯达唑的线性范围为 0 2～ 0 6 μg ,回归方程为 :Y =1.832× 10 6X +7.2 84× 10 3 (r=0 .9998) ;双羟萘酸噻嘧啶的线性范围为 0 .8～ 2 .4 μg ,回归方程为 :Y =1 2 5 5× 10 6X -1 736× 10 4(r=0 .9995 )。结论　所用方法简便、快速 ,准确、可靠。     

Assessment of liver slices for research on metabolic drug–drug interactions in cattle

1.?Precision-cut liver slices (PCLS) from food-producing animals have not been extensively used to study xenobiotic metabolism, and thus information on this field of research is sparse.

2.?The aims of the present work were to further validate the technique of production and culture of bovine PCLS and to characterize the metabolic interaction between the anthelmintic albendazole (ABZ) and the flavin-monooxygenase (FMO) inhibitor methimazole (MTZ).

3.?Nine steers were used as donors. PCLS were produced and incubated under two methods: a dynamic organ culture (DOC) incubator and a well-plate (WP) system.

4.?Tissue viability, assessed through both structural and functional markers, was preserved throughout 12?h of incubation. ABZ was metabolized to its (+) and (-) albendazole sulfoxide stereoisomers (ABZSO) in bovine PCLS. The interaction between ABZ and MTZ resulted in a reduction (p?p?5.?Both culture systems were suitable for assessing the interaction between ABZ and MTZ.

6.?Overall, the results presented herein show that PCLS are a useful and reliable tool for short-term studies on metabolic drug–drug interactions in the bovine species.     

Anthelmintic activity of ethanolic leaf extract of Jasminum mesnyi

ObjectiveTo evaluate the anthelmintic activity of ethanolic extract of leaves of Jasminum mesnyi.MethodsAnthelmintic activity was carried out on adult Indian earthworm Eisenia fetida. In this study, 20 mg/mL and 40 mg/mL concentrations of plant extract were tested which involved the time of paralysis and time of death of worm. Albendazole (10 mg/mL) was taken as reference standard drug whereas distilled water was used as control.ResultsThe extract exhibited significant anthelmintic acitivity which was more in higher concentration extract.ConclusionsIt was concluded from the present study that the plant exhibited significant anthelmintic activity.     

汉防己甲素和阿苯达唑体外抗细粒棘球蚴原头节作用的观察

通过比较汉防己甲素和阿苯达唑体外抗细粒棘球蚴原头节作用，以探讨中药单体汉防己甲素抗包虫病的作用，将汉防己甲素和阿苯达唑分别配成不同浓度，加入RPMI 1640培养基中，体外培养细粒棘球蚴原头节，观察其每天的死亡率。结果显示各用药组原头节的死亡率分别与对照组相比，差异均有统计学意义(P＜0．01)；阿苯达唑和汉防己甲素联合组与阿苯达唑组，汉防己甲素低、中浓度组相比，差异有统计学意义(P＜0．05)，而与汉防己甲素高浓度组相比，差别无统计学意义(P＞0．05)。表明汉防己甲素在体外有明显的抗原头节作用；汉防己甲素体外抗原头节作用与阿苯达唑相当．同时两药联合抗原头节效果明显优于单药组，两药联合可能具有协同效果。     

Synthesis and characterization of mesoporous SBA-15 and SBA-16 as carriers to improve albendazole dissolution rate

Albendazole (ABZ, anti-parasitic active pharmaceutical ingredient) is a crystalline low water-soluble drug, thus the dissolution rate in gastrointestinal fluids is limited. Consequently, the improvement of the water solubility and dissolution rate of ABZ implies a great challenge for a more efficient treatment of hydatidosis. In this context, SBA-15 and SBA-16 ordered mesoporous silica materials were synthetized and loaded with ABZ. X-ray diffraction, FT-IR spectroscopy, nitrogen physisorption manometry, particle size distribution and scanning electronic microscopy were used to characterize unloaded and loaded materials (ABZ/SBA-15 and ABZ/SBA-16). The loaded ABZ amount in the carriers was estimated by elemental analysis. For the loaded materials, the drug solubility and release profile were evaluated. In addition, mathematical models were compared to explain the dissolution kinetics of ABZ from mesoporous solids. ABZ was successfully loaded into the mesopores. The amorphous state of the adsorbed ABZ was confirmed by differential scanning calorimetry that resulted in a notable increment in the dissolution rate compared to crystalline ABZ. Drug release behaviors were well simulated by the Weibull model for ABZ/SBA-15 and by the Gompertz function for pure ABZ and ABZ/SBA-16. The SBA-15 carrier exhibited the highest drug loading and dissolution rate becoming a promising material to improve ABZ bioavailability.     

旋毛虫病的诊断与治疗

旋毛虫病无特异性的症状和体征, 临床诊断较困难, 所以流行病学资料非常重要, 患者常有食生或半生肉类史, 在该病暴发时期, 同批患者往往能追溯到聚餐史。 在肠道期可出现腹痛、 腹泻伴全身不适等症状。发热、 眼睑或面部水肿、 肌肉疼痛是急性期的主要表现, 重症患者可并发心肌炎、 肺炎及脑炎等。多数患者感染后2～5周外周血中嗜酸粒细胞增多。应用肌幼虫排泄-分泌(ES)抗原和合成的泰威糖(tyvelose, 3,6-双脱氧己糖)抗原ELISA检测旋毛虫抗体IgG, 具有较高的特异性和敏感性, 是初步诊断旋毛虫感染的首选血清学方法, ELISA阳性者需经蛋白质印迹分析确认。旋毛虫病的确诊主要依靠肌肉活检发现旋毛虫幼虫。阿苯达唑是治疗旋毛虫病的首选药物, 剂量为20～30 mg/(kg·d), 分2次口服, 疗程5～7 d。糖皮质激素可延长旋毛虫感染的肠道期和增加肌肉虫荷, 一般仅用于重症患者且需与阿苯达唑联合应用。     

与抗寄生虫药物阿苯达唑相关的中国发明专利

本文对在中国已授权的阿苯达唑药物发明专利进行综述,从专利角度反映抗寄生虫药物阿苯达唑的研究现状,为从事阿苯达唑药物研究或申请有关发明专利的研究人员提供资料。