高效液相色谱法测定柴辛注射液中有效组分含量的研究

为同时测定柴辛注射液中有效组分甲基丁香酚、细辛脂素的含量,建立了以核壳型分离填料为色谱柱,乙腈和水为流动相,检测器波长为287 nm,流量为1.0 mL/min的高效液相色谱方法。结果显示,在0.15~150 μg/mL的质量浓度范围内,甲基丁香酚的线性曲线为Y=7 243X-258,r=0.9999,检测限为0.025 μg/mL,平均回收率在97.47%~100.53%之间,RSD为0.92%~2.17%;细辛脂素的线性曲线为Y=18 853X -676,r=0.9999,检测限为0.012 μg/mL,平均回收率在88.47%~92.23%之间,RSD为1.48%~3.55%。该方法操作简单,准确度、重复性、精密度好,可适用于柴辛注射液的质量控制。     

长效土霉素注射液的配方筛选及其质量浓度测定

筛选长效土霉素注射液的最优配方,制备长效土霉素注射液,并对土霉素质量浓度进行测定。通过预试验,确定长效土霉素注射液的各组分及其大致范围,以质量浓度变化量为检测指标,利用正交试验确定长效土霉素注射液的最优配方。制备长效土霉素注射液,并利用紫外分光光度法对土霉素有效质量浓度进行考察,计算其回收率。长效土霉素注射液的最优配方为,每100 mL长效土霉素注射液中含有30 g盐酸土霉素、6 g MgCl2、0.6 g甲醛合次硫酸氢钠、60 mL复合有机溶媒(由甘油甲缩醛和聚乙二醇200按照适当比例配制)、7.5 g聚乙烯吡咯烷酮K175、.4 mL单乙醇胺、其余为注射用水。所制备的长效土霉素注射液在5~30mg/L时呈现良好线性关系,平均回收率为97.86%,RSD为1.15%。该长效土霉素注射液的配方合理,土霉素效价稳定,产品回收率高。     

澳洲茄胺盐酸盐注射剂对小鼠Lewis肺癌抑瘤作用研究

目的通过3次抑瘤实验观察研究澳洲茄胺盐酸盐注射剂对小鼠Lewis肺癌的抑瘤作用.方法通过肿瘤细胞悬液接种法,制备小鼠Lewis肺癌动物模型,采用腹腔注射给药法,连续7 d,2次/d.给药结束后解剖小鼠,取瘤称重,观察药物作用.结果从给药剂量上来看,与对照组比较,11 mg/kg剂量组开始出现抑瘤作用,抑瘤率为43.82%,P〉0.05,虽有抑瘤作用,但无统计学意义;22 mg/kg组抑瘤率为65.32%,P〈0.001;33 mg/kg组抑瘤率为66.92%,P〈0.001;44 mg/kg组抑瘤率为78.53%,P〈0.001;55 mg/kg组抑瘤率为79.73%,P〈0.001.结论受试药物澳洲茄胺盐酸盐注射剂对小鼠Lewis肺癌有明显的抑瘤作用,受试药物从22 mg/kg剂量组开始到55 mg/kg剂量组为有效剂量组,4个剂量组之间呈现明显的量效关系.     

地龙注射液免疫活性的体外研究

[目的]探讨地龙注射液的免疫调节活性及其作用机理。[方法]通过地龙注射液体外培养刺激小鼠脾淋巴细胞,采用MTT法和双抗夹心ELISA法测定地龙注射液对小鼠脾淋巴细胞增殖及分泌细胞因子IL-2的影响。[结果]地龙注射液能显著地直接或协同ConA或LPS刺激脾淋巴细胞增殖,也能极显著地增加IL-2的分泌量。[结论]该研究表明地龙注射液具有较明显的免疫调节活性。     

顶隙柱塞在非道路国Ⅱ排放柴油机中的研究及应用

对顶隙柱塞的工作原理进行分析,对我公司现生产的顶隙柱塞和普通柱塞的喷油提前特性进行了对比分析,并在某一非道路国Ⅱ排放发动机上进行性能及排放试验。试验结果表明,顶隙柱塞能够满足非道路国Ⅱ排放柴油机的性能和排放要求,具有推广价值。     

Combined subcutaneous administration of ivermectin and nitroxynil in sheep: Age/body weight related changes to the kinetic disposition of both compounds

The effect of age/body weight in the plasma disposition kinetics of ivermectin (IVM) and nitroxynil (NTX) after their co-administration as a combined formulation to sheep was studied. Sixteen (16) male sheep were allocated into two experimental groups (n = 8 each): (a) high body weight (high bw) (18-20 months old), and (b) low body weight (low bw) (6-8 months old). Animals in both groups were subcutaneously (sc) treated with IVM (200 μg/kg) and NTX (10 mg/kg) using a commercially available combined formulation (Nitromectin^®, Lab. Ovejero, Spain). Blood samples were taken by jugular venopuncture before (time 0), at 2, 4, 8, 12 h and at 1, 2, 3, 5, 7, 10, 15, 20, 25, 35, 40, 50 and 60 days after administration. Recovered plasma was analysed to quantify IVM and NTX by HPLC. Higher IVM plasma concentrations were measured until 20 days post-administration in “low bw” compared to “high bw” animals, where IVM was recovered up to 35 days post-treatment. The IVM absorption process greatly differed between experimental groups. A significantly higher (p < 0.01) C_max (36.7 ± 7.52 ng/ml) value was obtained at a delayed (p < 0.05) T_max (48.0 ± 0.0 h) in light compared to heavy (C_max: 8.0 ± 0.80 ng/ml; at 34.0 h) body weight sheep. IVM elimination half-life and mean residence time were significantly shorter in light compared to heavy (older) sheep. NTX mean plasma concentrations were lower in “low bw” compared to those measured in “high bw” sheep, with elimination phases declining up to 60 d post-administration in both experimental groups. The NTX AUC value in “low bw” (1188.5 ± 122.6 μg day/ml) was significantly lower (p < 0.05) than that obtained in the “high bw” (oldest) animals (1735.0 ± 155.8 μg day/ml). Shorter NTX elimination half-life and mean residence time (p < 0.01) were obtained in the youngest (“low bw”) compared to the oldest (high bw) sheep. The work reported here assessed for the first time the disposition of IVM and NTX after their combinated injection to sheep, demonstrating that animal body weight/development greatly affects the kinetic behaviour of both anthelmintic drugs.     

复方伊维菌素乳液在山羊体内的药代动力学研究

为了探讨复方伊维菌素乳液在动物体内的药物代谢,为兽医临床提供用药参考。试验选取7只山羊,每只山羊按0.1 mL/kg (伊维菌素0.2 mg/kg, 阿苯达唑10 mg/kg)剂量口服,给药后0.5、1、2、3、4、6、8、12、16、24、36、48、60 h颈静脉采血5 mL,分离血清,-20 ℃保存,用高效液相色谱仪检测样品血药浓度。试验结果表明,①伊维菌素在山羊体内的代谢情况为：0.5 h,0.112151 μg/mL; 第1次达峰时间为4 h, 0.302702 μg/mL;第2次达峰时间为16 h,0.258284 μg/mL;60 h,0.011118 μg/mL。②阿苯达唑在山羊体内的代谢情况为：0.5 h, 0.049285 μg/mL;第1次达峰时间为8 h,4.95283 μg/mL ;第2次达峰时间为16 h,5.694551 μg/mL;60 h,0.06434 μg/mL。复方伊维菌素中的伊维菌素和阿苯达唑在山羊体内代谢时间短,第60小时已达到很低的血药浓度。     

高效液相色谱法测定伊维菌素脂质体药物的含量及包封率

本试验旨在建立伊维菌素脂质体载体药物含量及包封率测定的高效液相色谱法。Waters surfire C18柱(150 mm×2.1 mm,5 μm),流动相为乙腈—甲醇—水(62∶30∶8),流速1 mL/min,检测波长245 nm,进样量10 μL,柱温30 ℃。采用凝胶过滤法、透析法、冷冻超速离心法、超滤离心法4种方法对脂质体与药物进行分离。结果表明,在优化色谱条件下伊维菌素与辅料及溶剂峰均得到良好分离,伊维菌素在1～50 μg/mL浓度范围内线性关系良好(r=0.9998,n=5),最终采用超速冷冻离心法可将脂质体与药物很好的分离,伊维菌素脂质载体的包封率可达98.54%±1.6%。该方法准确可靠、简单快速,可用于伊维菌素脂质体载体药物含量及包封率的测定。     

0.5%依维菌素微乳剂的研制

[目的]详细介绍0.5%依维菌素微乳剂的研制过程及性能测定技术。[方法]对0.5%依维菌素微乳剂的配方进行研究,筛选出最优良的表面活性剂、助表面活性剂,确定其最佳配方和制备方法,并对0.5%依维菌素微乳剂的质量指标和性能及防治效果进行测定,分析不同水质对其研制的影响。[结果]结果表明,0.5%依维菌素液乳剂含水量约为67%,加水稀释后在水中分散的油珠直径比乳油制剂稀释的小,显著提高了防治效果和原药利用率。同时不燃爆,贮运安全。[结论]0.5%依维菌素微乳剂是一个值得推广的农药新制剂。