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Pharmacokinetics of gamithromycin after intravenous and subcutaneous administration in pigs 总被引:1,自引:0,他引:1
H. Wyns E. MeyerE. Plessers A. WatteynS. De Baere P. De BackerS. Croubels 《Research in veterinary science》2014
The aim of this study was to investigate the pharmacokinetic properties of gamithromycin in pigs after an intravenous (i.v.) or subcutaneous (s.c.) bolus injection of 6 mg/kg body weight. The plasma concentrations of gamithromycin were determined using a validated high-performance liquid chromatography–tandem mass spectrometry method, and the pharmacokinetics were noncompartmentally analysed. 相似文献
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通过更换反应试剂和改变中间体的纯化方法,对加米霉素的合成进行了工艺优化,使整个反应过程更适合放大生产,且安全环保、成本更低廉。以9-脱氧-9-同型红霉素A (E)肟为原料,在碱性催化剂作用下生成9-脱氧-9-同型红霉素A (Z)肟,再经过贝克曼重排反应生成红霉素亚胺醚,然后硼氢化钠还原生成9-脱氧-8a-氮杂-8a-同型红霉素A,最后还原胺化反应得到加米霉素;并首次获得加米霉素单晶,X-射线衍射单晶结构测定表明,其结构为单斜晶系,C2空间群,具有手性,晶胞参数:a[?]=27.536(6),b[?]=9.6582(19),c[?]=18.529(4),α[°]=90,β[°]°=114.00(3),γ[°]=90,V[?3]=4501.6(15),Z=4,Dc[mg/m~3]=1.177,m[mm~(–1)]=0.086,F(000)=1750,GOF=1.043,Rint=0.0417,R1a,wR2b[I2σ(I)]=0.0492,0.1291,Residuals[e?-3]=0.0564,0.1354。加米霉素晶型的确定为后续研究加米霉素制剂新剂型等方面提供了新选择。 相似文献
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Michael Kellermann Rose A. Huang Andrew B. Forbes Steffen Rehbein 《Research in veterinary science》2014
This study assessed the plasma kinetics and skin/plasma concentration ratio of the azalide antibiotic gamithromycin (ZACTRAN®, Merial) in sheep after a single subcutaneous administration at 6 mg/kg bodyweight. Gamithromycin concentrations in plasma samples collected at various intervals up to 21 days following treatment and metacarpal skin obtained from animals at two, five and ten days after treatment were determined by liquid chromatography–tandem mass spectrometry methods. 相似文献
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本文详细阐述了加米霉素注射液的作用机制、抗菌谱、药代动力学、临床应用和残留研究等内容。加米霉素注射液在治疗肉牛和非泌乳奶牛的呼吸系统疾病中有较好的应用前景,本文为其研究与开发提供一定的参考。 相似文献
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建立牛血浆中加米霉素含量的UPLC-MS/MS检测方法。血浆样品经甲醇沉淀蛋白,外标法定量, 使用Waters ACQUITY UPLC HSS T3色谱柱,以甲醇:10 mM乙酸铵缓冲液为流动相,流速0.3 mL?min-1;柱温:50℃;进样量:10 μL。三重四级杆质谱仪电喷雾离子源(ESI),正离子扫描、多反应监测(MRM)。考察方法的线性范围、准确度与精密度、稳定性和稀释可靠性。结果显示,加米霉素出峰时间在1 min左右,本方法在1 ng?mL-1~100 ng?mL-1浓度范围内呈良好的线性关系,相关系数(r)≥0.999,检测限(LOD)和定量限(LOQ)分别为0.5 ng?mL-1和1 ng?mL-1。3个浓度(1 ng?mL-1、50 ng?mL-1和100 ng?mL-1)的空白血浆添加样品批内和批间平均回收率分别在85.2%~96.4%和87.7%~94.0%之间,相对标准偏差(RSD)分别在1.4%~13.9%和2.9%~8.6%之间。准确度和精密度、稳定性及稀释可靠性均符合生物样品分析的相关要求。本方法可用于牛的血浆中加米霉素的浓度测定及药代动力学研究。 相似文献
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