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涂佳卉,等:LC-MS/MS 法测定小型猪血浆中泰妙菌素浓度及其在不同制剂
第 57 卷第 1 期 药代动力学研究中的应用 59
Table 1 Main pharmacokinetic parameters of different tiamulin formulations in minipigs ( x ± s, n=6)
Tiamulin fumarate active
Parameter pharmaceutical ingredient Tiamulin formulation 1 Tiamulin formulation 2 Tiamulin formulation 3
(ig, 20 mg/kg)
(ig, 20 mg/kg)
(ig, 20 mg/kg)
(iv, 10 mg/kg)
c 0 /(ng/mL) 4 383.73±2 676.78 — — —
c max /(ng/mL) — 552.00±328.55 545.00±136.97 590.60±237.02
t max /h — 1.47±0.68 0.27±0.15 0.88±0.72
AUC 0-t /(h·ng/mL) 4 803.50±965.68 2 348.30±1 553.52 1 456.94±641.43 1 631.18±440.47
AUC 0-∞ /(h·ng/mL) 4 862.63±982.15 2 416.32±1 544.96 1 486.33±634.59 1 650.51±432.79
t 1/2 /h 4.66±1.68 3.89±1.00 3.39±0.80 3.46±0.73
V d */(L/kg) 13.58±3.09 59.15±35.89 75.02±32.78 64.24±23.15
−1
−1
#
CL /(L·kg ·h ) 2.14±0.46 10.20±3.97 15.86±6.88 12.80±3.27
MRT 0-∞ /h 4.43±1.60 4.90±1.08 4.00±1.00 4.36±0.71
F/% — 24.85 15.28 16.97
“ —” indicates the parameter has no pharmacokinetic significance under the corresponding administration route; “ *” indicates the parameters
#
corresponding to intragastric administration (ig) is V/F;“ ”indicates the parameters corresponding to intragastric administration (ig) is CL/F
靠性。通过非房室模型对不同制剂经灌胃后的主 change olid phase extraction-ultra performance liquid chro-
matography-tandem mass spectrometry[J]. J Zhejiang Univ Sci
要药动学参数进行比较,泰妙菌素制剂一在小型猪 Ed (浙江大学学报 理学版), 2019, 46(4): 466-473.
体内的暴露量 AUC 、AUC 0-∞ 及绝对生物利用度 [6] Yu C, Zhen JH, Xiang JL, et al. Determination of tiamulin and
0-t
F 均略高于其余两种制剂,提示其吸收程度和制剂 valnemulin in Chinese medicine preparations for veterinary use
by solid phase extraction-performance liquid chromatography-
工艺更优,但组间差异未达到统计学显著性水平 tandem mass spectrometry[J]. China Port Sci Technol (中国口
(P>0.05)。进一步分析制剂差异的潜在原因:泰妙 岸科学技术), 2023, 5(7): 64-71.
[7] Xu Q. Clinical effects of tiamulin on contagious pleuropneumo-
菌素制剂一的 c max (552.00±328.55 ng/mL)与其余两 nia of goat by using atomization administration[D]. Yangzhou:
组相近,且标准差较大(328.55 ng/mL),推测与预混 Yangzhou University, 2022.
[8] Elazab ST, Elshater NS, Hashem YH, et al. Tissue residues and
剂原料分散性不足或辅料工艺控制不当导致的个 pharmacokinetic/pharmacodynamic modeling of tiamulin
体吸收差异有关;而所有制剂的绝对生物利用度均 against Mycoplasma anatis in ducks[J]. Front Vet Sci, 2020, 7:
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不足 25%,可能与药物首过效应较强、在胃肠道稳
[9] Zeng JJ, Zhang XJ, Chen Y. Determination of tiamulin and val-
定性不足,或与制剂释放不完全、肝肠循环代谢损 nemulin in aquatic products by dispersive solid phase extrac-
失有关。本研究结果不仅为泰妙菌素最优制剂的 tion-ultra high performance liquid chromatography-tandem
mass spectrometry[J]. J Anhui Agric Sci (安徽农业科学), 2020,
筛选提供了直接实验依据,也为临床给药方案的优 48(10): 164-167,189.
化及兽药残留监测提供了技术参考。 [10] Xia BL, Wang ST, Yin JJ, et al. Simultaneous determination of
43 antibacterials from nine categories in water using automatic
sample loading-solid phase extraction-ultra performance liquid
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