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硝酸异山梨酯注射剂在中国志愿者中的药动学研究

Studies on the pharmacokinetics of isosorbide dinitrate (ISDN) injection in healthy volunteers
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摘要 目的 研究硝酸异山梨酯(ISDN)注射剂在中国志愿者中的药动学。方法 采用气相色谱-电子捕获检测方法测定人血浆中ISDN及其两个活性代谢产物:2-单硝酸异山梨酯(2-ISMN)和5-单硝酸异山梨酯(5-ISMN)的浓度。结果 ISDN,2-ISMN和5-ISMN的Cmax分别为(18.5±7.d),(58.8±4.4),(209.3±49.8)ng·mL-1;AUC0-T分别为(84.84±27.8),(380.5±59.4),(1384.1±426.6)ng·h·mL-1;t1/2分别为(1.0 4±9.2),(2.6±O.8),(6.1±0.9)h。结论 静脉滴注ISDN后可迅速起效,且维持时间长,是理想的快速起效的抗心肌缺血药物。 OBJECTIVE: To study the pharmacokinetic profiles of isosorbide dinitrate (ISDN) injection in Chinese healthy volunteers. METHODS: 20 mg of ISDN was intravenously infused to 18 heathy volunteers. ISDN, 2-ISMN and 5-ISMN concentrations in plasma were determined by gas chromatography with ECD detection. RESULTS: Cmax of ISDN, 2-ISMN and 5-ISMN were (18.5 ± 7.4), (58.8 ± 4.4) and (209.3 ± 49.8) ng&middotmL -1 respectively; AU0-T were (84.8 ± 27.8), (380.5 ± 59.4) and (1 384.1 ± 426.6) ng&middoth&middotmL-1 respectively; t1/2 were (1.0 ± 0.2), (2.6 ± 0.8) and (6.1 ± 0.9) h respectively. CONCLUSION: ISDN injection is an ideal vasodilator and anti-angina formulation, especially suitable for acute conditions due to its rapid onset and long duration.
出处 《中国药学杂志》 EI CAS CSCD 北大核心 2004年第5期369-371,共3页 Chinese Pharmaceutical Journal
关键词 硝酸异山梨酯注射剂 中国志愿者 药动学 气相色谱 电子捕获 测定 Body fluids Gas chromatography Health care Vaccines
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参考文献2

  • 1Booth BP, Bennett BM, Brien JF, et al.Assay of glyceryl trinitrate,isosorbide dinitrate, and their metabolites in plasma by large-pore capillary column gas-liquid chromatography [J].Biopharm Drug Disposit, 1990,11:663.
  • 2Santoni Y, Rolland PH, Cano JP.Determination of isosorbide dinitrate and its mononitrate metabolites in human plasma using Extrelut(R)purification and capillary column gas-liquid chromatography [ J ].J Chromatogr , 1984,306:165.

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