Objective: To study the absoulte bioavailability of dezocine oral liquid, a rapid HPLC-MS/MS for the determination of dezocine in human plasma wasdeveloped and applied. Methods: Sample preparation was performed through a simple protein precipitation by acetonitrile. The chromatographic separation was achieved on an Aglient SB-C18column (2.1 mm×50 mm, 3.5 μm) with the mobile phase of acetonitrile and 5 mmol·L -1of ammonium acetate buffer solution containing 0.1% formic acid. Mass spectrometer was operated in multiple reaction monitoring mode with positive electrospray ionization at m/z 246.2→97.2 for dezocine and m/z 409.2→228.0 for tamsulosin, respectively. Results: The method showed good linearity within the concentration range of 0.100-50.0 ng·mL-1for dezocine in plasma. The intra- and inter-batch precision of dezocine meet the criterias of Chinese Pharmacopoeia Appendix. The method was successfully applied to the pilot study of absoulte bioavailability of dezocine oral liquid. Conclusion: An accurate, simple and reliable HPLC-MS/MS method was developed. The pilot study result showed that the absolute bioavailability of dezocine oral liquid was 5.3%.%目的:建立快速测定人血浆中地佐辛浓度的HPLC-MS/MS方法,用于地佐辛口服液的绝对生物利用度预实验研究.方法:以坦洛新为内标,血浆经乙腈沉淀后进行HPLC-MS/MS分析.色谱柱:Aglient SB-C18column(2.1 mm×50 mm,3.5 μm),流动相为5 mmol·L-1醋酸铵(含0.1%甲酸)-乙腈(65:35,v/v).地佐辛和内标在多反应监测正离子模式下的离子对分别为m/z 246.2→97.2和409.2→228.0.结果:地佐辛在0.100~50.0 ng·mL-1范围内线性关系良好,检测方法的批内和批间精密度和准确度符合中国药典附录的相关要求,方法被成功应用于地佐辛口服液的人体绝对生物利用度预实验研究.结论:建立的HPLC-MS/MS法可以快速测定血浆中地佐辛的浓度;预实验结果显示地佐辛口服液的人体绝对生物利用度为5.3%.
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