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目的 :建立人血浆中螺旋霉素 (SPM )浓度的测定方法及进行人体药代动力学的研究。方法 :采用高效液相色谱法 ,色谱柱 :phenomenex C1 8色谱柱 (5 μm,2 5 0 mm× 4 .6 mm) ,以乙腈∶磷酸二氢钾缓冲液(0 .0 5 mol/ L,p H为 2 .86 ) =5∶ 18(v/ v)为流动相 ,以乳酸司帕沙星为内标 ,流速 1.0 ml/ min,柱温为 2 0℃ ,紫外检测波长 2 32 nm,用螺旋霉素与内标的峰面积比进行定量。线性范围 2 5～ 32 0 0μg/ L ,最低检测浓度为2 0μg/ L ,对 18名健康受试者单次口服 4 5 0万 u螺旋霉素片剂后的药代动力学进行研究。结果 :18名健康受试者的血药浓度数据经 3p97拟合 ,符合血管外给药一室模型 ,AU C0～ t为 (44 72 .0± 6 74 .3) μg· h/ L,Cmax为(16 14 .4± 2 98.2 ) μg/ L,Tmax为 (2 .75± 0 .31) h,T1 /2 ke为 (2 .6 4± 0 .70 ) h。结论 :该方法简便 ,稳定性好 ,噪音小 ,灵敏度和准确度高 ,能够满足人体内低浓度药物的测定及药代动力学研究的要求。
Objective: To establish a method for the determination of spiramycin (SPM) in human plasma and to study its pharmacokinetics. METHODS: High performance liquid chromatography (HPLC) was performed on a Phenomenex C1 8 column (5 μm, 250 mm × 4.6 mm) with acetonitrile: potassium dihydrogen phosphate buffer (0.05 mol / L, p H = 2.86) = 5:18 (v / v) as mobile phase, sparfloxacin lactate as internal standard, the flow rate of 1.0 ml / min, the column temperature of 20 ℃, UV detection wavelength of 2 32 nm, Spiramycin and internal standard peak area ratio for quantification. The linear range of 25 ~ 32 0 0μg / L, the lowest detection concentration of 20μg / L, 18 healthy subjects in a single oral 45 million u spiramycin tablet pharmacokinetics study. Results: The blood concentration data of 18 healthy subjects were fitted by 3p97, which was consistent with the one-compartment model of extravascular administration. The AU C0-t was (44 72.0 ± 6 74.3) μg · h / L, Cmax (16.14 ± 2 98.2) μg / L, Tmax was (2.75 ± 0.31) h and T1 / 2 ke was (2.64 ± 0.70) h. Conclusion: The method is simple, stable, low noise, high sensitivity and accuracy, and can meet the requirements of the determination of low concentrations of drugs and pharmacokinetics in the human body.