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目的 研究重组葡激酶 (r- SAK)静脉给药后在健康人体内的药代动力学。方法 9例健康成人每人给药 1 0 mg(先静脉推注 1 mg,2 m in内推完 ,余下 9mg30 min内推完 ) ,采血时间为开始给药后的 1、1 0、2 0、30、35、40、5 0、6 0、70、90、1 2 0、2 1 0和 2 70 min。以双夹心酶联免疫吸附法检测血药浓度。结果 中心室分布容积为 (4.45± 1 .6 2 ) L,药 -时曲线下面积(AUC0～ 2 70 )为 (89935± 1 32 2 8) min· ng/m l,药物总清除率为 (6 .30± 1 .0 5 ) L /h,T1 /2α(分布相半衰期 )为 (1 3.30± 2 .0 6 )min,T1 /2β(消除相半衰期 )为 (6 7.94± 2 1 .39) min。结论 r- SAK在健康人体内的药代动力学类型符合二室模型。建议临床给药方式为 1 0 mg r- SAK 30 min内静脉输注 ,必要时在第 1次给药结束后 30～ 6 0 min可再给 1 0 mg。
Objective To study the pharmacokinetics of recombinant staphylokinase (r-SAK) administered intravenously in healthy volunteers. Methods Nine healthy volunteers were given 10 mg per person (1 mg intravenous bolus and 2 min bolted within 9 min of the remaining 30 min). The blood sampling time was 1,1 0,2 0 after the start of administration 30, 35, 40, 50, 60, 70, 90, 120, 210 and 2 70 min. Double-sandwich enzyme-linked immunosorbent assay for plasma concentration. Results The volume of central compartment was (4.45 ± 1.62) L, the area under the drug-time curve (AUC0-270) was (89935 ± 1 3228) min · ng / ml and the total drug clearance was (1 3.30 ± 2.06) min, T1 / 2β (elimination phase half-life) was (6 7.94 ± 2.139) min. Conclusion The pharmacokinetics of r-SAK in healthy volunteers conform to the two-compartment model. Proposed clinical administration of 10 mg r-SAK intravenous infusion within 30 min, if necessary, after the first dose 30 ~ 60 min to give 10 mg.