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目的:研究甲磺酸帕珠沙星片在健康志愿者体内单次和多次给药的药动学特征。方法:健康受试者34例,分成4组,其中单次给药剂量组3组,多次给药剂量组1组。单次剂量组在分别给予甲磺酸帕珠沙星片200,400,800mg,多剂量组在给予甲磺酸帕珠沙星片200mg后,采用HPLC测定血药浓度,DAS2.0软件进行数据处理,求算药动学参数。结果:受试者单剂量口服甲磺酸帕珠沙星片后,Cmax分别为(6.1±1.1),(10.9±3.3),(20.5±5.2)mg.L-1;AUC0-∞分别为(13.7±2.3),(28.9±5.7),(71.3±15.7)mg.h.L-1;Tmax分别为(0.6±0.3),(0.8±0.5),(0.9±0.4)h;t1/2分别为(1.8±0.4),(1.90±0.30),(1.9±0.2)h;Cmax、AUC0-t随剂量的增加而成比例的增大。受试者多次口服甲磺酸帕珠沙星片200mg达稳态后:Cmax为(16.8±4.0)mg.L-1;Cmin为(0.13±0.06)mg.L-1,AUCss为(40.6±7.5)mg.h.L-1;tmax为(0.8±0.6)h;t1/2为(2.0±0.3)h。结论:在本研究剂量范围内,甲磺酸帕珠沙星片在国人体内过程符合一级消除二室模型,具有线性药动学特征,连续服用无蓄积作用。
OBJECTIVE: To study the pharmacokinetic characteristics of pazufloxacin mesylate tablets administered in single and multiple doses in healthy volunteers. Methods: 34 healthy subjects were divided into 4 groups, including 3 single dose groups and 1 repeated dose group. Single dose group were given pazufloxacin mesylate tablets 200,400,800mg, multiple dose group was given pazufloxacin mesylate tablets 200mg, the determination of plasma concentration by HPLC, DAS2.0 software for data processing, seeking Calculate pharmacokinetic parameters. Results: After oral administration of pazufloxacin mesylate tablets, the C max were (6.1 ± 1.1), (10.9 ± 3.3) and (20.5 ± 5.2) mg.L-1, respectively; AUC0-∞ were Tmax were (0.6 ± 0.3), (0.8 ± 0.5) and (0.9 ± 0.4) h respectively; t1 / 2 were (13.7 ± 2.3), (28.9 ± 5.7) and (71.3 ± 15.7) mg.hL- 1.8 ± 0.4), (1.90 ± 0.30) and (1.9 ± 0.2) h respectively. Cmax and AUC0-t increased proportionally with the increase of dose. After oral administration of 200 mg of pazufloxacin mesylate tablets for several times to steady state, the Cmax was (16.8 ± 4.0) mg.L-1; the Cmin was (0.13 ± 0.06) mg.L-1; the AUCss was ± 7.5) mg.hL-1; tmax was (0.8 ± 0.6) h; t1 / 2 was (2.0 ± 0.3) h. CONCLUSION: In the dose range of this study, pazufloxacin mesylate in the body of a Chinese patient fulfilled the first-order elimination two-compartment model with linear pharmacokinetic characteristics and no accumulation after continuous administration.