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目的:建立HPLC法测定人体血浆中帕珠沙星浓度的方法,进行甲磺酸帕珠沙星胶囊的人体生物利用度研究。方法:纳入24例健康男性受试者进行甲磺酸帕珠沙星胶囊人体生物利用度研究,受试者随机分为两组,前后交叉给予受试制剂甲磺酸帕珠沙星胶囊与参比制剂甲磺酸帕珠沙星注射液,评价受试制剂的生物利用度。采用HPLC法测定帕珠沙星浓度,用Win Nonlin药动学软件计算药动学参数和生物利用度。结果:健康受试者单次口服300 mg甲磺酸帕珠沙星胶囊剂后,达峰时间分别为(0.60±0.23)和(0.50±0.00)h;峰浓度分别为(5.09±1.75)和(6.92±3.13)μg·mL~(-1);AUC(0-t)分别为(11.24±3.45)和(11.63±3.77)μg·mL~(-1)·h;AUC(0-∞)分别为(11.58±3.44)和(11.97±3.77)μg·mL~(-1)·h;t1/2分别为(2.37±0.67)和(2.45±0.82)h。结论:以AUC0-t计甲磺酸帕珠沙星胶囊的绝对生物利用度为97.2%。
OBJECTIVE: To establish a HPLC method for the determination of pazufloxacin in human plasma and to study the bioavailability of pazufloxacin mesylate capsules. Methods: Twenty-four healthy male subjects were enrolled in the study of bioavailability of pazufloxacin mesylate capsules. The subjects were randomly divided into two groups. The pazufloxacin mesylate capsules Than the preparation of pazufloxacin mesylate injection, evaluate the bioavailability of the test preparation. The concentration of pazufloxacin was determined by HPLC and the pharmacokinetic parameters and bioavailability were calculated by Win Nonlin pharmacokinetic software. Results: In healthy subjects, the peak time was (0.60 ± 0.23) and (0.50 ± 0.00) h respectively after single oral administration of 300 mg pazufloxacin mesylate capsules; the peak concentrations were (5.09 ± 1.75) and (6.92 ± 3.13) μg · mL -1, AUC (0-t) were (11.24 ± 3.45) and (11.63 ± 3.77) μg · mL -1 (11.58 ± 3.44) and (11.97 ± 3.77) μg · mL -1 · h respectively, and the values of t 1/2 were (2.37 ± 0.67) and (2.45 ± 0.82) h respectively. Conclusion: The absolute bioavailability of pazufloxacin mesylate with AUC0-t was 97.2%.