甲磺酸帕珠沙星胶囊人体绝对生物利用度研究

Absolute bioavailability of pazufloxacin mesilate capsule in healthy Chinese subjects

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 develop an HPLC method for the absolute bioavailability of pazufloxacin mesilate capsule in healthy Chinese subjects. Methods： 24 healthy male volunteers were enrolled in this study. Volunteers were divided into two groups and administered capsule and injection in cross-over randomized way. Determined the pazufloxacin concentration with HPLC method and calculated the pharmaokinetics parameters with Win Nonlin program to evaluated the absolute bioavailability of pazufloxacin capsule. Results： The pharmacokinetic parameters following single oral dose of 300 mg pazufloxacin capsule and injection were as follows： the mean of Tmaxwere（ 0. 60 ± 0. 23） and（ 0. 50 ± 0. 00） h; the mean of Cmaxwere（ 5. 09 ± 1. 75） and（ 6. 92 ± 3. 13） μg·mL^（-1）; the mean of AUC（ 0-t）were（ 11. 24 ± 3. 45） and（ 11. 63 ± 3. 77） μg·mL^（-1）·h; the mean of AUC（ 0-∞）were（ 11. 58 ±3. 44） and（ 11. 97 ± 3. 77） μg·mL^（-1）·h; the mean of t1/2was（ 2. 37 ± 0. 67） and（ 2. 45 ± 0. 82） h. Conclusion：The absolute bioavailability was 97. 2%.