左氧氟沙星片剂绝对生物利用度研究

目的 在中国健康志愿者中进行左氧氟沙星(可乐必妥)500mg片剂药代动力学研究,并以左氧氟沙星500mg(100ml)注射液为对照,研究口服片剂的绝对生物利用度.方法 10名受试者分别单剂空腹口服左氧氟沙星500mg片剂和单次静脉滴注500mg(100ml)注射液.以高效液相色谱(HPLC)-荧光法测定血、尿样中左氧氟沙星药物浓度.结果 受试者单剂空腹口服左氧氟沙星500mg片剂后平均C_(max)实测值为(6.20±2.51)mg/L,T_(max)为(0.91±0.54)h,t_(1/2)为(6.71±0.88)h,AUC_(0-∞)为(41.88±5.72)mg·h/L,24h内尿中平均累积排出率为(69.40±7.27)%,其与注射液相比绝对生物利用度几何均数比为107.5%(以AUC_(0-∞)计),90%可信区间为(97.72～118.25)%.结论 左氧氟沙星500mg片剂单次口服给药后吸收迅速,且吸收完全.提示临床可以每日一次,500mg顿服,用于左氧氟沙星先静脉给药,继以口服的序贯疗法.

Absolute bioavailability of levofloxacin tablet in healthy Chinese male subjects

Objective To investigate the pharmacokinetics and absolute bioavailability of levofloxacin tablet in healthy Chinese subjects in order to provide rationale for developing safe and effective clinical dosage regimen in Chinese patients. Methods Ten subjects took single oral dose and intravenous of 500mg( 100ml) levofloxacin, respectively. The concentrations of levofloxacin in plasma and urine were determined by high performance liquid chromatogram-fluorescence method. Results The pharmacokinetic parameters following single oral dose of 500mg levofloxacin tablet were as follows. The mean of C_(max) was (6.20±2.51) mg/L. The mean of T_(max) was (0.91±0.54) h. The mean of t_(1/2) was (6.71±0.88) h. The mean of AUC_(0-∞) was (41.88±5.72) mg·h/L. The mean of accumulative urinary excretion with 24 hours post dosing was (69.40±7.27) %. The absolute bioavailability was (108.20±12.68) %. Conclusion The results indicate that levofloxacin was absorbed fast and completely. The preparations of tablet and intravenous of levofloxacin were equivalent.