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八名男性健康志愿者交叉口服甲磺酸培氟沙星(甲氟哌酸)片剂和原粉水溶液各400mg,进行药代动力学试验。血浆和尿标本同时用微生物法和HPLC法进行测定,药代动力学数据用3P87程序处理。两种剂型吸收均有迟滞时间,但吸收较快。用微生物法和HPLC法测得片剂的峰浓度分别为5.78(±0.39)和6.03(±0.80)mg/l;达峰浓度时间分别为1.37(±0.24)和1.40(±0.80)h;吸收迟滞时间(tlag)分别为0.28(±0.17)和0.27(±0.04)h。口服水溶液的峰浓度与片剂相似,但达峰时间明显短于片剂,与水溶液相比,片剂吸收完全。口服两种剂型的药时曲线均符合二室模型。表观分布容积大于总体液,不同方法测得V/F值为46.60(±3.27)—52.31(±8.98)1,提示可在组织中较好地分布。该药消除较慢,消除速率常数较小,不同方法测得β值为0.0449(±0.0034)—0.0529(±0.0020)h~(-1),消除半衰期较文献报道的值长,不同方法测得为13.80(±0.68)—16.09(±1.27)h,如按文献报道的给药方法,每12h给药400mg,应注意蓄积倾向。该药原型尿中回收率较低,片剂和水溶液分别为给药剂量的23.48(±7.04)和18.53(±3.20)%,表明非肾消除为其主要消除途径。用微生物法测得两种剂型尿中回收剂量远高于HPLC法。片剂和水溶液分别为给药剂量的46.04(±7.02)和43.51(±6.99)%,此为原型药物和活性代谢产物氟哌酸的总量。尿中药物浓度高且维持时间长,利于尿路感染的治疗。
Eight male healthy volunteers were given oral administration of 400 mg of pefloxacin mesylate (mefloxacin) tablets and each of the original powder aqueous solutions for pharmacokinetic tests. Plasma and urine samples were determined by both microbial and HPLC methods. Pharmacokinetic data were processed using the 3P87 program. Both formulations have lag time absorption, but faster absorption. The peak concentrations of the tablets were 5.78 (± 0.39) and 6.03 (± 0.80) mg / l, respectively. The peak time was 1.37 (± 0.24) and 1.40 (± 0.80) h, respectively. The lag time (tlag) was 0.28 (± 0.17) and 0.27 (± 0.04) h, respectively. The peak concentration of oral aqueous solution is similar to that of tablets, but the peak time is significantly shorter than that of tablets, and tablets are completely absorbed compared to aqueous solutions. Oral two formulations of the drug-time curve are in line with the two-compartment model. The apparent volume of distribution was larger than that of total fluid. The V / F values measured by different methods were 46.60 (± 3.27) -52.31 (± 8.98) 1, suggesting better distribution in tissues. The elimination of this drug is slower and the elimination rate constant is smaller. The β value measured by different methods is 0.0449 (± 0.0034) -0.0529 (± 0.0020) h ~ (-1), the elimination half-life is longer than the reported value in the literature. Is 13.80 (± 0.68) -16.09 (± 1.27) h. According to the method of drug administration reported in the literature, 400 mg should be administered every 12 h, and the tendency of accumulation should be noticed. The recovery rate of the prototype urine was lower, and the dosage of the tablets and the aqueous solution were 23.48 (± 7.04) and 18.53 (± 3.20)% respectively, indicating that non-renal elimination was the main elimination route. Microbial test measured two dosage forms of urine recovery is much higher than the HPLC method. The tablets and aqueous solutions were 46.04 (± 7.02) and 43.51 (± 6.99)%, respectively, of the administered dose, which is the total amount of the prototype drug and the active metabolite norfloxacin. High concentrations of urinary drugs and maintain a long time, which will help the treatment of urinary tract infection.