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氟罗沙星在健康志愿者中进行药物动力学研究。全部血、尿药物浓度以高效液相色谱法和微生物法测定。8名志愿者分别单次空腹口服氟罗沙星片剂和胶囊剂400mg后的体内过程符合二室模型,Cmax分别为6.52±1.20和6.74±2.31mg/L,并分别于给药后0.91±0.43和1.20±0.67h到达;其消除半衰期分别为11.07±1.73和10.81±2.00h;AUC分别为82.17±17.79和89.08±18.89hmg/L;给药量的68.95%±6.29%和77.23%±6.76%分别于给药后72h内自尿中排出。给药后24h内平均尿药浓度均超过140mg/L。健康志愿者单次空腹口服国产氟罗沙星片剂和胶囊剂400mg后的药动学参数与进口片剂者相仿,平均相对生物利用度相近。根据研究结果,对氟罗沙星的给药方案提出了建议
Fleroxacin performs pharmacokinetic studies in healthy volunteers. All blood, urine drug concentration by high performance liquid chromatography and microbiological determination. Eight volunteers in a single fasting oral fleroxacin tablets and capsules 400mg in vivo process in line with two-compartment model, Cmax were 6.52 ± 1.20 and 6.74 ± 2.31mg / L, respectively, and were 0.91 ± 0.43 and 1.20 ± 0.67 h arrived after administration; the elimination half-lives were 11.07 ± 1.73 and 10.81 ± 2.00 h, respectively; the AUC were 82.17 ± 17 respectively. 79 and 89.08 ± 18.89hmg / L, respectively; 68.95% ± 6.29% and 77.23% ± 6.76% of the dose were respectively excreted from the urine within 72h after administration. Within 24 hours after administration, the average urine concentration was more than 140mg / L. Pharmacokinetic parameters of healthy volunteers after a single fasting oral administration of fleroxacin tablets and capsules 400mg and imported tablets were similar, the average relative bioavailability similar. According to the results of the study, the proposed regimen of fleroxacin is proposed