氟罗沙星临床药物动力学研究

Studies on clinical pharmacokinetics of domestic fleroxacin

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。

The clinical pharmacokinetics of domestic fleroxacin in healthy volunteers were studied. All drug concentrations in serum and urine were assayed by HPLC and bioassay method. The experimental data obtained in 8 healthy volunteers after a single 400mg oral dose of fleroxacin tablet and capsule could be fitted to a two compartment model. The mean maximum serum drug concentrations being 6.52±1.20mg/L (domestic tablet) and 6.74±2.31mg/L (domestic capsule), reached at 0.91±0.43 and 1.20±0.67h after the drug administration respectively. Their elimination half lives (T 1/2β ) were 11.07±1.73 and 10.81±2.00h; AUC were 82.17±17.79 and 89.08±18.89h·mg/L. 68.95%±6.29% and 77.23%±6.76% of the given dosage were excreted in urine with 72h respectively. Mean urinary drug concentrations exceeded 140mg/L within 24 hours after the drug administration. The pharmacokinetic parameters and relative bioavailability of domestic tablet and capsule after a single 400mg dose were similar with that of imported tablet. According to the results in this paper, a scheme of dosage regimen of fleroxacin was suggested.