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本文报道国产洛美沙星在正常志愿者中的药物动力学研究结果。8名正常志愿者单次空腹口服洛美沙星片剂400mg后的体内过程符合二室模型,其吸收迅速,平均血药峰浓度为4.13±1.20mg/L,于给药后1.26±1.09h到达,其消除半衰期(T1/β)为6,78±0.81h。给药量的59.9±7.3%和67.0±6.6%分别于服药后24h和72h内自尿中排出,尿药峰浓度平均为391±187mg/L。正常志愿者单次空腹口服国产片剂及胶囊400mg后的体内过程与进口胶囊相仿,主要药代参数亦相近,相对生物利用度相仿。正常志愿者单次空腹口服国产洛美沙星片剂100~800mg剂量后均能很好耐受。根据研究结果,对洛美沙星的给药方案提出建议。
This article reports the results of pharmacokinetic studies of domestic Lomefloxacin in normal volunteers. 8 normal volunteers single oral fasting oral lomefloxacin tablets 400mg in vivo process in line with two-compartment model, its rapid absorption, the average peak plasma concentration of 4.13 ± 1.20mg / L, after administration of 1. 26 ± 1.09h, the elimination half-life (T1 / β) was 6,78 ± 0.81h. The dosage of 59.9 ± 7.3% and 67.0 ± 6.6% were respectively excreted from the urine within 24h and 72h after taking the medication. The peak urinary concentration was 391 ± 187mg / L. The normal volunteers single oral fasting oral domestic capsules and capsules 400mg in vivo process and import capsules similar to the main drug parameters are similar, the relative bioavailability similar. Normal volunteers single oral fasting domestic lomefloxacin tablets 100 ~ 800mg dose can be well tolerated. According to the results of the study, the proposed regimen of lomefloxacin was proposed.