论文部分内容阅读
本文报道了柱晶白霉素(LM)胃溶片的人体药代动力学研究结果,并对肠溶片口服后的血、尿中药物浓度作了动态观察。血、尿药物浓度用微生物杯碟法测定。健康志愿者分别口服柱晶白霉素胃溶片和肠溶片40万单位(相当于267mg)后,体内药物转运过程均符合一室开放模型。两种制剂的血药浓度达峰时间、峰浓度分别为0.5小时,0.94μg/ml和5小时,0.147μg/ml。其中胃溶片口服后的T(1/2)Ka和T(1/2)Ke分别为0.13和0.72小时,而MRT为1.22小时,MAT为0.18小时。 口服LM肠溶片多剂量组,从第2天起,血药峰浓度波动于0.42～0.68μg/ml,显著高于单剂量组的峰浓度,其谷浓度则波动于0.05～0.34μg /ml。 LM的肾排泄率极低,口服LM的胃溶片和肠溶片后24小时内,从尿中排出的药量仅占给药量的7.64‰和11.54‰。口服LM胃溶片后的C-T曲线出现双峰,可能与肠肝循环有关,在计算药动学参数时应予注意。
In this paper, we report the results of human pharmacokinetics study of levamisole (LM) gastric-dissolving tablets and observe the blood and urine concentrations of the enteric-coated tablets after oral administration. Blood, urine drug concentration using Microbiology cup dish method. Healthy volunteers were orally oral levamisole enteric-coated tablets and enteric-coated tablets 400000 units (equivalent to 267mg), the body of the drug transport process are in line with a room open model. The peak plasma concentrations of the two formulations were 0.5 h, 0.94 g / ml and 5 h, respectively, and the peak concentrations were 0.147 g / ml. The T (1/2) Ka and T (1/2) Ke after oral administration of Fu stomach tablet were 0.13 and 0.72 hours respectively, while MRT was 1.22 hours and MAT was 0.18 hours. The oral administration of LM enteric-coated multi-dose group, from the second day, peak blood concentration fluctuations in the 0.42 ~ 0.68μg / ml, significantly higher than the single-dose group peak concentration, the valley concentration fluctuations of 0.05 ~ 0.34μg / ml . LM renal excretion rate is very low, oral administration of LM stomach tablets and enteric-coated tablets within 24 hours after the discharge from the urine dose accounted for only the amount of 7.64 ‰ and 11.54 ‰. C-T curve of oral LM gastric smear appeared double peaks, which may be related to enterohepatic circulation, should be noted in the calculation of pharmacokinetic parameters.