摘要
目的 :建立内皮素受体拮抗剂CPU 0 2 13在小鼠和大鼠血清中的检测方法 ,测定单次静脉注射(iv)CPU 0 2 1380mg·kg-1后在小鼠和大鼠体内的药代动力学。方法 :用HPLC测定小鼠和大鼠血清中的药物浓度 ,3P97程序拟合药动学参数。结果 :CPU 0 2 13在 0 .4～ 2 0 0 μg·L-1的范围内呈良好的线性关系 (r =0 .9998) ,最低检测浓度为 35 μg·L-1。日内差小于 2 .7% ,日间差小于 6 .3% ,方法回收率大于 95 .9%。CPU 0 2 13在小鼠和大鼠体内的药 时数据均符合二室模型 ,消除半衰期分别为 83.0±1.8min和 96 .6± 11.5min。结论 :该方法灵敏、简单 ,专属性强 ,重现性好。单次ivCPU 0 2 1380mg·kg-1后 ,在小鼠和大鼠体内的药代动力学未见种属差异性。
AIM: To establish a method in determination of CPU-0213 in se rum of mice and rats and to investigate the pharmacokinetics parameters after a single injection at the dose of 80 mg·kg -1. METHODS: The concentration of CPU-0213 in serum was assayed by HPLC and the pharmacokine tics parameters were calculated by the program of 3P97. RESULTS: The linearity of CPU-0213 ranged from 0.4 to 200 mg·L -1 (r= 0.9998) and the limit of quantity was 35 μg·L -1. Th e RSD of intra-day was less than 2.7% and that of inter-day was less than 6.3%. The recovery was more than 95.9%. The disposition was conformed to a two-compartment model. The T 1/2β of CPU-0213 in mice and rats were 83.0± 1.8 and 96.6± 11.5 min, respectively. CONCLUSION: The study provides a simple, stable and special method for determining o f concentrations of CPU-0213 in serum of mice and rats. After intravenously inj ection of CPU-0213 at a single dose, there is no significantly difference in th e pharmacokinetics patterns of CPU-0213 in mice and rats.
出处
《中国临床药理学与治疗学》
CAS
CSCD
2004年第12期1357-1360,共4页
Chinese Journal of Clinical Pharmacology and Therapeutics
基金
国家自然科学基金重点项目资助 (№ 3 0 2 3 0 170
№ 3 0 1710 78)
