摘要
目的:比较苦参碱缓释片、苦参碱普通胶囊和苦参碱注射液的药代动力学及生物利用度。方法:对杂种犬进行单剂量及多剂量试验,采用反相液相色谱法测定血药浓度,对苦参碱的三种剂型进行药物动力学及生物利用度研究。结果:苦参碱普通胶囊tmax为(85±12)min,cmax为(6.360±0.215)μg/ml,缓释片的tmax为300min,cmax为(5.088±0.490)μg/ml,注射剂的tmax为10min,cmax为(6.500±0.404)μg/ml。缓释片相对于普通胶囊之相对生物利用度为(153.7±9.4)%,相对于注射剂的绝对生物利用度为(73.5±14.2)%。体内外相关性显著(r=0.9812,P<0.01)。结论:苦参碱缓释片释药迟缓,达峰时间长,血药浓度变化平缓,达到设计要求。
Objective:To compare the pharmacokinetics and relative bioavailability between matrine sustained release tablet,matrine conventional capsule and matrine injection. Methods: Dogs were given single oral dose and multiple doses of matrine sustained release tablet, capsule or injection in a randomized crossover way. Matrine concentrations in dog plasma were determined by RP-HPLC method. Results: The results showed that the t max and c max were 300 min and (5.088±0.490) μg/ml for matrine sustained release tablet, (85±12) min and (6.360±0.215) μg/ml for the conventional capsule, and 10 min and (6.500±0.404) μg/ml for the injection. The relative bioavailability of the sustained release tablet was (153.7±9.4)% compared with that of the conventional capsule; the absolute bioavailability of the sustained release tablet was (73.5±14.2)% compared with that of the injecetion. The in vivo absorption rate of the sustained release tablet was significantly correlated with the in vitro release rate(r=0.981 2,P<0.01). Conclusion: Matrine sustained release tablet, with sustained release, longer time for reaching peak, and smoothly changing concentration,can meet the requirements for drug design.
出处
《第二军医大学学报》
CAS
CSCD
北大核心
2005年第6期681-683,共3页
Academic Journal of Second Military Medical University
关键词
苦参碱
缓释片
胶囊
注射液
药代动力学
生物利用度
matrine
sustained release tablet
capsules injection
pharmacokinetics
biological availability
