摘要
目的:采用药效动力学方法评价复方丹参骨架缓释片(CDSRT)的缓释作用。方法:以市售复方丹参片(CDT)为对照,分别给予正常大鼠CDT、CDSRT(折算生药材2911.14mg/kg),于给药后0.25、0.5、0.75、1、2、4、8、12h制备含药血清,并将含药血清作用于心肌细胞,考察CDT和CDSRT对缺氧/复氧心肌细胞损伤的保护作用,评价CDSRT的缓释作用。结果:与模型组比较,CDT4、8h的含药血清和CDSRT2、4、8、12h的含药血清对缺氧/复氧损伤心肌细胞均有促增殖作用;CDT和CDSRT的效应半衰期t1/2(ka)分别为2.655和0.719h,效应达峰时间tmax分别为5.213和2.957h,效应消除半衰期t1/2(ke)分别为4.953和10.166h。与CDT相比,CDSRT效应半衰期和效应达峰时间短,消除速率低。结论:复方丹参骨架缓释片效应消除半衰期长,具有一定的缓释作用。药效动力学方法可作为其缓释作用的评价方法之一。
AIM：To evaluate the sustained-release effect on Compound Danshen Skeleton Sustained-Release Tablet （CDSRT） by pharmacodynamics method. METHODS： By reference to Compound Danshen Tablet（CDT）, Sprague-Dawley rats had been administrated with CDT and CDSRT with the content of crude drugs 2911.14 mg/kg. The medicated serum of CDT and CDSRT were prepared at the time of 0.25,0.5,0.75,1,2,4,8,12 h after single oral administration. The medicated serums were added to myocardial cells respectively. The protective effects of CDT and CDSRT on hypoxia/reoxygenation and the sustained-release effect of CDSRT were evaluated. RESULTS：Compared with the H/R model group, the medicated serum of CDT 4,8 h and CDSRT 2,4,8,12 h had apparent protective effects against proliferation inhibition caused by hypoxia/reoxygenation（H/R） induced injury in myocardial cells. The present half-life t1/2（ka） of CDT and CDSRT were 2.655 h and 0.719 h. The peak times of effective action were 5.213 h and 2.957 h. And the elimination half-life t1/2（ke） were 4.953 h and 10.166 h respectively. Compared with CDT, CDSRT had a higher speed of the effect present and the peak time of effective action and a lower speed of sustained-release.CONCLUSION： CDSRT has a certain sustained-release function as t1/2（ke） longer than that of CDT. Pharmacodynamics method is a feasible method for the evaluation of CDSRT sustained-release effect.
出处
《中国临床药理学与治疗学》
CAS
CSCD
2010年第7期794-798,共5页
Chinese Journal of Clinical Pharmacology and Therapeutics
基金
国家十一五支撑计划资助项目(2006BAI09B08-01)
关键词
复方丹参骨架缓释片
药效动力学
缓释作用
Compound Danshen Skeleton Sustained Release Tablet
Pharmacodynamics
Sustained-release function
