定尔心缓释片的药物动力学和生物利用度  

THE PHARMACOKINETICS AND RELATIVE BIOAVAILABILITY OF DILTIAZEM SUSTAINEDRELEASE TABLETS

作　　者：洪蕾[1] 陆继红[1] 王曼丽[1] 郭红英[1] 

机构地区：[1]北京友谊医院临床药理研究室

出　　处：《中国新药杂志》1998年第3期224-226,共3页Chinese Journal of New Drugs

摘　　要：目的：以美国ＭａｒｉｏｎＭｅｒｅｌＤｏｗ．Ｉｎｃ．的地尔硫卓缓释胶囊（ＣａｒｄｉｚｅｍＳＲ９０ｍｇ）为对照，考察印度Ｔｏｒｒｅｎｔ公司生产的定尔心缓释片（ＤｉｌｚｅｍＳＲ９０ｍｇ）的相对生物利用度和药代动力学参数。方法：采用自身对照法进行单剂量和多剂量给药，血样经预处理后采用高效液相色谱法测定浓度。结果：用ＣＲＦ１程序处理，定尔心缓释片的ｔ１／２（Ｋａ）＝０．５７ｈ，ｔ１／２（Ｋｅ）＝４．０１ｈ，Ｔｍａｘ＝２．２７ｈ，Ｃｍａｘ＝５０．６１ｎｇ／ｍｌ，ＡＵＣ＝４０７．１９ｎｇ·ｈ／ｍｌ，相对生物利用度Ｆ＝９０．２％，多剂量给药达稳态波动系数为０．７１。结论：定尔心缓释片的相对生物利用度符合《新药（西药）临床研究指导原则汇编》OBJECTIVE:DiltiazemSR capsules(MMD)were adopted as reference standard in study the relative bioavalability and pharmacokinetics of diltiazem sustainedrelease tablets(DilzemSR of Torrent).METHODS:A crossover selfcontrol study of single and multiple dose was conducted on 8 healthy volunteers.Blood drug concentrations were determined by HPLC.RESULTS:The pharmacokinetic parameters of diltiazem SR tablets(Torrent)were:t1/2(Ka)=0.57 h,t1/2(Ka)=4.01 h,Tmax=2.27 h,Cmax=50.61 ng/ml,AUC=407.19 ng·h/ml and a relative bioavlaibility of 90.2% was obtained.The fluctuation confficient for steady state of multidoses was 0.71.CONCLUSION:The bioavaliability data of DilzemSR 90 mg tablets obtained in the study are in compliance with the standard required by Chinese health authority.

关 键 词：地尔硫卓 生物利用度 高效液相色谱 药代动力学 

分 类 号：R972[医药卫生—药品]