摘要
目的制备单硝酸异山梨酯控释片,考察其在Beagle犬体内的药动学及相对生物利用度。方法采用单室渗透泵技术制备控释片,采用两制剂、双周期交叉试验设计,气相色谱-电子捕获法对犬体内血药浓度进行分析;DAS 2.0软件计算药动学参数。结果受试犬服用自制控释片和市售缓释片(参比制剂)后药时曲线相似,主要药动学参数分别为:t1/2(5.083±1.524)和(4.866±1.361)h,Cm ax(0.617±0.213)和(0.753±0.228)μg/m l,Tm ax(2.250±0.880)和(2.722±0.935)h,AUC(0-t)(5.086±0.832)和(4.997±0.916)μg.h/m l,AUC(0∞-)(5.254±0.754)和(5.258±1.032)μg.h/m l,相对生物利用度为(101.0±17.7)%。结论单硝酸异山梨酯控释片与市售缓释片主要药动学参数无显著性差异,两制剂具有生物等效性。
Objective To prepare isosorbide mononitrate controlled release tablets and study their pharmacokinetics and relative bioavailability in Beagle dogs.Methods Isosorbide mononitrate controlled release tablets were prepared by monolithic osmotic pump technique.These tablets and isosorbide mononitrate sustained release tablets（reference formulation） were given orally to Beagle dogs by a two-crossover design.Drug concentrations in plasma were determined by gas chromatography-electron capture detector and the pharmacokinetic parameters of isosorbide mononitrate were analyzed by DAS 2.0.Results The main pharmacokinetic parameters of the self-made controlled release tablets and reference formulation were as follows：t1/2 was（5.083±1.524）and（4.866±1.361）h,Cmax was（0.617±0.213）and（0.753±0.228）μg/ml,Tmax was（2.250±0.880） and（2.722±0.935） h;AUC（0-t） was（5.086±0.832）and（4.997±0.916）μg·h/ml,AUC（0-∞） was（5.254±0.754）and（5.258±1.032）μg·h/ml.The relative bioavailability was（101.0±17.7）%.Conclusion Compared with the sustained release tablets,isosorbide mononitrate controlled release tablets have a similar pharmacokinetic profile and the two formulations are bioequivalent.
出处
《解放军药学学报》
CAS
2011年第1期11-13,16,共4页
Pharmaceutical Journal of Chinese People's Liberation Army
关键词
单硝酸异山梨酯控释片
气相色谱-电子捕获法
药动学
生物利用度
isosorbide mononitrate controlled release tablets
gas chromatography-electron capture detector
pharmacokinetics
relative bioavailability
