摘要
目的:研究单硝酸异山梨酯滴丸的人体相对生物利用度和生物等效性。方法:健康志愿者18名,随机双交叉单剂量口服单硝酸异山梨酯滴丸(试验制剂)和胶囊(参比制剂),剂量分别为40mg,剂间间隔为1周。分别于服药后36h内多点抽取静脉血;用高效液相色谱法测定血浆中单硝酸异山梨酯的浓度。用DAS药动学程序计算相对生物利用度并评价2种制剂生物等效性。AUC(0-36),AUC(0-∞)和Cmax经方差分析和双单侧t检验,tmax进行秩和检验。结果:单剂量口服单硝酸异山梨酯试验和参比制剂后,血浆单硝酸异山梨酯的Cmax分别为(453.2±67.4)μg.L-1和(434.3±63.2)μg.L-1;tmax分别为(0.60±0.13)h和(0.69±0.14)h;AUC(0-36)分别为(3013.7±576.3)μg.h.L-1和(2974.2±754.4)μg.h.L-1;AUC(0-∞)分别为(3156.0±582.8)μg.h.L-1和(3161.1±766.5)μg.h.L-1。AUC(0-36)、AUC(0-∞)、Cmax的90%可信区间分别为95.8%～108.9%,94.8%～106.6%和100.5%～108.2%。试验与参比制剂的人体相对生物利用度为(103.4±16.9)%。结论:两制剂具有生物学等效性。
OBJECTIVE To study the relative bioavailability and bioequivalence of isosorbide mononitrate pills in healthy volunteers, METHODS A single oral dose （40 mg of test and reference formulation） were given to 18 healthy volunteers in a randomised crossover study. The concentrations of isosorbide mononitrate in plasma were determined by HPLC. The pharmaeokinetics parameters were calculated and the bioavailability and bioequivalence of two formulations were evaluated by DAS program. RESULTS After a single dose, the pharmacokinetics parameters for isosorbide mononitrate were as follows：Cmax（453. 2± 67. 4）μg·L^-1 and （434. 3±63. 2）μg·L^-1;tmax （0. 60±0. 13）h and （0. 69±0. 14） h; AUC（0-36） （3013.7±576. 3 ）μg·h·L^-1 and（2974. 2 μ754. 4）μg·h·L^-1; AUC（0-∞）（3156. 0±582. 8）μg·h·L^-1 and （3 161.1±766. 5）μg·h·L^-1 for tested and reference formulation respectively. The 90% confidential interval of AUC（0-36） ,AUC（0-∞） and Cmax of tested formulation were 95.8% - 108. 9%,94. 8% - 106. 6% and 100. 5% - 108. 2% respectively. The relative bioavailability was （103. 4±16. 9）%. CONCLUSlON The results of the statistic analysis showed that the two formulations were bioequivalent.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2009年第15期1292-1295,共4页
Chinese Journal of Hospital Pharmacy
关键词
单硝酸异山梨酯
滴丸
药动学
生物等效性
高效液相色谱法
isosorbide mononitrate
pills
pharmacokinetics
bioequivalence
high performance liquid chromatography
