摘要
目的:研究健康Beagle犬口服吲达帕胺控释片的药动学和相对生物利用度。方法:采用两制剂、双周期交叉试验设计,用HPLC-MS法测定6只健康Beagle犬单次口服1.5 mg受试制剂(吲达帕胺控释片)和参比制剂(市售吲达帕胺缓释片)后血浆中吲达帕胺浓度,并绘制血药浓度-时间曲线;用统计分析软件计算药动学参数,进而计算相对生物利用度。结果:受试犬服用受试制剂和参比制剂后药时曲线相似,血浆中吲达帕胺的t1/2分别为(11.71±1.69)和(11.87±1.72)h;Cmax分别为(87.17±22.03)和(87.64±24.24)μg·L^-1;Tmax分别为(6.67±0.52)和(6.83±0.75)h;AUC0-48 h分别为(1 200.31±577.16)和(1 162.53±463.85)μg·h·L^-1;AUC0~∞分别为(1 276.73±619.22)和(1 250.20±507.63)μg·h·L^-1。以AUC0~48 h计算,受试制剂的相对生物利用度F为(101.0±17.7)%。结论:吲达帕胺控释片具有与市售缓释片相似的缓释效果,主要药动学参数无显著差异,两个制剂生物利用度接近。
Objective:To study the pharmacokinetics and relative bioavailability of indapamide controlled release tablets in healthy Beagle dogs.Methods:Indapamide controlled release tablets(test product) and indapamide sustained release tablets(reference product) were given orally to six healthy Beagle dogs by a two-crossover design.Indapamide concentrations in plasma were determined by HPLC-MS and the plasma concentration-time curves were plotted.The pharmacokinetic parameters and relative bioavailability were calculated and evaluated using statistic computer program.Results:The concentration-time curve of indapamide controlled release tablets was similar to that of indapamide sustained release tablets,and their t1/2 were(11.71±1.69) and(11.87±1.72) h,Cmax were(87.17±22.03) and(87.64±24.24) μg·L^-1,Tmax were(6.67±0.52) and(6.83±0.75) h,AUC0~48 h were(1 200.31±577.16) and(1 162.53±463.85) μg·h·L^-1,AUC0~∞ were(1 276.73±619.22) and(1 250.20±507.63) μg·h·L^-1,respectively.According to AUC0~48 h,the relative bioavailability of indapamide controlled release tablets was(101.0±17.7)%.Conclusion:Compared with the sustained release tablets,indapamide controlled release tablets have similar pharmacokinetic profile and bioavailability.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2010年第9期808-812,共5页
Chinese Journal of New Drugs