高效液相色谱法测定复方吲哚美辛贴剂中沙丁胺醇兔体内的药动学

Study on the pharmacokinetics of salbutamol in indomethacin patch in rabbits

目的:研究复方吲哚美辛贴剂中沙丁胺醇在家兔体内的药动学特征。方法:外贴及灌胃给药,采用离子对(DEHP)二氯甲烷萃取,并用HPLC荧光法测定血浆中沙丁胺醇的浓度。结果:外贴和灌服给药的药动学过程均为一室模型,主要药动学参数分别为:AUC:(435.7±101.8)μg·h·L-1和(23.9±6.3)μg·h·L-1;Cmax:(68.7±21.8)μg·L-1和(5.8±2.1)μg·L-1;Tmax:(2.51±0.18)h和(1.95±0.09)h;t1/2(ke):(2.7±0.8)h和(1.41±0.30)h。双、单侧t检验结果表明,两制剂的AUC、Cmax、Tmax、Ke、t1/2(ke)等参数有显著性差异(P<0.05)。结论:贴剂有达峰时间长和体内保留时间长的特点,具有长效缓释作用。

OBJECTIVE To study the pharmacokinetic of salbutamol for patch in rabbit. METHODS The indomethacin patch and salbutamol suspensio were given to rabbit in single dose manner. The drug concentration in plasma was determined by HPLC with fluorescence detection. RESULTS The concentration-time curves of the two preparations fitted to open one-compartment model. The main pharmacokinetic parameters for indomethacin patch and salbutamol suspension were： AUC： （435.7±101.8）μg·h·L^-1 and（23.9±6.3）μg·h·L^-1；Cmax：（68. 7±21.8） μg·L^-1 and （5.8±2. 1） μg·L^-1 ;Tmax（2.51±0. 18） h and （1.95±0.09） h; t,/2（ke）：（2. 7 ± 0. 8） h and （1.41±0. 30） h. The results showed significant difference between the two preparations （P〈0. 05）. CONCLUSION The patch has long-releasing property. The drug concentration in plasma of salbutamol in patch is higher than that in suspension,the patch has better efficacy.