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目的:研究沙美特罗白蛋白微球在大鼠体内的药动学特征。方法:12只大鼠随机分成沙美特罗白蛋白微球组和沙美特罗溶液组,每组6只,分别灌胃给药(20μg·kg~(-1))后不同时间取血,HPLC法测定血药浓度,用3P97软件计算药动学参数。结果:沙美特罗溶液和沙美特罗白蛋白微球在大鼠体内的主要药动学参数:t_(max)分别为(0.73±0.15)和(3.22±0.20)h,C_(max)分别为(1.10±0.19)和(1.25±0.24)μg·m1~(-1),t_(1/2ka)分别为(0.35±0.05)和(1.58±0.07)h,t_(1/2ke)分别为(2.30±0.85)和(8.21±1.20)h,AUC_(0→∞)分别为(1.55±0.25)和(3.45±0.55)mg.h·L~(-1)。结论:与沙美特罗溶液相比,沙美特罗白蛋白微球具有明显的缓释效果,同时提高了药物的生物利用度。
Objective: To study the pharmacokinetics of salmeterol albumin microspheres in rats. Methods: Twelve rats were randomly divided into salmeterol microsphere group and salmeterol solution group, with 6 rats in each group. Blood samples were taken at different times after intragastric administration (20μg · kg ~ (-1)), HPLC Method of determination of plasma concentration, using 3P97 software to calculate pharmacokinetic parameters. RESULTS: The main pharmacokinetic parameters of salmeterol and salmeterol microspheres in rats were: t max (0.73 ± 0.15) and (3.22 ± 0.20) h, respectively, and C max were (1.10 ± 0.19) and (1.25 ± 0.24) μg · m ~ (-1) respectively, t 1/2 (1/2) were (0.35 ± 0.05) and (1.58 ± 0.07) 2.30 ± 0.85 and 8.21 ± 1.20 h respectively, and AUC 0-0∞ were (1.55 ± 0.25) and (3.45 ± 0.55) mg.h · L -1, respectively. Conclusion: Compared with salmeterol salmeterol salmeterol microspheres has a significant sustained release effect, while improving the bioavailability of the drug.