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采用膜控法制备布洛芬缓释微丸,应用转篮法(50r/min,37±1℃)比较了缓释微丸和普通片剂的体外药物溶出速率,采用HPLC法测定了制剂的血药浓度,并研究了制剂在人体内的药物动力学。缓释微丸的体外药物溶出符合一级动力学过程(K_r=0.4505h~(-1));体内动力学过程符合一级吸收和一级消除的单室模型,k_a=0.27h~(-1),K=0.27h~(-1),V_d=7.54L,t_(max)=3.97h,C_(max)=19.52μg/ml。多剂量给药血药浓度测定及计算表明:缓释微丸具有维持有效血药浓度(8.5μg/ml)时间长,血药浓度波动范围小的特点。此外,缓释微丸的体内外数据具有显著的相关性(p<0.01)。
The ibuprofen sustained-release pellets were prepared by membrane-controlled method. The drug dissolution rate of the sustained-release pellets and ordinary tablets was compared by the spin-drying method (50r / min, 37 ± 1 ℃) Drug concentration and studied the pharmacokinetics of the formulation in humans. In vitro drug dissolution of sustained-release pellets was in accordance with the first-order kinetics (K_r = 0.4505 h -1); the in-vivo kinetic process was in accordance with the first-order absorption and first- 1), K = 0.27 h -1, V_d = 7.54 L, t max = 3.97 h and C max = 19.52 μg / ml. Multi-dose administration of plasma concentration measurement and calculation showed that: sustained-release pellets with the maintenance of effective plasma concentration (8.5μg / ml) for a long time, the characteristics of small fluctuations in blood concentration characteristics. In addition, there was a significant correlation between sustained-release pellets in vitro and in vivo data (p <0.01).