【摘要】 目的:研究尼美舒利微丸在家兔体内释药行为及其与体外溶出的相关性。方法:建立检测体内尼美舒利血药浓度的高效液相色谱法,研究家兔灌服微丸后的血药浓度经时变化情况,采用3p87药代动力学程序计算药动学参数。结果:缓释微丸的主要药动学参数Cmax(12.24±0.21)μg·ml-1;tpeak(3.78±0.02)h;t1/2a(2.04±0.15)h;AUC(130.74±4.08)μg·h·ml-1.溶出度结果体外累积溶出百分率与体内吸收分数的相关方程F2.0104+0.6339X,r=0.9938。结论:微丸在体外累积溶出百分率与体内吸收分数有显著相关性,且体内有良好的缓释作用。更多还原

【Abstract】 Objective: To study the correlation between the absorption in vivo and the dissolution in vitro of nimesulide sustained-release micropellets in rabbits, the drug-releasing process of nimesulide sustained-release micropellets in rabbits’bodies, and whether the parameters of in viro and in vitro had the correlation. Method: To establish a method for determination of nimesulide concentration in blood to study the drug-time change after the micropellets ig. The parameters of pharmacokinetics of each rabbit were individually calculated by a 3p87 program. Result: The main parameters of sustained-release micropellets were : Cmax 12. 24,21 μg·ml-1 ;tmax (3.78±0.02)h;t1/2a(2.04±0. 15)h; AUC00-∞ 130.74±4.08 μg·h·ml-1. TSA linear regression equation was established between the of percentage absorprtion in vivo and the percentage of accumulate dissolution in vitro of nimesulide. F =2. 0104 +0. 6339X, r = 0.993 8. Conclusion: There was a significant correlation between the absorption in vivo and the dissolution in vitro, and had a good sustained-release effect in body.更多还原