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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。
Objective: To study the drug release behavior of nimesulide pellets in rabbits and its correlation with in vitro dissolution. Methods: To establish a HPLC method for the determination of nimesulide in human plasma. The changes of plasma concentration of rabbits after oral administration of pellets were investigated. Pharmacokinetic parameters were calculated by 3p87 pharmacokinetic program. Results: The main pharmacokinetic parameters of sustained-release pellets were Cmax (12.24 ± 0.21) μg · ml-1, tpeak (3.78 ± 0.02) h and t1 / 2a (2.04 ± 0.15) h, AUC (130.74 ± 4.08) μg · h · ml-1 dissolution results in vitro cumulative dissolution percentage and body absorption fraction correlation equation F2.0104 +0.6339X, r = 0.9938. Conclusion: The cumulative dissolution percentage of pellets in vitro has a significant correlation with the absorption fraction in vivo, and it has good sustained release in vivo.