尼美舒利栓剂的制备及其药动学

The preparation and pharmacokinetics of nimesulide suppository

目的 :制备尼美舒利栓剂并考察其体内药动学过程。方法 :以半合成脂肪酸甘油酯为基质制备尼美舒利栓剂 ,高效液相色谱法测定血浆中尼美舒利浓度 ,用 3P97程序计算家兔直肠给药后药动学参数。结果 :该方法精密度好 ,回收率高 ,栓剂Tmax为 (3.8± 0 .8)h ,T1 / 2 (Ke) 为 (5 .0± 0 .8)h ,Cmax为 (40 .7± 9.2 )mg·L-1 。结论 :尼美舒利栓剂具有良好的药动学特征 ,为开发尼美舒利栓剂提供了依据。

OBJECTIVE To study the preparation and pharmacokinetic properties of the suppository. METHODS The plasma concentration of nimesulide was determined by high performance liquid chromatography.The Pharmacokinetic parameters were calculated with 3P97 program after rectal administration in rabbits. RESULTS The precision was high and recovery was good. T max was ( 3.8± 0.8)h, T 1/2ke was ( 5.0± 0.8)h and C max was ( 40.7± 9.2)mg·L -1. CONCLUSION Nimesulide suppository has good pharmacokinetic property,and can be developed as a new drugproduct.