尼美舒利口腔崩解片生物等效性研究

目的研究尼美舒利口腔崩解片的药代动力学和相对生物利用度。方法采用HPLC法测定20名健康男性志愿受试者,随机自身交叉单剂量口服尼美舒利口腔崩解片和尼美舒利片200mg后的血药质量浓度,得出相应的药时曲线,计算各药代参数和相对生物利用度。结果半衰期t1/2分别为(3.626±1.098)h和(3.369±0.55)h,达峰时间tmax分别为(3.70±0.80)h和(3.55±0.76)h,峰值血浆质量浓度Cmax(实测值)分别为(8.47±1.86)mg·mL-1和(8.55±2.41)mg·mL-1,药时曲线下面积AUC0～16h分别为(56.90±12.58)和(54.63±17.35)mg.h.L-1。2种制剂的药动学参数无显著性差异(P>0.05),受试制剂的相对生物利用度(F)为106.62%。结论2种制剂具有生物等效性。

Study on pharmacokinetics and relative bioavailabity of nimesulide orally disintegrating tablets

Objective To study the relative bioavailability and the phamacokinetics of nimesulide orally disintegrating tablets.Method A single oral administration 200 mg of nimesulide orally disintegrating tablets were given in 20 healthy male volunteers divided into two groups according to randomized crossover design.Nimesulide concentrations in plasma were determined by HPLC.The pharmacokinetic parameters and relative bioavailability of tested tablets were calculated and compared with that of reference tablets.Result After a single oral administration 200 mg of orally disintegrating tablets and reference tablets,the obtained pharmacokinetic parameters were as follows :t1/2(3.626±1.098)h and(3.369±0.55)h;tmax(3.70±0.80)h and(3.55±0.76)h;Cmax:(8.47±1.86)mg·L-1 and(8.55±2.41)mg·L-1;AUC0~16 h(56.90±12.58)mg·h·L-1 and(54.63±17.35)mg·h·L-1.respectively.The relative bioavailability of tested tablets was 106.62%.No significant differences were found among the main pharmacokinetic parameters(P>0.05).Conclusion The two preparations presented bioequivalent.