台灣人口服nimesulide的藥物動力參數可能和西方人不同，我們需更多的藥物動力學，藥效學及藥物基因學之研究，來確定台灣人使用此藥時之最佳劑量。 Background and purpose
Nimesulide is a selective cyclooxygenase-2 (COX-2) inhibitor exerting analgesic, antipyretic and antiplatelet activity. COX-2 inhibitor was shown to have less gastrointestinal adverse effects. However, its cardiovascular side effect has been drawn much attention recently. The purpose of the study is to compare the pharmacokinetics of nimesulide(via oral administration) in Taiwanese subjects to that of Western peoples.
Twelve healthy Taiwanese subjects (25 to 39 years) enrolled in the study. Each subject received a single oral dose of 100mg numesulide in fasting state. After orally administrated, blood samples were drawn up to 24 hours. The plasma concentrations of nimesulide were determined using HPLC and pharmacokinetic parameters were derived from nimesulide plasma concentration-time profiles..
Following oral administration of 100mg nimesulide in Taiwanese subjects, the AUC0-∞was 59.27±22.78μg‧h/ml, which is 1.14 to 3.73 times to the results in Western peoples. The Cmax was 6.09±1.10μg/ml, which is 0.94 to 2.13 times higher compared to the results of Western peoples. Clearance in Taiwanese was only 31.0 to 71.7% compared to the clearance of Western groups. Both data as well as previous publication, showed taht higher Cmax , AUC and lower clearance, lower volume distribution in Taiwanese subjects were observed compared to those in Western people. Tmax and t1/2 did not differ significantly between Taiwanese and Western people.
The pharmacokinetics parameters of nimesulide in Taiwanese subjects may be different from other ethnic populations. More pharmacokinetic and pharmcodynamic studies are needed to determine the optimal dosage of nimesulide for Taiwanese.