制备塞来昔布(1)包合物并采用紫外和红外分析方法验证。建立了大鼠血浆中1的LC-MS测定法,考察1混悬液及1--环糊精包合物单剂量(10 mg/kg)灌胃给予大鼠后的体内药动学行为。结果表明,1的两种剂型在大鼠体内的经时过程均符合一室模型,1混悬液及包合物的cmax分别为(2 644.2±435.3)和(3 811.0±313.1)g/L;AUC0→48 h分别为(20 957.5±3 040.6)和(31 086.5±4 401.1)g.h.L-1。1包合物对1混悬液的相对生物利用度为148.3%。 Celecoxib (1) inclusion complex was prepared and verified by UV and IR analysis. An LC-MS method was established for the determination of plasma 1 in rat plasma. The in vivo pharmacokinetics of 1 suspension and 1-cyclodextrin inclusion complex were determined by intragastric administration of a single dose (10 mg / kg). The results showed that the time course of the two formulations of 1 in rats were in line with the one-compartment model, the cmax of 1 suspension and inclusion complex were (2 644.2 ± 435.3) and (3 811.0 ± 313.1) g / L ; AUC0 → 48 h were (20 957.5 ± 3 040.6) and (31 086.5 ± 4 401.1) ghL-1.1 respectively. The relative bioavailability of inclusion complex to 1 suspension was 148.3%.