目的研究吡罗昔康环糊精包合物Beagle犬体内药物动力学。方法 6只Beagle犬采用随机、双周期交叉给药,单剂量灌胃给予吡罗昔康受试制剂或参比制剂,用HPLC法测定吡罗昔康血浆浓度,用统计矩原理进行血药浓度-时间数据分析。结果吡罗昔康包合物的达峰时间tmax快于普通片剂,分别为(0.89±0.09)、(3.92±0.49)h,两者有显著差异(P<0.01),两者的半衰期t1/2分别为(31.30±4.38)、(29.38±1.83)h,曲线下面积(AUC0～t)分别为(242.92±30.04)、(230.55±8.06)μg/(h.ml),最高血药浓度(Cmax)分别为(7.82±0.44)、(7.49±0.36)μg/ml,清除率(Cl)分别为(80.92±10.65)、(85.27±2.95)ml/h,表观分部容积(Vd)分别为(3.36±0.51)、(3.22±0.19)L,均无明显差异(P>0.05),吡罗昔康包合物相对于市售片剂的相对生物利用度为106.74%。结论建立的HPLC分析方法准确可靠。两种剂型的生物利用度相似,将吡罗昔康制成包合物后能大大加快药物在体内的吸收速度,使其更快发挥药效。 Objective To study the pharmacokinetics of piroxicam inclusion cyclodextrin inclusion body in Beagle dogs. Methods Six Beagle dogs were randomized to receive double-cycle crossover and single-dose intragastric administration of piroxicam test or reference formulation. Plasma concentrations of piroxican were determined by HPLC and plasma concentration-time data . Results The peak tmax of piroxicam inclusion complex was (0.89 ± 0.09) and (3.92 ± 0.49) h respectively, which was significantly higher than that of the conventional tablet (P <0.01). The half-life t1 / 2 (AUC0 ~ t) were (242.92 ± 30.04), (230.55 ± 8.06) μg / (h.ml), and the highest plasma concentration (Cmax) were (31.30 ± 4.38) and (29.38 ± 1.83) ) Were (7.82 ± 0.44) and (7.49 ± 0.36) μg / ml respectively, and the clearance rates were (80.92 ± 10.65) and (85.27 ± 2.95) ml / (3.36 ± 0.51) and (3.22 ± 0.19) L, respectively (P> 0.05). The relative bioavailability of piroxicam inclusion complex relative to the commercial tablets was 106.74%. Conclusion The established HPLC method is accurate and reliable. The bioavailability of the two formulations is similar, the inclusion of piroxicam can greatly accelerate the rate of drug absorption in the body to make it faster to play a pharmacodynamic effect.