摘要:Objective: To evaluate the bioequiavailability of the domestic and the imported paracetamol and oxycodone hydrochloride capsules. Methods: The blood concentrations of paracetamol and oxycodone capsules in two capsules in 24 healthy male volunteers were determined by HPLC-UV and HPLC-MS-MS after a single oral dose with a randomized crossover method.Results: The main pharmacokinetic parameters of the paracetamol in the test and reference preparation were as follows: tmax were (0.75 ± 0.48) and (0.64 ± 0.43) h, respectively; Cmax were (13.45 ± 6.13)and (13.72 ± 5.24) mg·L-1, respectively; t1/2 were (1.92 ± 0.51 )and (2.24 ± 0.72) h, respectively; AUC0-tn were (39.55 ± 8.34) and (39.65 ± 8.58) mg·L-1·h, respectively; AUC0-∞ were (42.30 ± 8.85)and (42.95 ± 10.11 ) mg· L-1· h, respectively. The relative bioavailability of paracetamol in the test preparation was (101.56 ± 19.43)%.The main pharmacokinetic parameters of the oxycodone in the test and reference preparation were as follows: tmax were (0.86 ± 0.34)and (0.90 ± 0.42) h, respectively; Cmax were (25.81 ± 9.54) and (22.53 ± 7.32) μg·L-1, respectively; t1/2 were (4.51 ± 0.87) and (4.52 ± 0.73) h, respectively; AUC0-tn were (129.67 ± 37.27) and (116.78 ± 41.35) tg· L-1· h, respectively; AUC0-∞ were (134.07 ± 38.69)and (121.61 ±42.13) μg· L-1·h, respectively. The relative oxycodone bioavailability of the test preparation was (116.18±25.90)%.Conclusion: The domestic paracetamol and oxycodone hydrochloride capsules were bioequivalent to the imported ones.%目的:评价国产与进口两种氨酚羟考酮胶囊的生物等效性.方法:24名健康男性志愿者随机交叉单剂量口服2种氨酚羟考酮胶囊,采用高效液相色谱.紫外法和高效液相.质谱.质谱法分别测定血浆中对乙酰氨基酚和盐酸羟考酮的浓度.结果:受试制剂与参比制剂中时乙酰氨基酚的t<,max>,分别为(0.75 ±0.48)和(0.64±0.43)h,C<,max>分别为(13.45±6.13)和(13.72±5.24)mg·L<'-1>,t<,1/2>分别为(1.92±0.51)和(2.24±0.72)h;AUC<,0-tn>分别为(39.55±8.34)和(39.65±8.58)mg·L<-1>·h,AUC<,0-∞>分别为(42.30±8.85)和(42.95±10.11)mg·L<'-1>·h,受试制剂的相对生物利用度为(101.56±19.43)%;而盐酸羟考酮的t<,max>分别为(0.86±0.34)和(0.90±0.42)h;C<,max>分别为(25.81±9.54)和(22.53±7.32)μg·L<'-1>;t<,1/2>分别为(4.51±0.87)和(4.52±0.73)h;AUC<,0-tn>分别为(129.67±37.27)和(116.78±41.35)μg·L<'-1>·h,AUC<,0-∞>分别为(134.07±38.69)和(121.61±42.13)μg·L<'-1>·h;受试制荆的相对生物利用度为(116.18±25.90)%.结论:两制荆具有生物等效性.