摘要
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对乙酰氨基酚的tmax分别为(0.75±0.48)和(0.64±0.43)h,Cmax分别为(13.45±6.13)和(13.72±5.24)mg.L-1,t1/2分别为(1.92±0.51)和(2.24±0.72)h;AUC0-tn分别为(39.55±8.34)和(39.65±8.58)mg.L-1.h,AUC0-∞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tmax分别为(0.86±0.34)和(0.90±0.42)h;Cmax分别为(25.81±9.54)和(22.53±7.32)μg.L-1;t1/2分别为(4.51±0.87)和(4.52±0.73)h;AUC0-tn分别为(129.67±37.27)和(116.78±41.35)μg.L-1.h,AUC0-∞分别为(134.07±38.69)和(121.61±42.13)μg.L-1.h;受试制剂的相对生物利用度为(116.18±25.90)%。结论:两制剂具有生物等效性。
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) μg·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.
出处
《中国药物应用与监测》
CAS
2011年第1期9-12,共4页
Chinese Journal of Drug Application and Monitoring