【摘要】 目的:研究磷酸可待因缓释片在正常人体内的药物动力学和生物利用度.方法:采用RP-HPLC法测定可待因的血药浓度,研究8名志愿者单剂量po 90mg磷酸可待因缓释片及普通片后药物动力学及相对生物利用度;另对8例志愿者po 90mg磷酸可待因缓释片及iv磷酸可待因30mg后绝对生物利用度进行了研究.结果:单剂量po 90mg缓释片及普通片后,AUC_0→∞分别为（524.17±129.61）和（337.90±85.20）ng·h/ml;t_max分别为（2.75±0.46）和（1.31±0.26）h,C_max分别为（74.34±7.84）和（89.63±10.58）ng/ml,两种制剂的AUC_0→∞、t_max、C_max均有显著性差异（P<0.05）.磷酸可待因缓释片相对及绝对生物利用度分别为（156.1±6.3）%和（84.1±4.8）%.结论:缓释片与普通片为生物不等效制剂.更多还原

【Abstract】 AIM:To study the bioavailability and pharmacokinetics of codeine phosphate sustained release tablets in healthy volunteers . METHODS: The plasma concentration of codeine was determined by reversed phase high performance liquid chromatography in 8 volunteers after single oral administration 90 mg codeine phosphate sustained release tablets and conventional tablets. The absolute bioavailability of sustained release tablets was studied in 8 volunteers after given 90 mg sustained release tablets and 30 mg codeine injections. RESULTS: cmax of sustained release tablets and conventional tablets was (74.34±7.84) and (89.63±10.58)ng/ml,tmax was(2.75±0.46) and (1.31±0.26)h;AUC0-∞was (524.17±129.61) and (337.90±85.20)ng·h/ml; respectively. The results of statistical analysis showed significant difference of tmax,cmax and AUC0-∞ between 2 preparations(P<0. 05). The relative and absolute bioavailability of codeine phosphate sustained release tablets were (156.1±6.3)% and (84.1±4.8)% ,respectively.CONCLUSION: Codeine phosphate sustained release tablets and conventional tablets are not bioequivalent.更多还原