目的评价国产的双氯芬酸钠缓释片在正常人体内药代动力学和生物等效性,为临床合理用药提供依据。方法采用随机交叉试验设计,健康男性志愿者单次和多次口服受试和参比两种双氯芬酸钠缓释片,运用HPLC法测定血浆中双氯芬酸钠的药物浓度,计算两药的药物动力学参数。结果单次口服受试制剂和参比试剂的cm ax分别为(501±111)μg.L-1和(518±120)μg.L-1;tm ax分别为(3.9±0.9)和(3.8±0.9)h;AUC0~24分别为(4568±861)和(4724±1044)μg.h-1.L-1。多次口服受试制剂和参比制剂的稳态峰浓度cssm as分别为(534.6±04.0)和(545.8±109.4)μg.L-1,稳态谷值浓度cssm in分别为(19.6±4.9)μg.L-1和(18.6±3.8)μg.L-1,tssm ax(4.0±0.8)h和(3.8±0.9)h,AUCss分别为(4820±882)μg.h-1.L-1和(4787±877)μg.h-1.L-1,Css,av分别为(371.3±75.9)μg.L-1和(367.7±69.5)μg.L-1,DF值分别为142%±3%和140%±3%。试验制剂对参比制剂的相对生物利用度F(以AUC0~24作为评价依据)为98%±10%。结论试验制剂与参比制剂具有生物等效性。 Objective To evaluate the pharmacokinetics and bioequivalence of domestic diclofenac sodium sustained-release tablets in normal human and provide basis for clinical rational drug use. Methods A randomized crossover design was used in this study. Two diclofenac sodium sustained-release tablets were tested orally and several times in healthy male volunteers. The drug concentration of diclofenac sodium in plasma was determined by HPLC. The pharmacokinetic parameters . Results The cm ax of single oral formulation and reference reagent were (501 ± 111) μg.L-1 and (518 ± 120) μg.L-1, respectively; the tm ax values ​​were (3.9 ± 0.9) and ± 0.9) h; AUC0 ~ 24 were (4568 ± 861) and (4724 ± 1044) μg.h-1.L-1, respectively. The steady-state peak concentrations cssm as of multiple oral test preparations and reference preparations were (534.6 ± 04.0) and (545.8 ± 109.4) μg.L-1, respectively, and the steady-state trough concentrations cssm in were (19.6 ± 4.9) The mean AUCss were (4820 ± 882) μg.h-1.L-1 and (18.6 ± 3.8) μg.L-1, tssm ax (4.0 ± 0.8) h and (3.8 ± 0.9) And (4787 ± 877) μg · h-1.L-1 respectively, and the values ​​of Css and av were (371.3 ± 75.9) μg.L-1 and (367.7 ± 69.5) μg.L- 3% and 140% ± 3%. The relative bioavailability of the test formulation to the reference formulation, F (based on AUC0-24) was 98% ± 10%. Conclusion The test preparation and the reference preparation are bioequivalent.