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目的 :验证盐酸奈福泮缓释片的缓释特性并判定其生物等效性。方法 :18名健康受试者随机分成两组 ,采用双周期交叉试验设计 ,单剂量、多剂量连续给药 ,用高效液相色谱法测定血药浓度 ,以3p97药代动力学程序求算相关参数。结果 :单剂量给药的结果表明 :缓释片在给药后 2～ 12h内血药浓度维持在 2 0～ 4 0mg·L- 1之间 ,cmax 为 (45 .8±15 .7)mg·L- 1,tpeak为 (3.4± 0 .8)h ;普通片在给药后 0 .5～ 8h内血药浓度维持在 2 0mg·L- 1以上 ,cmax为 (72 .7± 2 6 .0 )mg·L- 1,tpeak为 (1.6± 0 .6 )h。两制剂的AUC分别为 (36 3.4± 10 7.7)及 (374 .8±12 5 .7)mg·h·L- 1,平均相对生物利用度为 1.0 2±0 .2 5。多剂量给药的结果表明 :缓释片和普通片的cmax分别为 (31.5± 12 .7)及 (33.7± 10 .5 )mg·L- 1,cmin分别为 (13.4± 4 .4 )及 (10 .9± 5 .4 )mg·L- 1,tpeak分别为 (2 .6± 0 .6 )及 (1.2± 0 .5 )h ,FI分别为0 .77± 0 .2 6及 1.0 4± 0 .18。结论 :该缓释片具有缓释特征 ,两制剂生物利用度 (AUC)具有等效性
Objective: To verify the sustained-release characteristics of nefopam hydrochloride sustained-release tablets and determine its bioequivalence. Methods: Eighteen healthy subjects were divided into two groups at random. The study was designed by double-cycle crossover design. Single and multi-dose continuous administration, plasma concentration was determined by high performance liquid chromatography and correlated with 3p97 pharmacokinetic program parameter. Results: The results of single-dose administration showed that the sustained-release tablets maintained the plasma concentration of 20 ~ 40 mg · L-1 within 2 ~ 12 h after administration, and the cmax was (45.8 ± 15.7) mg · L-1 and tpeak were (3.4 ± 0.8) h. The plasma concentration of common tablets remained above 20 mg · L -1 within 0.5-5 h after administration, the cmax was (72.7 ± 2 6) .0) mg · L- 1 and tpeak (1.6 ± 0.6) h. The AUC of the two preparations were (36 3.4 ± 10 7.7) and (374.8 ± 125.7) mg · h · L -1, respectively. The average relative bioavailability was 1.0 2 ± 0.52. The results of multiple dose administration showed that the cmax of sustained-release tablets and ordinary tablets were (31.5 ± 12.7) and (33.7 ± 10.5) mg · L-1, respectively, and the cmin values were (13.4 ± 4. 4) and (10.9 ± 5.4) mg · L-1, tpeak were (2.6 ± 0.6) and (1.2 ± 0.5) h, FI were 0.77 ± 0.26 and 1.0 4 ± 0 .18. Conclusion: The sustained-release tablets have the characteristics of sustained release, bioavailability (AUC) of two preparations has the equivalent