盐酸奈福泮缓释片药代动力学及生物等效性  

Pharmacokinetics and bioequivalence of sustained-released tablet of nefopam

作　　者：王少华[1] 于宝东[1] 陈安进[1] 初晓[1] 姜新道[1] 赵美玲[1] 闫美兴[1] 

机构地区：[1]青岛市立医院临床药理基地,青岛266011

出　　处：《中国临床药理学与治疗学》2002年第1期57-59,共3页Chinese Journal of Clinical Pharmacology and Therapeutics

摘　　要：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)AIM: To verify the bioequivalence between sustained released tablet of nepopam and normal one. METHODS: 18 volunteers were randomly devided into two groups. Double periodical crossed design was used, and poly dose of nefopam was administered to 18 volunteers following single dose after one week interval. The concentration of nefopam hydrochloride in serum was determinated by HPLC, and the related parameters came out through 3p97 programme. RESULTS: In the single dose test the drug concentration of sustained released tablet maitained 2040 mg·L -1 for 10 h ,c max was ( 45.8 ±15.7) mg·L -1 ,t peak was ( 3.4 ± 0.8) h , and the corresponding parameters of normal tablet were over 20 mg·L -1 for 7.5 h ,( 72.7 ±26.0) mg·L -1 ,and ( 1.6 ± 0.6) h . The AUC was ( 363.4 ± 107.1 ) and ( 374.8 ±125.7) mg·h·L -1 respectively, and F was ( 1.02 ± 0.25 ). In the poly dose test the c max of sustained released and normal one was ( 31.50 ± 12.65 ) and ( 33.68 ±10.51) mg·L -1 ,c min was ( 13.4 ± 4.4 ) and ( 10.9 ±5.4) mg·L -1 , t peak was ( 2.6 ± 0.6 ) and ( 1.22 ± 0.46) h , and FI was ( 0.77 ± 0.26 ) and ( 1.04 ± 0.18 ) respectively. CONCLUSION: The sustained released tablet is credible and the two types of tablet are equieffective in AUC.

关 键 词：盐酸奈福泮缓释片 高效液相色谱法 生物等效性 药物动力学 镇痛药 

分 类 号：R969.1[医药卫生—药理学] R971.1[医药卫生—药学]