双氯芬酸钠迟效制剂的药动学

目的 :以双氯芬酸钠普通肠溶片 (R)为对照 ,比较国产双氯芬酸钠迟效制剂 (T)的相对生物利用度和药动学。方法 :采用双交叉、自身对照的方法 ,将 2 4名受试者分为 2组 ,单剂量组分别口服T和R各 10 0mg ;多剂量组 ,每日分别口服T和R各10 0mg ,共 4d。结果 :单剂量组T和R的Cmax,Tmax,T1/2 ,MRT ,AUC0～τ分别为 (115 6±s 36 1)和(3910± 96 8) μg·L- 1,(3.0± 1.0 )和 (2 .3± 0 .5 )h ,(6 .6± 2 .3)和 (2 .9± 1.5 )h ,(12 .3± 2 .3)和 (4.4±1.0 )h ,(92 37± 994 )和 (874 5± 12 16 ) μg·h·L- 1,T的F为 (10 7± 12 ) %。多剂量口服T和R的Cav,FI分别为 (343± 4 6 ) μg·L- 1和 (333± 6 4) μg·L- 1,(2 5 4± 82 ) %和 (40 4± 97) %。结论 :2种制剂口服吸收相似 ,迟效制剂具有峰谷浓度差异小 ,血药浓度波动幅度小等缓释药动学特征。

Pharmacokinetics of diclofenac sodium delayed-action preparation

AIM: To compare pharmacokinetics and bioavailability of diclofenac sodium delayed-action preparation with enteric coated tablets. METHODS: A double cross-over, controlled study was conducted. Twenty-four healthy male volunteers were divided into two groups.Diclofenac sodium delayed-action preparation and diclofenac sodium enteric coated tablets were taken in a single or multidose of 100 mg.A HPLC method was used to determine the plasma drug concentration. RESULTS: The C max,T max, T 1/2,MRT,AUC 0～τ of diclofenac sodium delayed-action preparation and diclofenac sodium enteric coated tablets after single dose oral administration were(1 156±s 361)and (3 910±968) μg·L -1, (3.0±1.0)and (2.3±0.5) h,(6.6±2.3) and (2.9±1.5) h,(12.3±2.3) and (4.4±1.0) h,( 9 237±994)and(8 745±1 165)μg·h·L -1, F value of diclofenac sodium delayed-action preparation was (107±12)%.The average C av, FI values after multidose oral administration were (343±46)and (333±64)μg·L -1, (254±82) and (404±97)%,respectively. CONCLUTION:The two formulations are bioequivalent and the delayed-action preparation shows smaller difference between C max and C min ,and smaller FI of plasma concentration compared with the enteric coated tablets.