双氯芬酸钠缓释微丸在兔体内的药动学

Pharmacokinetic study of diclofenac sodium sustained release micropellets in rabbit

目的 :测定双氯芬酸钠缓释微丸 (DS SRMP)在家兔体内药动学及相对生物利用度。方法 :用紫外分光光度法测定家兔体内的血药浓度 ,研究DS SRMP的吸收动力学及生物利用度。结果 :DS SRMP在体内 0～ 8h的吸收速度符合表观零级动力学过程 ,其Ka0 =12 .14 % /h。结论 :体内药动学研究表明 ,DS SRMP缓释效果明显 ,给药后血药浓度较为平缓 ,持续作用时间长 ,可减少给药次数。该缓释制剂相对于其普通片剂具有释药稳定 ,生物利用度高 。

OBJECTIVE To determine pharmacokinetic and relative bioavailability of diclofence sodium sustained release micropellets(DS?SRMP) in vivo.METHODS UV method was established for assaying serum diclofence sodium concentrations in rabbits. To study theabsorptive kinetics and bioavailability of DS?SRMP. RESULTS The absorption rate of DS?SRMP in vivo was found to conform apparent zero orderkinetics(Ka 0= 12.14% /h)during the first 8 h .CONCLUSIONS The studies of pharmacokinetics in vivo indicated DS SRMP had sustained release effect.The drug concentration in blood was steady after oral administration, it could last longer and reduce the times of adminstration. The preparation release stability, bioavailability and safty.