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采用HPLC法测定血清中阿西美辛的活性代谢物吲哚美辛的浓度,研究了国产阿西美辛缓释胶囊的药代动力学及其相对进口阿西美辛生物利用度。12名健康受试者自身交叉口服单剂量阿西美辛缓释胶囊和进口阿西美辛缓释胶囊(90mg),血清中吲哚美辛的Cmax分别为:0.98±0.30mg·L-1和1.01±0.29mg·L-1;Tpeak分别为:3.00±0.60h和3.08±1.08h,AUC0-∞分别为:6.47±2.44mg·h·L-1和6.53±1.99mg·h·L-1。国产阿西美辛缓释胶囊的相对生物利用度为99.78±23.79%。12名健康受试者自身交叉口服多剂量阿西美辛缓释胶囊和进口阿西美辛缓释胶囊(90mg,qd,共7d)后,测得吲哚美辛的Css,max分别为:1.08±0.25mg·L-1和1.06±0.36mg·L-1,Cs,min分别为:0.06±0.02mg·L-1和0.07±0.02mg·L-1;AUC0-t分别为:6.22±1.81mg·h·L-1和6.11±1.84mg·h·L-1;波动系数(FI)分别为1.78±0.07和1.76±0.06。国产阿西美辛缓释胶囊的相对生物利用度为104.10±?
The concentration of indometacin, the active metabolite of Asimesin in serum, was determined by HPLC. The pharmacokinetics of Asiamicin Sustained Release Capsules and the relative bioavailability of Asimustine were also studied. Twelve healthy volunteers crossed with single dose of Simixin sustained release capsules and imported Simitin sustained release capsules (90mg). The Cmax of serum indomethacin was 0.98 ± 0.30mg · L-1 and 1.01 ± 0.29 mg · L-1, Tpeak were 3.00 ± 0.60 h and 3.08 ± 1.08 h respectively, AUC0-∞ were 6.47 ± 2.44 mg · h · L-1 and 6.53 ± 1.99 mg · h · L-1. The relative bioavailability of domestic asi mesin sustained release capsules was 99.78 ± 23.79%. Twelve healthy volunteers crossed with oral multi-dose simvastatin and extended-dose asiracetam capsules (90mg, qd for 7 days), and measured the Css, max of indomethacin as follows: 1.08 ± 0.25 mg · L-1 and 1.06 ± 0.36 mg · L-1, Cs, min were 0.06 ± 0.02 mg · L-1 and 0.07 ± 0.02 mg · L-1; AUC0-t were 6.22 ± 1.81 mg · h · L-1 and 6.11 ± 1.84 mg · h · L-1, respectively; the volatility coefficients were 1.78 ± 0 .07 and 1.76 ± 0.06. The relative bioavailability of domestic asi mesin sustained release capsules was 104.10 ±?