吲哚美辛控释胶囊稳态血药学浓度测定及稳定性考察

 选择6名男性健康志愿受试者，口服给予多剂量吲哚美辛控释胶囊，并测定了给药达稳态后的血药浓度。与普通胶囊比较，控释胶囊75mg／次，qd给药，稳态时血浓波动性明显比普通胶囊25mg／次，tid的血浓波动性小，峰谷比为：控释胶囊2．69～～2．93，普通胶囊6．55～10．24。控释胶囊的峰、谷浓度均在有效血浓范围之内，说明每日给药1次，即可维持24h药效。用FDA低温考察法、光照和加热稳定性试验考察了控释胶囊的稳定性。结果表明，其稳定性良好，使用期限可达2年以上。

Steady-state serum concentration and stability of controlled release in-domethacin capsule

The steady- State serum concentrations of drug were derermined following multiple-dose administration of controlled release indomethacin capsule(CRIC)in 6 human subjects. Com-pared with a conventional indomethacin capsule(CIC),CRIC demonstrated a smoother serumconcentration- time profile(75mg,once a day)than that of CIC(25mg,three times a day).CRLCcan maintain serum concentration of drug in therapeutic range to be taken once a day only. Thestability of CRIC was also determined.The results showed CRIC is stable within two years.