吲哚美辛控释胶囊稳态血药浓度测定及稳定性考察

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

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。

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.