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采用沸腾包衣工艺制成到吲哚美辛膜控释微丸,并用此微几制成含吲哚美辛75mg,日服1次,可维持24h药效的控释胶囊。对大体外溶出和人体生物利用度的研究表明,控释胶囊的体外溶出符合一级动力学过程(Kr=0.2266h ̄(-1),r=0.9997),体内血药浓度明显比普通胶囊平稳,持续时间长,生物利用度略高于普通胶囊,达到了预期的控释效果。控释胶囊体内吸收分数与体外累积溶出百发率之间具有显著的线性相关性(r=0.9901,P<0.01)。
The indometacin membrane-controlled release pellets were prepared by using the boiling coating process, and the controlled release capsules containing indomethacin 75 mg and daily for 1 hour were prepared using the micro-capsules. The study of in vitro dissolution and bioavailability showed that in vitro dissolution of controlled release capsules was in accordance with the first order kinetics (Kr = 0.2266h ~ (-1), r = 0.9997). The in vivo plasma concentration significantly Ordinary capsules smooth, long duration, bioavailability slightly higher than ordinary capsules, to achieve the desired effect of controlled release. There was a significant linear correlation between the absorption fraction of controlled release capsules and the cumulative rate of dissolution in vitro (r = 0.9901, P <0.01).