吲哚美辛控释胶囊的制备及人体生物利用度

 采用沸腾包衣工艺制成吲哚美辛膜控释微丸，并用此微丸制成含吲哚美辛75mg，日服1次,可维持24h药效的控释胶囊。对其体外溶出和人体生物利用度的研究表明，控释胶嚢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，达到了預期的控释效果，控释胶囊体内吸收分数与体外累枳溶出百发率之间具有显著的线性相关性(r=0.9901,P＜0.01)。

Preparation and bioavailability in human subjects of controlled releaseindomethacin capsule

In order to avoid high initial peak of the commercially available indomethacinformulations and increase the interval between dosages,controlled release capsule contahingindomethacin pellets,coated with polymethacrylates,were prepared by using fluidized bed coatedtechnique.Each capsule contained 75mg indomethacin,and was taken once a day. The in vitrodissolution and in vivo bioavilability(in 12 human subjects)of the capsule were determined andcompared.Determination of indomethacin serum comcentral was capsule out by HPLC.The studies showed the capsule relese drug with a first-order kinetics in vitro(K_r=0.2266h^-1)and demonsteatad a smoother serum concentration-time profile than a conventional capsule in elimination phase but much lower in macximum concentration in vivo.There was a linear relationship between percent absorption in vivo and percent dissolition in vitro(r=0.9901.P＜0.01).Bioavailability of the controlled release was also better than that of the concentional capsule.