摘要
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）。
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 comcentration was carried out by HPLC. Thestudies showed the capsule release drug with a first-order kinetics in vitro(K_r=0. 2266h￣(-1))anddemonstrated a smoother serum concentration-time profile than a conventional capsule inelimination phase but much lower in maximum concentration in vivo. There vvas a linearrelationship between percent absorption in vivo and percent dissolution in vitro(r=0. 9901 ,P<0.01).Bioavailability of the controlled release capsule was also better than that of the conventionalcapsule.
出处
《中国药学杂志》
CAS
CSCD
北大核心
1994年第9期533-536,共4页
Chinese Pharmaceutical Journal
关键词
吲哚美辛
控释胶囊
生物利用度
indomethacin ,controlled release capsule,dissolution ,bioavailability
