阿司匹林胃漂浮型缓释胶囊的制备及药物动力学研究

Development and pharmacokinetic study on aspirine sustained release floating capsule for oral use

本实验利用流体动力学平衡体系（ＨＢＳ）原理，研制了阿司匹林胃漂浮型缓释胶囊（Ａ－ＨＢＳＣ）；并进行了体外溶出速度测定及兔体内药动学研究。Ａ－ＨＢＳＣ的体外溶出属零级动力学过程，Ｋ°ａ＝９．２１％／ｈ（ｔ≤８ｈ）；体内０～８ｈ的吸收速度符合表观零好动力学过程，Ｋ°ａ＝１０．５１％／ｈ；体内外数据具有显著的相关性（ｒ＝０．９９１７，Ｐ＜０．０１）。体内药动学研究表明Ａ－ＨＢＳＣ缓释效果明显，给药后血药浓度较为平缓，持续作用时间长，可减少给药次数；并由于Ａ－ＨＢＳＣ采用轻质辅料具漂浮性能，缓慢释药，有利于降低对胃肠道的刺激性及其它不良反应。

spirine sustained release floating capoules(A-HBSC)for oral use were developed according to the principle of the hy-drodynanamically balanced system(HBS).Their dissolu tion rates in vitro were detected,and the pharmacokinetics in rabbitswere studied,The dissolution test showed that the release- mechan ism of A- HBSC in vitro may be described by apparent zero-order kinetics,K°a=9.21%/h(t≤8h);The rate of absorption of A-HBSC in vivo was found to conform to apparent zero-or-der kinetics (K°a=10.51%/h) during the first 8h,and there is a linere relationship between percent absorption in vivo and per-cent dissolution in vitro (r=0.9917,P<0.01). The studies of the pharmacokinetics in vivo indicated A-HBSC had sustainedrelease effect.The drug concentration in blood was steady after oral administration,it could last longer and reduce the times ofadministration. Because the light-excipient were used in A-HBSC,which had floating properties and could make drug releaseslowly.A-HBSC could decrease the irritations or side effects of gastrointestinal tract.