摘要
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.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
1994年第6期243-246,共4页
Chinese Journal of Hospital Pharmacy
关键词
阿司匹林
缓释胶囊
药物动力学
aspirine,sustained release capsule, pharmacokinetics