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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。
In this study, aspirin floating sustained-release capsules (A-HBSC) were developed by using the principle of fluid dynamic equilibrium system (HBS). The dissolution rate in vitro and the pharmacokinetics in rabbits were studied. In vitro dissolution of A-HBSC is a zero-order kinetic process, K ° a = 9.21% / h (t≤8h); the absorption rate of 0 ~ 8h in vivo accords with the apparent zero good kinetic process, .51% / h. There was a significant correlation between in vivo and in vitro data (r = 0.9917, P <0.01). In vivo pharmacokinetics study showed that A-HBSC slow release effect is obvious after administration of plasma concentration is relatively smooth, long duration of action, can reduce the number of dosing; and A-HBSC with light auxiliary materials with floating performance, slow release , Helps to reduce the gastrointestinal irritation and other adverse reactions.