【摘要】 本文研制了炎痛喜康控释片,其体外溶出行为符合一级动力学过程,讨论了相关试验条件对体外溶出度的影响。服用炎痛喜康制剂后体内血浓用HPLC测定,其体内配置状态符合单室药动学模型,经计算机模型嵌合处理求得药动学参数,控释片(A)相对于普通片(B)的生物利用度为100.5%,体内外相关关系结果表明:体内吸收分数与累积释药百分率之间有较好的线性相关关系。与普通片相比,控释片对家兔胃的急性刺激性明显降低。更多还原

【Abstract】 A controlled release tablet of piroxicam (A) was developed. The drug dissolution behaviors can be described by the first order kinetecs. The factors influencing the drug dissolution were studied. Determination of piroxicam plasma concentrations was carried out by HPLC. The drug pharmacokinetic disposition can be well fitted by one compartment model. The parameters were estimated by using a non-linear regression computer program. Bioavailability of a relative to a conventional tablet (B) is 100.5%. The results of correlation test showed there is a good linear relationship between fraction absorbed in vivo and percentage cumulative dissolved in vitro. The results of acute irritation test in rabbits showed that the irritation of A in the stomach was significantly lower than that of B.更多还原