目的研究氨茶碱被无创、定位释放于健康人胃肠道特定部位(近端小肠)内的药动学特征。方法用自主研制的消化道药物定位释放胶囊系统,将150mg氨茶碱无创、精确的定位释放在志愿者的近端小肠内,用TDx测定氨荼碱的血药浓度,计算机拟合房室模型并计算药动学参数。结果氨茶碱于志愿者近端小肠内定位释放的时效曲线符合一室模型,ρmax为3.6mg·L^-1,fmax为1.89h,t1/2为6.8h,AUC0-24为42.87mg·h·L^-1。结论氨茶碱于近端小肠定位释放后吸收很快且有很好的吸收。
OBJECTIVE To study the pharmacokinetic characteristics of aminophylline released at specific regions of the gastrointestinal tract of healthy volunteers ( the proximal small intestine) with a non-invasive manner. METHODS 150 mg Aminophylline was delivered in the proximal small intestine of healthy volunteers by RECOCATM capsule system. The concentration of aminophylline in serum was determined by TDx. The pharmacokinetic parameters were calculated using the 3P87. RESULTS The pharmacokinetic profile of aminophylline was fitted with an one compartment model after a single delivered dose of anainophylline( 150 mg) in upper small intestine of healthy volunteers. The main parameters were as follows : ρmax 3.6 mg·L^-1, tmax 1.89 h,t1/2 6.8 h, AUC0-24 42. 87 mg·h·L^-1. CONCLUSION The pharmaeokineties of aminophylline showed that there were rapid and good absorption in the proximal small intestine of healthy volunteers.