盐酸奈福泮药物树脂缓释胶囊药物动力学

Pharmacokinetics of nefopan hydrochloride-resin complexes

目的考察盐酸奈福泮药物树脂缓释胶囊体内药物动力学情况。方法采用HPLC法测定了口服盐酸奈福泮药物树脂缓释后不同时刻家犬体内的血药浓度,并与口服盐酸奈福泮片的相比较。结果与市售片相比,盐酸奈福泮药物树脂缓释胶囊的血药浓度比较平稳,ρmax降低,Tmax后移。盐酸奈福泮药物树脂缓释胶囊相对于市售片的相对生物利用度为93.64%。结论盐酸奈福泮药物树脂缓释胶囊的体内药物释放情况表明其具有明显的缓释特征。说明采用离子交换树脂结合包衣工艺的方法来制备盐酸奈福泮的缓释制剂是可行的。

Objective To investigate the release profile of nefopam from the nefopan hydrochloride-resin complexes in vivo.Method The drug plasma concentration was determined by HPLC,in vivo release profiles of nefopam from the nefopan hydrochloride-resin complexes and the nefopan hydrochloride tablets were compared.Results Comparing with the nefopan hydrochloride tablets,the drug plasma concentration fluctuation of the nefopan hydrochloride-resin complexes was lower,while ρmax decreased and tmax being delayed.The relative bioavailability of the nefopan hydrochloride-resin complexes and the nefopan hydrochloride tablets was 93.64%.Conclusion The sustained release characteristics of nefopam from the nefopan hydrochloride-resin complexes is proved in vivo.It is showed that to prepare prolong-released preparation by using ion exchange and coating technology was feasible.