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目的研究尼索地平醇质体控释贴剂的体外经皮渗透及在大鼠体内的药动学特征。方法采用Franz扩散池法进行体外透皮研究;采用HPLC法测定尼索地平的血药浓度,用3p87软件分析药动学参数。结果贴剂在体外经皮渗透的规律符合零级动力学模型;与口服给药相比,贴剂给药的血药浓度平稳,达峰时间延后,持效时间延长,相对生物利用度为242.32%。结论尼索地平控释贴剂具有显著控释特征,可较长时间维持稳定的血药浓度。
Objective To study the in vitro transdermal permeation of nisoldipine and its pharmacokinetic characteristics in rats. Methods Franz diffusion cell method was used to study the in vitro transdermal delivery. The plasma concentration of nisoldipine was determined by HPLC and the pharmacokinetic parameters were analyzed by 3p87 software. Results The transdermal patch in vitro was in accordance with the zero-order kinetic model. Compared with the oral administration, the plasma concentration of the patch was stable, the peak time was delayed and the sustained-effect time was prolonged. The relative bioavailability was 242.32%. Conclusion Nisoldipine controlled release patch has significant controlled release characteristics and can maintain stable plasma concentration for a long time.