普鲁斯的明缓释片体外释放与体内吸收的相关性研究

Correlation Between in vitro Release and in vivo Absorption of Sustained-releasing Tablets of Neostigmine Bromide

目的评价普鲁斯的明缓释片体外释放和体内吸收之间的相关性。方法以水为溶出介质,测定普鲁斯的明缓释片的体外释放度,采用高效液相色谱法测定兔单剂量口服普鲁斯的明缓释片或普通片后的血药浓度,分别以Loo-Riegelman法计算体内吸收分数Fa和反卷积分法计算输入函数R。结果以体外累计释放度Y与Fa和R建立的回归方程分别为:Fa=0.9298Y+4.6074,r=0.9961;R=2.0163Y-11.242,r=0.9270。结论普鲁斯的明缓释片体外释放与体内吸收之间相关性良好。

Objective To determine the correlation between in vitro release and in vivo absorption of sustained-releasing tablets of neostigmine bromide. Methods Water was used as dissolution medium to measured in vitro release of neostigmine bromide. After a single oral administration of 100 mg neostigmine bromide to rabbits, the plasma concentrations of neostigmine bromide in the rabbits were determined by HPLC. The compartment model and deconvolution method were employed to explain the in vitro-in vivo correlation. Results Using Y as cumulative in vitro release and Fa as percentage of absorption, the regression equation was established： Fa = 0. 9298Y＋4. 6074,r=0. 9961. The input function of R=2. 0163Y-11. 242,r=0. 9270. Conclusion The correlation between in vitro release and in vivo absorption of neostigmine bromide is good.