溴吡斯的明磷脂复合物纳米乳体外溶出度与体内吸收的相关性

目的 采用Loo-Riegelman法评价溴吡斯的明磷脂复合物纳米乳(PPNE)体内外的相关性.方法 制备PPNE后,采用动态膜透析法研究PPNE体外释放行为,高效液相色谱法(HPLC)测定大鼠口服制剂后的血药浓度,以Loo-Riegelman法计算体内吸收百分数(Fa),并与体外累积释放率作线性回归.结果 PPNE的体外累积释放率(X)与体内Fa(Y)建立的线性方程为Y=1.376 9X-47.543 2,r=0.941 1,r大于相关系数临界值r(6.0.001) (P＜0.001).结论 PPNE体外释放与体内吸收之间具有良好的相关性.

Pyridostigmine bromide phospholipid complex nanoemulsion: correlation between dissolution in vitro and absorption in vivo

Objective To investigate the correlation between in vitro release and in vivo absorption of pyridostigmine bromide phospholipid complex nanoemulsion (PPNE) by Loo-Reieglman method. Methods PPNE was prepared and dynamic penetration system was used to analyze its in vitro release. The plasma concentration of pyridostigmine bromide was determined by HPLC after oral administration in rats. Loo-Riegelman method was employed to calculate the in vivo absorption percentage (Fa). Then the regression equation was established between absorption percentage and cumulative release. Results The regression equation was set up as follows: Y=1.376 9X-47.543 2, r=0.9411 (P<0.001). Y represented in vivo absorption percentage and X represented in vitro cumulative release rate. Conclusion There is a significant correlation between in vitro release and in vivo absorption of PPNE.