双嘧达莫缓释微丸体内血药浓度及体外溶出度的相关性研究

Investigation on release of dipyridamole controlled release pellets i n vitro and in vivo and their correlation

目的 测定自制双嘧达莫缓释微丸的血药浓度 ,通过双嘧达莫缓释微丸的体外溶出度实验 ,利用统计学方法研究其体内外参数的相关性并提供质控方法。方法 采用改进的HPLC测定血浆药物浓度 ,释放度实验按中国药典 2 0 0 0年版附录中有关转篮法规定进行 ,以美国HansonResearch全自动溶出测定仪进行操作。结果 以药物累积吸收百分率Y与相应时刻的体外累积释放百分数X建立的一元线性回归方程为 :Y =1 0 .90 0 6 +1 .1 792X (r =0 .90 3 6) (P <0 .0 1 )。

OBJECTIVE: To determine the plasma levels of dipyridamole after oral administration and to study in vitro and in vivo correlation of dipyridamole controlled release pellets. METHOD: A rapid and sensitive RP-HPLC assay was modified for the determination of the drug levels in plasma. The dissolution was tested according to Chinese Pharmacopoeia 2000, using the first methed. RESULTS: The linear regressive equation was established between the absorption percentage in vivo and the accumulate dissolution percentage in vitro of dipyridamole as Y=10.9006 + 1.179 2X (r(=0.9036) (P<0.01). CONCLUSION: The results suggested that there was a significant correlation between the absorption in vivo and the dissolution in vitro of dipyridamole controlled release pellets.