尼莫地平片体外溶出度与体内吸收的相关性研究

Study on correlation between dissolution in vitro and absorption in vivo of nimodipine tablets

目的 考察两种尼莫地平片体外溶出度与体内吸收的相关性。方法 按中国药典2000年版附录中转篮法测定尼莫地平片在人工胃液中的溶出度;8名男性健康志愿者口服尼莫地平片120mg,HPLC测定血药浓度,Loo-Reigelman法计算药物累积吸收分数。以药物累积吸收百分率或血药浓度(Y)对相应时刻的体外累积溶出百分率(X)进行回归。结果两种尼莫地平片体内吸收对体外溶出度回归方程分别为:Y=2.2304X-60.72,r=0.9983(P<0.01)和Y=3.7085X-107.41,r=0.8951(P<0.05)。结论两种尼莫地平片体外溶出度与体内吸收有显著的相关性。

OBJECTIVE To study the correlation between the diss,lulion in vitro and the absort）tion in vivo of nimodipine tablets. METHODS the dissolution of nimodipine in vitro was tested according to Chinese pharmacopoeia 2000, using the first method with RC disoyution tester. A single oral dose of nimodipine was given to 8 healthy male vohmteers. Nimodipine concentration in plasma were determined by HPLC and the absorption percentage was calculated according to Loo-Reigelman formula. RESULTS The linear regressive equation established between the absorption percentage in vivo and the dissolution percentage in vitro of nimodipine tablets were Y = 2. 230 4X - 60.72, r = 0.998 3（P 〈 0.01）and Y = 3.708 5X - 107.41, r = 0.895 1（ P 〈 0.05） ,respectively. CONCLUSION The results suggested that there was a significant eonetation between the absorption in vivo and the dissolution in vitro of nimodipine tablets.