喘平缓释片体外释放与人体内吸收的相关性研究

Correlation between dissolution in vitro and absorption in vivo of Chuanping sustained release tablets

目的:研究喘平缓释片体外释放与人体内吸收的相关性。方法:以麻黄碱、伪麻黄碱为指标成分,体外采用转篮法结合HPLC测定喘平缓释片在不同pH介质中的累积溶出率;体内采用尿药法结合HPLC测定尿液中的药物浓度;应用Wagner-Nelson法评价喘平缓释片体内外相关性。结果:喘平缓释片人体内不同时间点的吸收百分数F与体外累积溶出率f的线性回归方程分别为F麻黄碱=1.572 5f-20.729(R2=0.974 5),F伪麻黄碱=1.237f-0.147 6(R2=0.959 5)。结论:喘平缓释片体内-体外相关性良好,体外释放度测定方法可用于控制喘平缓释片内在质量和预测其生物利用度。

Objective： To investigate the correlation between dissolution in vitro and absorption in vivo of Chuanping sustained release tablets. Method： The ephedrine, pseudoephedrine were chosen as marker components, dissolution in vitro of Chuanping sus- tained release tablets in the different pH were tested by the rotating basket method and HPLC;urine drug levels were determined by HPLC and absorption fractions were calculated according to Wagner-Nelson＇s formula and deconvolution technique. Result： The linear regressive equation between the absorption percentage in vivo F and accumulative release percentage in vitro of Chuanping sustained re- lease tablets was established as Fephedrine = 1. 572 5f= 20. 729（Rz =0. 974 5） ;Fpseudoephedrine = 1. 237f-0. 147 6（R2 =0. 959 5）. Con- clusion： The resuhs suggested that there was fine correlation between the absorption percentage in vivo and the accumulative release percentage in vitro of Chuanping sustained release tablets.