山楂叶总黄酮缓释片的制备及Beagle犬体内外相关性研究

Preparation and in vitro-in vivo Correlation in Beagle Dogs of Hawthorn Leaves Flavonoids Sustained-release Tablets

以山楂叶总黄酮为模型药物,羟丙甲纤维素(HPMC)、乙基纤维素(EC)及丙烯酸树脂(EudragitL100)为混合骨架材料制备日服两次的缓释片,以牡荆素为指标成分,考察Beagle犬单剂量口服缓释片后的药代动力学特征。结果表明,本品缓释特征较好,体外释放较符合Weibull模型,本品体外释放度与Beagle犬体内药物吸收分数之间相关系数为0.98。

Twice a day sustained-release tablets were developed for the Hawthorn leaves flavonoids, using hydroxypropyl methylcellulose （HPMC）, ethylcellulose （EC） and Eudragit L100 as combined matrix materials. Pharmacokinetics of the tablets were investigated in Beagle dogs with vitexin as marker compound. Results showed that the prepared tablets possessed a good sustained-release characteristic. Weibull model was the optimal model for the description of drug release profile. The correlation coefficient between the fraction of absorption in vivo and the release rate in vitro was 0.98.