非诺贝酸胆碱盐缓释片的制备及体内外评价

Preparation and in vitro-in vivo Evaluation of Choline Fenofibrate Sustained-release Tablets

以HPMC K4M为凝胶骨架制备非诺贝酸胆碱盐缓释片。测定了自制缓释片和参比制剂(Trilipix)在不同介质(pH3.5、6.0和6.8磷酸盐缓冲液和水)中的释放行为。采用相似因子(2)法评价两种制剂体外释放行为的相似度。结果表明,自制品在pH 3.5磷酸盐缓冲液中2 h累积释放率低于10%,在其他3种介质中的释放行为与参比制剂相似(2值均大于50)。Beagle犬体内药动学研究表明,自制品与参比制剂生物等效。

The choline fenofibrate sustained-release tablets were prepared with HPMC K4M as the gel matrix. The in vitro release behaviors of the product and the reference capsules （Trilipix） in pH 3.5, 6.0 and 6.8 phosphate buffer （PBS） and water were determined. The similarity factor （f2） was calculated to evaluate the similarity of the two preparations. The results showed that the cumulative release of the product at 2 h in pH 3.5 PBS was below 10 %. While in other three media, the release behavior curves of the product were similar with the reference capsules because the f2 values were all above 50. The results ofpharmacokinetics in Beagle dogs showed that the product was bioequivalent to the reference capsules.