Tablets compressed with gastric floating pellets coated with acrylic resin for gastro retention and sustained release of famotidine: in-vitro and in-vivo study
Tablets compressed with gastric floating pellets coated with acrylic resin for gastro retention and sustained release of famotidine: in-vitro and in-vivo study
复制标题
胃漂浮小丸压片，涂有丙烯酸树脂，用于胃滞留和法莫替丁缓释：体外和体内研究
DOI：
10.1111/jphp.12339
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发表时间：
2015
影响因子：
3.3
通讯作者：
Wu Zhenghong
中科院分区：
文献类型：
--
作者：
Qi Xiaole;Jiang Yingchun;Zhang Huiting;Wu Zhenghong
目的制备一种以丙烯酸树脂为包衣材料的胃内漂浮微丸，以延长法莫替丁的胃内滞留时间，提高其口服生物利用度。采用挤出滚圆法制备了1：10：1的微球，用丙烯酸树脂包衣，然后与Avicel PH 301微丸和交联聚乙烯吡咯烷酮压片。采用Box-Behnken设计对包衣质量、Eudragit RL 30 D与RS30 D的体积比、包衣液固含量进行了优化，结果表明：在0.1M盐酸中，片剂能迅速崩解成微丸，微丸漂浮，释药时间可达12 h以上。法莫替丁胃漂浮微丸的AUC 0-∞大鼠给药后的释放度（7776.52 ± 1065.93 h ng/ml）显著高于市售速释片（中国上海兴义）（4166.23 ± 312.43 h ng/ml），相对生物利用度为187.01 ± 22.81%结论优化后的处方为胃内滞留和缓释提供了新的途径法莫替丁的口服吸收。
ObjectivesThe aim of this study was to prepare a disintegrating gastric floating tablet composed of floating pellets coated with acrylic resin to prolong the gastric residence time and increase the oral bioavailability of famotidine.MethodsThe gastric floating pellets containing famotidine, stearyl alcohol and microcrystalline cellulose (1 : 10 : 1) were prepared by extrusion–spheronization process and coated with acrylic resin, then compressed into tablets with Avicel PH 301 pellets and cross-linked polyvinylpyrrolidone. The coating weight, volume ratio of Eudragit RL30 D and RS30 D and solid content of coating fluid were optimized by Box–Behnken design.Key findingsIn 0.1 M HCl, tablets can immediately disintegrate into pellets which can remain floating and sustained drug releasing over 12 h. The AUC0-∞of famotidine gastric floating pellets (7776.52 ± 1065.93 h ng/ml) administered into rats was significantly higher than that of marketed rapid release tablets Xingfading® (Xingyi, Shanghai, China) (4166.23 ± 312.43 h ng/ml), while the relative bioavailability was 187.01 ± 22.81%.ConclusionsThe experimental results indicated that the optimized formulation did offer a new gastro retention and sustained release approach to enhance the oral absorption of famotidine.