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藻酸-黄蓍胶凝胶包被的油包埋藻酸盐珠用于胃滞留型利培酮给药。

Alginate-sterculia gum gel-coated oil-entrapped alginate beads for gastroretentive risperidone delivery.

机构信息

Department of Industrial Pharmacy, Gokaraju Rangaraju College of Pharmacy, Bachupally, Hyderabad 500090, India.

Department of Industrial Pharmacy, Gokaraju Rangaraju College of Pharmacy, Bachupally, Hyderabad 500090, India.

出版信息

Carbohydr Polym. 2015 Apr 20;120:74-84. doi: 10.1016/j.carbpol.2014.12.009. Epub 2014 Dec 19.

Abstract

Novel floating-mucoadhesive oil-entrapped alginate beads coated with crossslinked alginate-sterculia gum gel membrane was developed for gastroretentive risperidone delivery. Oil-entrapped alginate beads containing risperidone as core were prepared by ionotropic gelation technique. Effects of polymer to drug ratio and oil to water ratio on drug entrapment efficiency (%) and cumulative drug release after 8h (%) were studied to optimize the core beads by a 3(2) factorial design. The optimized beads (F-O) demonstrated drug entrapment efficiency of 83.73±0.81% and cumulative drug release of 70.84±0.27% after 8h. The biopolymeric-coated optimized beads exhibited excellent buoyancy, better ex vivo mucoadhesion and slower drug release rate. The drug release profiles of risperidone-loaded uncoated and coated beads were best fitted in Korsmeyer-Peppas model with Fickian diffusion mechanism. The beads were also examined for the drug-excipients compatibility, drug crystallinity and surface morphology by FTIR, P-XRD and SEM analyses, respectively.

摘要

开发了一种新型的漂浮型、粘膜粘附型、包被交联海藻酸钠-葎草胶凝胶膜的海藻酸钠包油微球,用于胃滞留型利培酮给药。采用离子凝胶化技术制备载有利培酮的海藻酸钠包油微球。通过 3(2) 析因设计,研究了聚合物与药物的比例和油与水的比例对药物包封效率(%)和 8 小时后累积药物释放(%)的影响,以优化载药微球。优化后的微球(F-O)在 8 小时后表现出 83.73±0.81%的药物包封效率和 70.84±0.27%的累积药物释放率。生物聚合物包被的优化微球表现出优异的漂浮性、更好的体外粘膜粘附性和更慢的药物释放速率。利培酮载药未包被和包被微球的药物释放曲线最符合 Korsmeyer-Peppas 模型,具有菲克扩散机制。还通过 FTIR、P-XRD 和 SEM 分析分别考察了微球的药物-赋形剂相容性、药物结晶度和表面形态。

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