载盐酸齐拉西酮的具有黏膜黏附-漂浮特性的锌-果胶-桃胶互穿聚合物网络珠。
Mucoadhesive-floating zinc-pectinate-sterculia gum interpenetrating polymer network beads encapsulating ziprasidone HCl.
机构信息
Department of Industrial Pharmacy, Gokaraju Rangaraju College of Pharmacy, Bachupally, Hyderabad 500090, Andhra Pradesh, India.
Department of Industrial Pharmacy, Gokaraju Rangaraju College of Pharmacy, Bachupally, Hyderabad 500090, Andhra Pradesh, India.
出版信息
Carbohydr Polym. 2015 Oct 20;131:108-18. doi: 10.1016/j.carbpol.2015.05.042. Epub 2015 May 27.
A novel dual crosslinked low-methoxyl (LM) pectinate-sterculia gum (SG) interpenetrating polymer network (IPN) beads was developed for intragastric ziprasidone delivery. The IPN beads were accomplished by simultaneous ionotropic gelation with zinc acetate and covalent crosslinking with glutaraldehyde. The effects of pectin and SG contents on drug entrapment efficiency (DEE, %), and cumulative drug release after 8h (Q8, %) were studied to optimize the IPN beads using a 3(2) factorial design. The optimized beads encapsulating ziprasidone HCl (F-O) displayed DEE of 87.98±1.15% and Q8 of 58.81±1.50% with excellent buoyancy (floating lag time <2min, % buoyancy at 8h >63%) and good mucoadhesivity with the goat gastric mucosa. In most cases, the drug release behaviour obeyed Higuchi kinetics with anomalous transport mechanism. The Zn-pectinate-SG IPN beads were also characterized by SEM, FTIR, DSC and P-XRD analyses.
一种新型的双重交联低甲氧基（LM）结冷胶-葎草胶互穿聚合物网络（IPN）珠粒被开发用于胃内齐拉西酮递送。通过与乙酸锌的离子凝胶化和与戊二醛的共价交联同时完成 IPN 珠粒。使用 3(2)因子设计研究了果胶和 SG 含量对药物包封效率（DEE，%）和 8 小时后累积药物释放（Q8，%）的影响，以优化 IPN 珠粒。包封齐拉西酮盐酸盐的优化珠粒（F-O）显示 DEE 为 87.98±1.15%，Q8 为 58.81±1.50%，具有出色的漂浮滞后时间（<2 分钟）和良好的胃黏膜黏附性（8 小时时漂浮率>63%）。在大多数情况下，药物释放行为遵循 Higuchi 动力学和异常传输机制。Zn-结冷胶-葎草胶 IPN 珠粒还通过 SEM、FTIR、DSC 和 P-XRD 分析进行了表征。
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