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新型海藻酸盐水凝胶核壳系统用于盐酸雷尼替丁和醋氯芬酸的联合递送。

Novel alginate hydrogel core-shell systems for combination delivery of ranitidine HCl and aceclofenac.

机构信息

Department of Pharmaceutics, Gupta College of Technological Sciences, Asansol 713301, WB, India.

Department of Pharmaceutics, Gupta College of Technological Sciences, Asansol 713301, WB, India.

出版信息

Int J Biol Macromol. 2015 Mar;74:85-92. doi: 10.1016/j.ijbiomac.2014.11.027. Epub 2014 Dec 3.

DOI:10.1016/j.ijbiomac.2014.11.027
PMID:25478963
Abstract

A novel hydrogel system was successfully developed based on core-shell approach for the delivery of ranitidine HCl and aceclofenac. Aceclofenac-loaded alginate microspheres coated with eudragit L-100 was used as core material and that of freeze-thaw cross-linked chitosan-PVA gels containing ranitidine HCl served as the shell-forming material. The alginate microspheres coated with eudragit L-100 showed drug encapsulation efficiency of 56.06±1.12 to 68.03±2.16% and had average particle sizes of 551.29±25.92 to 677.18±27.05 μm. The viscosity of chitosan-PVA gels ranged between 505.74±1.04 and 582.41±2.09 cps. The formulations were characterized by FTIR, SEM and polarized microscopy analyses. The release of ranitidine HCl was comparatively higher in acidic medium (pH 1.2) than in alkaline medium (pH 7.4). The release of aceclofenac became slower in alkaline medium (pH 7.4) and continued up to 3.5 h. Super case-II transport mechanism was assumed for the release of ranitidine HCl in both media; whereas non-Fickian (anomalous) diffusion mechanism predominated in the release of aceclofenc. Thus, hydrogel-based core-shell formulations were found suitable for simultaneous delivery of aceclofenac and ranitidine HCl which could minimize the chances of excessive gastric acid secretion through suitable ranitidine HCl release in gastric region.

摘要

基于核壳方法成功开发了一种新型水凝胶系统,用于递送盐酸雷尼替丁和醋氯芬酸。用壳聚糖-PVA 冻融交联凝胶作为壳形成材料,包载醋氯芬酸的海藻酸钠微球作为核材料。包载 Eudragit L-100 的海藻酸钠微球显示出 56.06±1.12%至 68.03±2.16%的药物包封效率,平均粒径为 551.29±25.92μm 至 677.18±27.05μm。壳聚糖-PVA 凝胶的粘度在 505.74±1.04cps 至 582.41±2.09cps 之间。通过傅里叶变换红外光谱(FTIR)、扫描电子显微镜(SEM)和偏光显微镜分析对制剂进行了表征。盐酸雷尼替丁的释放速度在酸性介质(pH1.2)中明显高于碱性介质(pH7.4)。在碱性介质(pH7.4)中,醋氯芬酸的释放速度变慢,并持续了 3.5 小时。在两种介质中,盐酸雷尼替丁的释放被假设为超二级传输机制;而在醋氯芬酸的释放中,主要为非菲克(异常)扩散机制。因此,基于水凝胶的核壳制剂被认为适合同时递送醋氯芬酸和盐酸雷尼替丁,通过在胃区适当释放盐酸雷尼替丁,可以最大限度地减少胃酸分泌过多的机会。

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