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阿莫西林控释型卡拉胶大珠的配方。

Formulation of controlled release gellan gum macro beads of amoxicillin.

机构信息

Department of Pharmacal Sciences, Harrison School of Pharmacy, Auburn University, AL 36849, USA.

出版信息

Curr Drug Deliv. 2010 Jan;7(1):36-43. doi: 10.2174/156720110790396445.

Abstract

Gellan gum has been reported to have wide pharmaceutical applications such as tablet binder, disintegrant, gelling agent and as a controlled release polymer. Multiparticulate delivery systems spread out more uniformly in the gastrointestinal tract and reduce the local irritation. The purpose of this study is to explore possible applicability of gellan macro beads as an oral controlled release system of a sparingly soluble drug, amoxicillin. Gellan gum beads were prepared by ionotropic gelation with calcium ions. The effect of drug loading, stirring time, polymer concentration, electrolyte (CaCl2) concentration, curing time etc. influencing the preparation of the gellan gum macro beads and the drug release from gellan gum beads were investigated in this study. Optimal preparation conditions allowed very high incorporation efficiency for amoxicillin (91%) The release kinetics of amoxicillin from gellan beads followed the diffusion model for an inert porous matrix in the order: 0.1 N HCl > phosphate buffer > distilled water. Change in curing time did not significantly affect the release rate constant, but drug concentration, polymer concentration and electrolyte concentration significantly affect the release rate of amoxicillin from the beads. The gellan macro beads may be suitable for gastro retentive controlled delivery of amoxicillin.

摘要

结冷胶已被报道具有广泛的药物应用,如片剂粘合剂、崩解剂、凝胶剂和控释聚合物。多颗粒给药系统在胃肠道中更均匀地分散,减少局部刺激。本研究旨在探索结冷胶大珠作为一种难溶性药物阿莫西林的口服控释系统的可能适用性。结冷胶珠通过离子凝胶化作用与钙离子形成。研究了药物负载量、搅拌时间、聚合物浓度、电解质(CaCl2)浓度、固化时间等因素对结冷胶大珠的制备和结冷胶珠中药物释放的影响。最佳的制备条件允许阿莫西林的包封效率非常高(91%)。阿莫西林从结冷胶珠中的释放动力学遵循惰性多孔基质的扩散模型,顺序为:0.1 N HCl > 磷酸盐缓冲液 > 蒸馏水。固化时间的变化不会显著影响释放速率常数,但药物浓度、聚合物浓度和电解质浓度显著影响阿莫西林从珠中的释放速率。结冷胶大珠可能适用于阿莫西林的胃滞留控释。

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