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海藻酸钠类型对壳聚糖-海藻酸钠原位成膜片释药的影响。

Effect of Sodium Alginate Type on Drug Release from Chitosan-Sodium Alginate-Based In Situ Film-Forming Tablets.

机构信息

School Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.

Application Development and Innovation, DuPont Nutrition and Health, New Century, USA.

出版信息

AAPS PharmSciTech. 2020 Jan 6;21(2):55. doi: 10.1208/s12249-019-1549-y.

Abstract

Natural polymers are promising as the carrier of matrix-based sustained release tablets but limited by their diversity in source and structure properties. Our previous studies found that chitosan (CS)- and alginate (SA)-based tablets can form self-assembled polyelectrolyte complex (PEC) film on the surface, which controlled drug release with a novel mechanism. To elucidate whether PEC-based sustained drug delivery system could weaken the influence of single-matrix material diversity on drug release behavior, taking theophylline as a drug model, the effect of SA structure properties, including viscosity, G/M ratio, SA salt type, and degree of esterification on drug release profiles, swelling, and erosion of CS-SA composite system was investigated. The results showed that the viscosity, G content, salt type, and esterification degree of SA had a remarkable influence on drug release when SA alone was used as a matrix, but little effect of these parameters on drug release was observed in CS-SA combination system. SA of low viscosity is superior in controlling drug release from CS-SA combination system. Potassium, magnesium salt of SA, and esterified SA can help form PEC of higher thickness with different swelling and erosion extent. In conclusion, this study demonstrated that drug release diversity due to SA structure difference can be well eradicated by using CS-SA combination system, which is a promising strategy to manufacture natural polymer-based products with constant quality.

摘要

天然聚合物作为基质型缓控释片剂的载体具有很大的潜力,但受到其来源和结构性质多样性的限制。我们之前的研究发现,壳聚糖(CS)和海藻酸钠(SA)基片剂可以在表面形成自组装聚电解质复合物(PEC)膜,这种膜具有一种新颖的控制药物释放的机制。为了阐明 PEC 为基础的缓控释给药系统是否可以减弱单一基质材料多样性对药物释放行为的影响,我们以茶碱为药物模型,考察了 SA 的结构性质(包括粘度、G/M 比、SA 盐的类型和酯化度)对 CS-SA 复合系统中药物释放、溶胀和侵蚀的影响。结果表明,当 SA 单独用作基质时,SA 的粘度、G 含量、盐的类型和酯化度对药物释放有显著影响,但在 CS-SA 复合系统中,这些参数对药物释放的影响很小。低粘度的 SA 更有利于控制 CS-SA 复合系统中药物的释放。SA 的钾盐、镁盐和酯化 SA 有助于形成具有不同溶胀和侵蚀程度的较厚 PEC。总之,本研究表明,通过使用 CS-SA 复合系统可以很好地消除由于 SA 结构差异导致的药物释放多样性,这是制造具有稳定质量的天然聚合物基产品的一种很有前途的策略。

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