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壳聚糖的盐形式和分子量对壳聚糖基质片剂溶胀和药物释放的影响。

Impact of salt form and molecular weight of chitosan on swelling and drug release from chitosan matrix tablets.

机构信息

Faculty of Pharmaceutical Science, Burapha University, Chonburi 20131, Thailand.

出版信息

Carbohydr Polym. 2013 Aug 14;97(1):26-33. doi: 10.1016/j.carbpol.2013.04.073. Epub 2013 May 1.

Abstract

Magnetic resonance imaging (MRI) and gravimetric techniques were used to assess swelling and erosion behaviors of hydrophilic matrix tablets made of chitosan. The impact of salt form, molecular weight (MW) and dissolution medium on swelling behavior and drug (theophylline) release was studied. The matrix tablets made of chitosan glycolate (CGY) showed the greatest swelling in both acid and neutral media, compared to chitosan aspartate, chitosan glutamate and chitosan lactate. MRI illustrated that swelling region of CGY in both media was not different in the first 100 min but glassy region (dry core) in 0.1N HCl was less than in pH 6.8 buffer. The tablets prepared from chitosan with high MW swelled greater than those of low MW. Moreover, CGY can delay drug release in the acid condition due to thick swollen gel and low erosion rate. Therefore, CGY may be suitably applied as sustained drug release polymer or enteric coating material.

摘要

磁共振成像(MRI)和重量法技术被用于评估壳聚糖亲水基质片的肿胀和溶蚀行为。研究了盐形式、分子量(MW)和溶解介质对溶胀行为和药物(茶碱)释放的影响。与天冬氨酸壳聚糖、谷氨酸壳聚糖和乳酸壳聚糖相比,壳聚糖甘醇酸盐(CGY)制成的基质片在酸性和中性介质中具有最大的溶胀。MRI 表明,CGY 在两种介质中的溶胀区域在前 100 分钟没有差异,但在 0.1N HCl 中的玻璃态区域(干核)小于 pH 6.8 缓冲液。MW 较高的壳聚糖制备的片剂比 MW 较低的片剂溶胀更大。此外,CGY 可以由于厚的溶胀凝胶和低的侵蚀率而在酸性条件下延迟药物释放。因此,CGY 可能适合用作持续释放药物的聚合物或肠溶包衣材料。

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