Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, Thailand.
Eur J Pharm Biopharm. 2011 Feb;77(2):320-6. doi: 10.1016/j.ejpb.2010.11.019. Epub 2010 Nov 30.
Magnetic resonance imaging (MRI) was used to assess in situ swelling behaviors of spray-dried chitosan acetate (CSA) in 0.1N HCl, pH 6.8 and pH 5.0 Tris-HCl buffers. The in vitro drug releases from CSA matrix tablets containing the model drugs, diclofenac sodium and theophylline were investigated in all media using USP-4 apparatus. The effect of chitosan molecular weight, especially in pH 6.8 Tris-HCl, was also studied. In 0.1N HCl, the drug release from the matrix tablets was the lowest in relation to the highest swelling of CSA. The swelling kinetics in Tris-HCl buffers are Fickian diffusion according to their best fit to Higuchi's model as well as the drug release kinetics in all the media. The high swelling rate (k(s)(')) was found to delay the drug release rate (k'). The linear relationship between the swelling and fractions of drug release in Tris-HCl buffers was observed, indicating an important role of the swelling on controlling the drug release mechanism. Additionally, CSA of 200 and 800 kDa chitosan did not swell in pH 6.8 Tris-HCl but disintegrated into fractions, and the drug release from the matrix tablets was the highest.
磁共振成像(MRI)用于评估喷雾干燥醋酸壳聚糖(CSA)在 0.1N HCl、pH6.8 和 pH5.0 三羟甲基氨基甲烷盐酸缓冲液中的原位溶胀行为。采用 USP-4 装置在所有介质中研究了含有模型药物双氯芬酸钠和茶碱的 CSA 基质片剂的体外药物释放情况。还研究了壳聚糖分子量的影响,特别是在 pH6.8 三羟甲基氨基甲烷盐酸缓冲液中。在 0.1N HCl 中,与 CSA 的最高溶胀相比,基质片剂中药物的释放最低。在 Tris-HCl 缓冲液中的溶胀动力学符合 Higuchi 模型的最佳拟合,为菲克扩散,以及所有介质中的药物释放动力学。发现高溶胀率(k(s)('))会延迟药物释放率(k')。在 Tris-HCl 缓冲液中观察到溶胀与药物释放分数之间的线性关系,表明溶胀在控制药物释放机制方面起着重要作用。此外,分子量为 200 和 800 kDa 的 CSA 在 pH6.8 三羟甲基氨基甲烷盐酸缓冲液中不溶胀,而是分解成碎片,并且基质片剂中的药物释放量最高。