Effect of drying methods on swelling, erosion and drug release from chitosan-naproxen sodium complexes
Effect of drying methods on swelling, erosion and drug release from chitosan-naproxen sodium complexes
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DOI：
10.1208/s12249-007-9001-0
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发表时间：
2008-03-01
影响因子：
3.3
通讯作者：
Kadam, Shivajirao S.
中科院分区：
文献类型：
--
作者：
Bhise, Kiran S.;Dhumal, Ravindra S.;Kadam, Shivajirao S.
本研究的目的是探讨纳米纤维素钠（NS）与壳聚糖（CH）之间的离子相互作用在托盘干燥法（TD）和喷雾干燥法（SD）制备复合物（NSC）中的应用。在透析研究的基础上优化了NSC中的药物-聚合物比例（1：1）。采用盘式干燥法和喷雾干燥法制备了NSC微粒体系。将缓释聚合物加入到NSC和含有NS-CH的物理混合物中，并比较它们在不同pH下对水吸收、基质侵蚀和药物释放的影响。喷雾干燥复合物（SDC）是球形的、自由流动的、轻的和细的无定形颗粒，与结晶的、硬的、坚韧的、不规则形状的、密度更大的托盘干燥复合物（TDC）形成对比，所述托盘干燥复合物具有差的流动性。差示扫描量热法（DSC），粉末X-射线衍射（PXRD）和傅里叶变换红外（FTIR）模式证实的转换结晶到高能量的非晶相适合离子相互作用在NSC。在NSC压块中存在释放阻滞聚合物、κ角叉菜胶和羟丙基甲基纤维素（HPMC）阻滞药物释放并改善基质完整性。角叉菜胶基质比HPMC片剂表现出更多的阻滞。FTIR图谱、侵蚀、溶胀和基质药物释放支持NSC中NS和CH之间的离子相互作用。在酸性pH下药物从壳聚糖基质中释放延迟的原因包括药物在酸性pH下的溶解度差、沿基质外围沿着形成限速聚合物凝胶屏障以及带相反电荷的部分之间的离子相互作用。
The purpose of this research was to explore theapplication of ionic interactions between naproxen sodium (NS) and chitosan (CH) in complexes (NSC) prepared by tray drying (TD) and spray drying (SD) methods. Drug-polymer ratio (1:1) in the NSC was optimized on the basis of dialysis studies. The particulate systems of NSC were prepared by tray drying (TD) and spray drying (SD) methods. Release retarding polymers were added to the NSC and to the physical mixtures containing NS-CH and their effects on water uptake, matrix erosion and drug release at different pH were compared. Spray dried complexes (SDC) were spherical, free flowing, light and fine amorphous particles in contrast to the crystalline, hard, tenacious, irregularly shaped, denser tray dried complexes (TDC) with poor flowability. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and Fourier transform infrared (FTIR) patterns confirm the conversion of crystalline to high energy amorphous phase suitable for ionic interactions in NSC. Presence of release retarding polymers, kappa carrageenan and hydroxypropylmethylcellulose (HPMC) in the NSC compacts retarded the drug release and improved the matrix integrity. Carrageenan matrices exhibited more retardation than HPMC tablets. FTIR patterns, erosion, swelling and drug release from matrices support ionic interactions between NS and CH in NSC. The reasons for retarded drug release from the chitosan matrices at acidic pH include poor solubility of drug at acidic pH, formation of a rate limiting polymer gel barrier along the periphery of matrices and the ionic interactions between oppositely charged moieties.