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疏水性弱酸聚合物作为控制释放载体。

Hydrophobic weak acid polymers as controlled release carriers.

机构信息

Facultad de Ciencias Químicas e Ingeniería, Universidad Autónoma de Baja California, Calzada Universidad 14418, Parque Industrial Internacional, Tijuana, México.

出版信息

Pharm Dev Technol. 2012 Mar-Apr;17(2):170-6. doi: 10.3109/10837450.2010.529147. Epub 2010 Nov 4.

Abstract

Poly(carboxyalkyl methacrylates) were studied as a cationic-drug delivery system, at pH 6.8 and 8.0. Different polymer/drug complexes were used to prepare compressed tablets. By kinetics experiments, we have found that drug release is dependent on both the hydrophobicity of the whole complex and the pH of the environment. Furthermore, a mechanism of dissociation/erosion clearly describes the drug release from a complex formed by a polymer soluble at target pH; otherwise, a mechanism of dissolution/diffusion is depicted. Additionally, we have observed that hydrophilic fillers increase the drug release rate. Since our results using different polymer/drug complexes exhibit pH-sensitive drug release, we propose that the poly(carboxyalkyl methacrylates) have potential as a colon-specific drug-delivery system.

摘要

聚(羧酸酯甲基丙烯酸酯)被研究为一种阳离子药物传递系统,在 pH 值 6.8 和 8.0 下。使用不同的聚合物/药物复合物来制备压缩片剂。通过动力学实验,我们发现药物释放既依赖于整个复合物的疏水性,也依赖于环境的 pH 值。此外,解离/侵蚀的机制清楚地描述了从在目标 pH 值下可溶的聚合物形成的复合物中释放药物;否则,描述了溶解/扩散的机制。此外,我们观察到亲水性填充剂增加了药物释放速率。由于我们使用不同的聚合物/药物复合物的结果显示出 pH 敏感的药物释放,因此我们提出聚(羧酸酯甲基丙烯酸酯)具有作为结肠特异性药物传递系统的潜力。

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