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Zero-order release by enzymatic degradation in matrix tablets of modified starch (contramid~direct R)

机译:改性淀粉基质片剂中酶促降解的零级释放(contramid〜direct R)

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The release of low solubility drugs from hydrophilic matrices has always been a challenge especially when zero-order profiels are desired. As it is the case also for drugs with pH dependant solubilities, diffusion mechanism alone falls short of giving linear release profiles. In such situations, a combination of diffusion and progressive matrix erosion was found most successful~1. Contramid being a starch based excipient~2, it can be degraded enzymatically by alpha-amylase at intestinal pH. The objective of this work was to demonstrate the potential of combining modified starch and alpha-amylase in a simple matrix tablet to release low solubility drugs following a zero-order kinetics.
机译:从亲水性基质中释放低溶解度的药物一直是一个挑战,尤其是在需要零级仿制药的情况下。与具有pH依赖性溶解度的药物一样,仅扩散机制就不能提供线性释放曲线。在这种情况下,发现扩散和渐进的基质侵蚀相结合最成功〜1。 Contramid是一种基于淀粉的赋形剂〜2,在肠道pH值下可以被α-淀粉酶酶促降解。这项工作的目的是证明在简单的基质片剂中结合变性淀粉和α-淀粉酶以遵循零级动力学释放低溶解度药物的潜力。

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