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首页> 外文期刊>Current drug delivery >Improvement in chemical and physical stability of fluvastatin drug through hydrogen bonding interactions with different polymer matrices.
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Improvement in chemical and physical stability of fluvastatin drug through hydrogen bonding interactions with different polymer matrices.

机译：通过与不同聚合物基质之间的氢键相互作用，改善氟伐他汀药物的化学和物理稳定性。

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Solid dispersions of Fluvastatin with polyvinylpyrrolidone (PVP), eudragit RS100 (Eud), and chitosan (CS) as drug carrier matrices, were prepared using different techniques in order to evaluate their effect on Fluvastatin stability during storage. The characterization of the three different systems was performed with the use of differential scanning calorimetry (DSC) and wide angle X-ray diffractometry (WAXD). It was revealed that amorphization of the drug occurred in all of the solid dispersions of Fluvastatin as a result of drug dissolution into polymer matrices and due to physical interactions (hydrogen bonding) between the polymer matrix and Fluvastatin. This was established through the use of FTIR spectroscopy. SEM and micro-Raman spectroscopy showed that Fluvastatin was interspersed to the polymer matrices in the form of molecular dispersion and nanodispersion, too. The finding that completely different polymer matrices, used here as drug carriers, produce completely different dissolution profiles for each one of the solid dispersions, suggests that each matrix follows a different drug release mechanism. Hydrogen bonding interactions as in the case of CS/Fluva solid dispersions lead to controlled release profiles. All formulations were subjected to accelerated aging in order to evaluate Fluvastatin stability. From by-products analysis it was found that Fluvastatin is very unstable during storage and anti-isomer as well as lactones are the main formed by-products. On the other hand, solid dispersions due to the evolved interactions of their reactive groups with Fluvastatin provide a sufficient physical and chemical stability. The extent of interactions seems to play the most important role in the drug stabilization.
机译：使用不同的技术制备了氟伐他汀与聚乙烯吡咯烷酮（PVP），eudragit RS100（Eud）和壳聚糖（CS）作为药物载体基质的固体分散体，以评估其对氟伐他汀在储存过程中稳定性的影响。使用差示扫描量热法（DSC）和广角X射线衍射法（WAXD）对三个不同系统进行了表征。揭示了由于药物溶解到聚合物基质中以及由于聚合物基质和氟伐他汀之间的物理相互作用（氢键），氟伐他汀的所有固体分散体中都发生了药物的无定形。这是通过使用FTIR光谱确定的。扫描电镜和显微拉曼光谱表明，氟伐他汀也以分子分散和纳米分散的形式散布到聚合物基质中。发现完全不同的聚合物基质（在此用作药物载体）对每种固体分散体产生完全不同的溶出度的发现，表明每种基质遵循不同的药物释放机理。在CS / Fluva固体分散体中，氢键相互作用产生控释曲线。为了评估氟伐他汀的稳定性，将所有制剂进行加速老化。从副产物分析中发现氟伐他汀在储存过程中非常不稳定，抗异构体以及内酯是主要的副产物。另一方面，由于它们的反应性基团与氟伐他汀相互作用而形成的固体分散体具有足够的物理和化学稳定性。相互作用的程度似乎在药物稳定中起着最重要的作用。

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