Background

Nifedipine (NIF) is a 1,4-dihydropyridine, calcium channel blocker, widely used in the treatment of cardiovascular diseases. NIF is poorly soluble in water at room temperature. Biodegradable porous starch foam (BPSF) has great potential as a solid dispersion carrier and can improve the solubility of poorly water-soluble drugs like NIF.

Objective

To formulate and evaluate tablet formulation of nifedipine-loaded biodegradable porous starch foam to improve the solubility of the drug.

Methods

The physical properties and the dissolution profile of NIF/BPSF mixtures and tablets were investigated. The BPSF was prepared by using a solvent exchange method, and NIF was loaded using an immersion/solvent evaporation method. The samples were characterized using differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), and optical microscopy.

Results

The in vitro dissolution studies demonstrated the immediate release of NIF from the BPSF formulated tablets. The formulation containing a ratio of NIF:BPSF (1:10) gave around 70% drug release in 30 min as compared to the control NIF tablets that showed 11% drug release.

Conclusion

These results showed an increase in the drug release of NIF from BPSF as a carrier thereby supporting the mechanism of drug adsorption.

中文翻译：

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负载多孔淀粉泡沫基于纳米化的溶解度增强：硝苯地平片剂配方

背景

硝苯地平 (NIF) 是一种 1,4-二氢吡啶类钙通道阻滞剂，广泛用于治疗心血管疾病。NIF 在室温下难溶于水。可生物降解的多孔淀粉泡沫（BPSF）作为固体分散载体具有很大的潜力，可以提高NIF等水溶性差的药物的溶解度。

客观的

制定和评估负载硝苯地平的可生物降解多孔淀粉泡沫的片剂配方，以提高药物的溶解度。

方法

研究了 NIF/BPSF 混合物和片剂的物理性质和溶出曲线。BPSF 采用溶剂交换法制备，NIF 采用浸没/溶剂蒸发法加载。使用差示扫描量热法 (DSC)、傅里叶变换红外光谱 (FTIR)、粉末 X 射线衍射 (PXRD) 和光学显微镜对样品进行表征。

结果

体外溶出研究表明，NIF 从 BPSF 配制的片剂中立即释放。与显示 11% 药物释放的对照 NIF 片剂相比，含有比例 NIF:BPSF (1:10) 的制剂在 30 分钟内产生约 70% 的药物释放。

结论

这些结果表明，作为载体的 BPSF 中 NIF 的药物释放增加，从而支持药物吸附机制。